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  • Spektralphotometrie  (167)
  • bioavailability  (65)
  • pheromone  (60)
  • Springer  (292)
  • American Association for the Advancement of Science
  • Cambridge University Press
  • 1975-1979  (292)
Collection
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  • Springer  (292)
  • American Association for the Advancement of Science
  • Cambridge University Press
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 293-299 
    ISSN: 1432-1041
    Keywords: Rifampicin ; p-aminosalicylic acid ; bentonite ; drug interaction ; bioavailability ; drug adsorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability (plasma concentrations, AUC and urinary excretion) of an oral solution of rifampicin was investigated in six healthy volunteers. Simultaneous administration of PAS granules produced a significant decrease in the absorption of RMP, whereas Na-PAS tablets had no effect. This indicated that the dosage form of the granules and not PAS itself was responsible for the interaction, and that the dissolution of RMP was not involved. The interaction could be reproduced by giving dummy granules that contained the same excipients but no PAS. The disintegration and dissolution of PAS granulesin vitro correlated well with the disappearance of RMP from the solution. The major excipient of the granules, bentonite (a mineral closely related to kaolin), was found to adsorb rifampicin rapidly and strongly.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 365-370 
    ISSN: 1432-1041
    Keywords: Particle size ; bioavailability ; digoxin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of digoxin in three tablets prepared from materials with different particle sizes was measured in healthy volunteers in a cross-over study using an alcoholic solution of digoxin as a reference standard. Its bioavailability in tablets with particle sizes of 7 µ or 13 µ was 78–97% of that of digoxin in solution. The tablet with largest particle size (102 µ) showed markedly lower bioavailability than the reference solution, namely 39%. It is obvious that particle size is an important determinant of the dissolution rate and bioavailability of digoxin.
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  • 3
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    European journal of clinical pharmacology 9 (1975), S. 209-212 
    ISSN: 1432-1041
    Keywords: Anticonvulsants ; phenytoin ; diphenylhydantoin ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma phenytoin levels were measured in 60 patients under steady-state conditions for a period of six weeks. During the trial, the preparation of phenytoin was changed from Phenytoin BP (Regent) to Epanutin Infatabs. A significant increase in plasma phenytoin levels following the change of tablet was matched by a decrease in the number of seizures.
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  • 4
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    European journal of clinical pharmacology 9 (1975), S. 213-218 
    ISSN: 1432-1041
    Keywords: Phenytoin ; diphenylhydantoin ; anticonvulsants ; bioavailability ; drug absorption ; generic inequivalence
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In order to evaluate the bioavailability of four different brands of phenytoin (diphenylhydantoin, DPH) tablets single doses of 600 mg DPH in acid form were given to six volunteers in a cross-over study. A micronized DPH-acid suspension was used as the reference standard. Significant differences between various products were found. The areas under the serum DPH concentration-time curves (AUC) were 26, 59, 68 and 90 per cent of the AUC of the DPH suspension. The peak serum DPH concentrations using the different tablets were 24, 54, 55 and 80 per cent of the peak value of the DPH suspension. It is likely that the differences in bio-availability of the DPH tablets are of clinical significance.
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  • 5
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    European journal of clinical pharmacology 9 (1976), S. 315-317 
    ISSN: 1432-1041
    Keywords: Tolamolol ; bioavailability ; maximum exercise tachycardia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Bioavailability of capsule and tablet formulations of tolamolol were compared by measuring plasma concentration of tolamolol and reduction in maximum exercise heart rate over a period of twelve hours in eight healthy subjects in a two-way cross-over study. Tolamol was absorbed more rapidly from capsules than from tablets; this did not result in any significant difference in the reduction in maximum exercise heart rate between the two formulations. There was no significant difference between area under curve of reduction in exercise tachycardia and area under curve of plasma concentration of tolamolol for the two formulations. Reduction in maximum exercise heart rate was related to logarithm of plasma concentration of tolamolol between two and twelve hours after both formulations.
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  • 6
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    European journal of clinical pharmacology 9 (1976), S. 373-379 
    ISSN: 1432-1041
    Keywords: Methyldigoxin ; repetitive doses ; bioavailability ; deep compartments ; oral and i.v. dose ; volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary To obtain true half lives, glycoside elimination from six healthy subjects was studied for 14 days after multiple intravenous doses or oral administration of a daily maintenance dose of β-methyldigoxin 0.3 mg. After oral or intravenous administration of β-methyldigoxin ceased, the plasma concentrations declined from the 14th to the 16th days with a half life of 1.7 days. From the 16th to the 20th day a change from a shorter to a longer half life of 2.8 and 2.9 days was observed. Similar half lives were found in urine: after the last dose the initial slope from the 14th to the 16th day had a half life of 1.8 days, and the terminal slope had one of 3.2 days. The results indicate release of the glycoside from slowly equilibrating tissues.
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  • 7
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    European journal of clinical pharmacology 8 (1975), S. 371-376 
    ISSN: 1432-1041
    Keywords: Digoxin ; bioavailability ; plasma levels ; cumulative urinary excretion ; particle size ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Various brands of digoxin tablets, and even different batches of one brand, may differ greatly in bioavailability. Digoxin-Sandoz® tablets have been compared with Lanoxin® manufactured between 1969 and 1972 and after May 1972. Comparisons were also made between and within batches of Digoxin-Sandoz tablets. Three separate cross-over studies were conducted involving a total of 20 volunteers. Digoxin-Sandoz tablets were shown to have a constant bioavailability and to produce plasma concentrations very similar to “new” Lanoxin. Storage for 2 years of one batch of Digoxin-Sandoz did not alter the bioavailability. Particle size was shown to influence bioavailability. Care should be exercised when plasma data alone are interpreted as an index of bioavailability. Measures of bioavailability based on plasma data obtained up to 6 h after administration differed from those based on cumulative urinary excretion data (in this study by a factor of about 2), which can lead to the belief that a difference in bioavailability is much greater than is actually the case. Data from cumulative urinary excretion, collected over a sufficiently long period of time, are likely to be the most reliable method for determining the bioavailability of a substance such as digoxin.
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  • 8
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    European journal of clinical pharmacology 16 (1979), S. 211-215 
    ISSN: 1432-1041
    Keywords: fluoride ; bioavailability ; calcium
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of milk products on the gastrointestinal absorption of fluoride from sodium fluoride tablets was studied in five healthy subjects. Two different diets were tested: (1) 250 ml standardized milk (3% fat) and (2) 500 ml of milk, 3 pieces of white bread with cheese and 150 ml of yoghurt. The 100% bioavailability of sodium fluoride tablets during fasting was greatly decreased by coadministration of milk products: with Diet 1 the absolute bioavailability calculated from combined plasma and urine data was in the range 50–79% and with Diet 2 it ranged from 50–71%. It is suggested that the decreased bioavailability produced by dairy products should be taken into account when establishing fluoride dosage regimens for prophylaxis of caries.
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  • 9
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    European journal of clinical pharmacology 10 (1976), S. 231-236 
    ISSN: 1432-1041
    Keywords: Digoxin ; beta-methyl-digoxin ; capsules ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The intestinal absorption and urinary elimination rate of total cardioactive material was compared following digoxin and beta-methyldigoxin (BMD) administration to twelve healthy volunteers. Significantly more injected digoxin was recovered in urine. Urinary clearance was more rapid for digoxin, mean half-lives of elimination being 35 hours for digoxin and 40 hours for BMD. Calculated percentage intestinal absorption was lowest for digoxin tablets with a dissolution rate of 77% in one hour, intermediate for BMD tablets, and maximal for an experimental soft gelatin formulation of digoxin in solution. Respective mean values were 75%, 87% and 97%. Similar steady state plasma concentrations followed twice daily ingestion of the 0.25 mg digoxin tablets and 0.20 mg BMD tablets. Mean peak plasma concentration and percentage urinary recovery of ingested dose were higher during continued BMD administration. Between-subject variation in absorption was higher for the digoxin tablets. The comparative intestinal absorption of BMD and digoxin depends upon the formulation. Digoxin is virtually completely absorbed from a solution encapsulated in soft gelatin. Relatively more BMD is eliminated by nonrenal routes.
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  • 10
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    European journal of clinical pharmacology 10 (1976), S. 251-256 
    ISSN: 1432-1041
    Keywords: Sisomicin ; pharmacokinetics ; bioavailability ; two-compartment analysis ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of sisomicin, a new single component aminoglycoside antibiotic related to gentamicin c1a, were determined in four healthy volunteers after intravenous and intramuscular administration of a 1 mg/kg dose. The elimination profile of this antibiotic follows two-compartment model kinetics after I.V. administration. The fast (α) and slow (β) disposition rate constants averaged 0.072 and 0.004 min−1, respectively. The volume of distribution at the steady-state averaged 0.185 liters/kg which approximately corresponds to the volume of extracellular space. The physiological availability of an intramuscular dose appeared to be complete. A method of administration adapted to the kinetic properties of the drug is proposed.
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  • 11
    ISSN: 1432-1041
    Keywords: Cefoxitin ; lidocaine ; intramuscular ; bioavailability ; pain
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The use of lidocaine HCl solution at concentrations of 0.5 and 1.0% to reconstitute sodium cefoxitin relieves the pain associated with intramuscular injections of the antibiotic. Cefoxitin absorption by the intramuscular route is initially rapid and is virtually complete. Peak serum concentrations, corresponding to about one-half those of a comparable intravenous infusion, are achieved in 30 min. Continuing absorption tends to maintain higher serum concentrations for longer times. Renal clearance and serum half-life of cefoxitin do not appear to be affected by lidocaine at its effective anaesthetic concentrations.
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  • 12
    ISSN: 1432-1041
    Keywords: p-Chlorophenoxyisobutyric acid ; clofibrate ; steady-state plasma concentrations ; bioavailability ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma concentrations and bioavailability of clofibrinic acid have been estimated under conditions approaching the steady-state during a ten-day period of administration as clofibrate or as a calcium clofibrinate-carbonate combination (1:1 w/w) at a dosage interval of 12 h. Formulation — related differences in bioavailability were not significant, and the 95% confidence limits of these differences were within −2% to +8% of the mean for the reference formulation of clofibrate. The mean steadystate plasma concentrations of clofibrinic acid measured on the tenth day of dosing were 116 µg/ml±22 S.D. and 119 µg/ml±23 S.D. after administration of 885 mg as clofibrate and the calcium clofibrinate-carbonate combination respectively. The peaks of mean plasma concentrations were 70 µg/ml±15 S.D., 119 µg/ml±32 S.D. and 131 µg/ml±26 S.D. on the first, fifth and tenth day of dosing with clofibrate, and 62 µg/ml±13 S.D., 127 µg/ml±S.D. and 143 µg/ml±25 S.D. on the corresponding days of dosing with the calcium clofibrinate-carbonate combination. After the last dose on the tenth day of dosing, the mean apparent half-lives of elimination of clofibrinic acid from plasma were 24.2 h±4.4 S.D. and 25.5 h±3.2 S.D. after administration of clofibrate and the calcium clofibrinate-carbonate combination respectively.
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  • 13
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    European journal of clinical pharmacology 13 (1978), S. 125-128 
    ISSN: 1432-1041
    Keywords: bioavailability ; diuretics ; gastrointestinal absorption ; hydrochlorothiazide ; thiazides ; food effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Hydrochlorothiazide (hct) 75 mg was administered orally to eight healthy volunteers without (Study I) or together with a standardized meal (Study II), and plasma and urine concentrations of hct were analyzed by GLC. The plasma levels of hct were higher initially when the tablets were taken on an empty stomach, but after 5 h they were higher in Study II. There was no difference between the two studies in the area under plasma concentration time curves. The urinary recovery of hct totalled 55.6±4.9 mg when the drug was given with food and 47.4±6.0 when it was taken on an empty stomach. The difference is significant (p〈0.01). As the urinary recovery represents the uptake of hct, it appears that the gastrointestinal absorption of hct is enhanced when the drug is given with food.
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  • 14
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    European journal of clinical pharmacology 10 (1976), S. 257-262 
    ISSN: 1432-1041
    Keywords: Anti-inflammatory and analgesic drug ; indoprofen ; pharmacokinetics ; bioavailability ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a pharmacokinetic study of the new analgesic and anti-inflammatory drug indoprofen, plasma levels and urinary excretion were determined in four healthy volunteers after 100 mg and 200 mg iv, and after 100 mg (capsules) and 200 mg (tablets) oral doses. After iv administration, the mean biological half-life (t1/2 β) was about 2 h (range 1.4 to 3.2 h). The apparent volume of distribution Vdβ ranged between 11 to 17 % of body weight, indicating its limited extravascular distribution. Most of the drug was excreted in urine as glucuronide and a smaller proportion as unchanged indoprofen: the 24 h urinary excretion of these compounds accounted for 67 to 95 % of an iv dose. Peak plasma levels occurred between 30 and 120 minutes after oral administration of 100 mg as capsules or 200 mg as tablets. The mean biological half-life was about 2 h, as after iv administration. The bioavailability of oral doses was assessed using both plasma levels and urinary excretion data. The absorption of capsules and tablets was practically complete, that of the former being faster.
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  • 15
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    European journal of clinical pharmacology 10 (1976), S. 101-108 
    ISSN: 1432-1041
    Keywords: Cardiac glycosides ; methyl proscillaridin ; plasma concentrations ; electrocardiogram ; bioavailability ; 86Rb-erythrocyte assay
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The aim of this study was to obtain data about the pharmacological properties of a new glycoside derivative in man. Plasma concentrations and ECG parameters were measured after oral and intravenous administration of a single dose of 1.2 mg methyl proscillaridin in 16 healthy volunteers, using a strictly randomized, two-period change-over design. Glycoside concentrations were measured using a modified86Rb-erythrocyte-assay. QT-duration, corrected for frequency (QTc), was the principal variable measured in the ECG. By either route, there was a maximum plasma level after 1 hour, which had decreased to a minimum at 3 hours, followed by a second peak at 4 to 10 hours (orally〉iv). From 10 to 72 hours the concentrations decreased with a median t 1/2 of 23.3 hours (iv) and 33.0 hours (orally). Comparison of the ratio of plasma concentrations following oral and iv administration resulted in a bioavailability of 69 % using the 48 hour plasma levels, and 59 % using the areas under the concentration-time curves. The mean QTc was maximally shortened to 28 msec at 1 hour after iv and to 19 msec at 10 hours after the oral dose. A distinct similarity between time-concentration and time-QTc curves was seen after the initial distribution phase, both after oral and intravenous administration. The new derivative shows a rapid elimination. Its bioavailability is reasonably high.
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  • 16
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    European journal of clinical pharmacology 16 (1979), S. 417-421 
    ISSN: 1432-1041
    Keywords: theophylline ; aminophylline ; bioavailability ; rapidly dissolving tablet
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of a rapidly dissolving tablet of theophylline and three brands of standard aminophylline tablets was estimated in a four way cross-over study involving 8 healthy adult volunteers. The relative extent of bioavailability as assessed by the measurement of the total area under the plasma concentration time curves showed no difference between the products (P〉0.05). Computed estimates of the rate of drug absorption were similar for all 4 products tested. The results indicate that the rapidly dissolving tablet offers no advantage in respect to rate and extent of absorption over conventional aminophylline tablets.
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  • 17
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    European journal of clinical pharmacology 12 (1977), S. 69-72 
    ISSN: 1432-1041
    Keywords: Metronidazole ; serum concentration ; bioavailability ; food intake ; healthy subjects ; Crohn's disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The possible influence of food intake on the bioavailability of metronidazole was examined in ten healthy volunteers by administration of a single dose of metronidazole on an empty stomach, and with a standardized breakfast. Food intake did not significantly alter the bioavailability of metronidazole. The interindividual variation in bioavailability appeared to be slight. In nine patients with Crohn's disease, the absorption of metronidazole appeared to be reduced and to be more variable than in healthy subjects. In both groups there was a clear relationship between the amount absorbed and dose/kg body weight. Thus, from the pharmacokinetic point of view, metronidazole can safely be given either with or between meals. The dose should be related to body weight.
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  • 18
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    European journal of clinical pharmacology 12 (1977), S. 285-290 
    ISSN: 1432-1041
    Keywords: Phenytoin acid ; phenytoin calcium ; bioavailability ; inequivalence of generics ; normal subjects ; volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Serum phenytoin concentrations have been studied in epileptic patients and healthy subjects taking tablets of phenytoin calcium (Desitin), A, phenytoin acid (Desitin), B, and phenytoin acid (Nordmark), C. Retrospective data and prospective investigation of hospitalized patients on long-term phenytoin treatment showed that significantly higher serum concentrations of phenytoin were produced by the phenytoin acid preparations B and C than by the phenytoin calcium preparation A. In a cross over study six volunteers received 200 mg/day of preparations A, B, and C for three weeks. In this study, too, higher phenytoin serum concentrations were produced by B and C than by A, although the differences were not statistically significant. The reasons for the discrepancies between the studies in healthy and epileptic subjects are discussed.
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  • 19
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    European journal of clinical pharmacology 12 (1977), S. 383-386 
    ISSN: 1432-1041
    Keywords: Benzodiazepine ; temazepam ; pharmacokinetics ; bioavailability ; hard and soft gelatine capsules
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma levels of temazepam were determined in healthy subjects after single oral administration of soft and hard gelatin capsules, and after 7 consecutive night-time doses in soft capsules. Absorption from soft gelatin capsules was significantly faster and produced earlier and higher peak plasma levels. The two pharmaceutical forms did not show any significant difference in relative availability. The apparent half-life of temazepam after night-time administration was significantly shorter than after morning administration, but no change in half-life was observed between the first and seventh night-time doses.
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  • 20
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    European journal of clinical pharmacology 14 (1978), S. 253-259 
    ISSN: 1432-1041
    Keywords: Pseudoephedrine ; side effects ; bioavailability ; multiple oral dosing
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Dose tolerance and pharmacokinetic studies of pseudoephedrine sustained action capsules were performed in thirty-three adult male subjects who received either 120 mg or 150 mg capsules every twelve hours for seven consecutive days in a double-blind parallel design study. Although only one subject in the 150 mg group was discontinued prematurely from this study, a large number of side effects typical of CNS stimulation were seen. A placebo effect might account for a portion of these complaints, however symtoms evaluated as being due to drug were significantly more severe and persistent in the 150 mg group. Pulse rates showed a persistent and significant increase while systolic and diastolic blood pressure fell from the baseline values in both groups. A pharmacokinetic analysis of the pseudoephedrine plasma concentration-time data provided estimates of half-life and the volume of distribution/availability ratio. The values obtained were in good agreement with values reported by others. Half-life was not influenced by urine pH probably as a result of the narrow range of urine pHs observed in the subjects. Calculations of relative bioavailability suggest that the 120 mg capsule formulation has a 30% greater bioavailability compared to the 150 mg capsule.
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  • 21
    ISSN: 1432-1041
    Keywords: chlorthalidone ; pharmacokinetics ; oral and i.v. doses ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Seven normal human volunteers each received a constant-rate infusion of chlorthalidone for 2 h, and the same (commonly 50 mg) single oral dose on separate occasions. The concentration of unchanged chlorthalidone was analyzed over a 100 to 220 h period in plasma, red blood cells, urine and faeces after both dosage forms. A three compartment model was required to describe the intravenous plasma concentrations in five of the subjects. A two compartment model sufficed to account for the decay of the oral plasma concentrations in all seven subjects. The mean plasma t1/2 after i.v. dosing was 36.5 h (±10.5 SD), and the mean plasma t1/2 after oral doses was 44.1 h (±9.6 SD). The mean red blood cell concentration t1/2 after i.v. doses was 46.4 h (±9.9 SD), and the mean red blood cell t1/2 after the oral doses was 52.7 h (±9.0 SD). The shorter i.v. half-live was not equally manifest in all subjects, being mainly apparent in three of them. In all cases the urinary excretion rate plots were parallel to the plasma concentration curves. As the faster decay after i.v. administration was not accompanied by increased renal clearance, the difference must have been due to non-renal mechanism. The mean total of 65.4 (±8.6 SD) % of the intravenous dose was excreted in urine over infinite time, whereas the mean total excretion after the oral dose was 43.8 (±8.5 SD) %. Faecal excretion ranged from 1.3–8.5% of dose in the i.v. study to 17.5–31.2% of dose in the oral study. The sum of the amounts present in urine plus faeces pointed strongly to an important metabolic route of elimination of chlorthalidone. Bioavailability estimates (F) from three sets of data were — a mean F of 0.61 from plasma concentrations, 0.67 from urinary excretion measurements and 0.72 from the erythrocyte concentrations. Simulations with a non-linear model indicated lesser validity of the estimate from erythrocyte concentrations. It was concluded that the average of plasma and urine data, F=0.64, yielded the best estimate of the oral availability of chlorthalidone 50 mg in man.
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  • 22
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    European journal of clinical pharmacology 16 (1979), S. 31-38 
    ISSN: 1432-1041
    Keywords: bezafibrate ; hyperlipoproteinemia ; bioavailability ; pharmacokinetics ; GC-MS
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition kinetics of bezafibrate, a newly developed drug of great lipid-lowering potency, were investigated in normal male subjects. Five male volunteers received14C-labelled bezafibrate orally in solution, and a further 10 were given the same dose (300 mg) of un-labelled drug as tablets. The concentration of bezafibrate in serum and urine from the latter was determined by GC, and in the former total radioactivity in serum, urine and feces was followed for 48 h, and urinary excretion products were analysed by TLC and GC-MS. Rapid absorption from the gastrointestinal tract led to peak serum levels 30 min and 2 h after administration of solution and tablets, respectively. Since approximately 95% of the administered14C-bezafibrate was excreted in urine within 48 h, and almost all the remainder was detected in feces, absorption can be regarded as complete after administration in solution. The relative optimal bioavailability from the tablets was also complete, since in both cases approximately 50% of the administered dose was detected as unchanged bezafibrate in urine within 24 h by GC in the tablet study, and by TLC in the solution study. Of the decomposition products, more than 20% of the dose was present as glucuronides and the remainder consisted of several more polar compounds, one of which was identified as a hydroxyderivative of bezafibrate. Since the apparent halflife of bezafibrate in serum was 2.1 h, this new drug possesses favourable pharmacokinetic features: rapid and complete absorption, even from tablets, combined with a conveniently short half-life, and clearance which is half renal (56 ml/min) and half metabolic (43 ml/min), giving a total clearance of 99 ml/min.
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  • 23
    ISSN: 1432-1041
    Keywords: indobufen ; platelet aggregation ; single dose ; bioavailability ; pharmacodynamics ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six healthy volunteers received single iv and oral doses of 2-[p-(1-oxo-2-isoindolinyl)phenyl] butyric acid 100 mg (indobufen; K 3920), an inhibitor of platelet aggregation. Plasma levels and urinary excretion of the drug were determined by GLC. Collagen-induced platelet aggregation was assessed turbidimetrically at various intervals after administration. The plasma half-life of the drug was 7–8 h and more than 70% of the administered dose was recovered within 48 h in urine, as unchanged drug and as the glucuronide of indobufen. After oral administration of tablets of two different formulations, the drug was completely absorbed, but one formulation showed faster absorption. The maximal inhibitory effect on platelet aggregation was observed 1 to 4 h after iv administration, and it had decreased by 8 h. After tablets, peak effect and the time of the peak were similar, but activity was significantly prolonged, in accordance with the higher plasma levels found at 8 h. The data suggest that the effect of indobufen on platelets is reversible, and that for this drug platelets behave as a compartment that slowly equilibrates with plasma.
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  • 24
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    European journal of clinical pharmacology 16 (1979), S. 45-48 
    ISSN: 1432-1041
    Keywords: quinidine ; slow release formulation ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of quinidine in two sustained release preparations A and B has been compared in three females and three males with i.v. administration of quinidine. The initial rate of oral absorption did not differ between the two drug preparations; the peak concentration was observed after 4 h both for A and B, but was significantly higher after B. A slower decrease in plasma concentration was observed after preparation A than B. Absolute bioavailability did not differ significantly between A (median value 78.4%) and B (median 87.1%). Drug absorption in vivo was in good agreement with the results of in vitro dissolution tests on both preparations. The slower decrease in plasma concentration found for the new sustained release form of quinidine should be of clinical advantage.
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  • 25
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    European journal of clinical pharmacology 10 (1976), S. 183-187 
    ISSN: 1432-1041
    Keywords: Hydralazine ; bioavailability ; pharmacogenetics ; first pass effect ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After oral administration of a single 50 mg dose of hydralazine (Apresoline®), the serum half-life (T1/2) and bioavailability (AUC0−∞) were assessed in 16 healthy volunteers. The half-life was 2.57±0.14 h (S.E.) in 10 slow acetylators of sulphadimidine, and 2.18±0.15 h in 6 fast acetylators (difference not statistically significant). AUC0−∞ was significantly higher in slow acetylators, at 1.04±0.10 µg·hour·ml−1, compared to 0.66±0.12 µg·hour·ml−1 in the fast acetylators (p〈0.025). Treatment with Apresoline® 25 mg tid produced minimum serum concentrations at steady-state of 57.3±7.3 ng·ml−1 and 33.4±4.2 ng·ml−1 in 8 slow and 5 fast acetylators, respectively (p〈0.05). The corresponding maximum concentrations were 228.8±20.3 ng·ml−1 and 147.6±15.0 ng·ml−1 in slow and fast acetylators, respectively (p〈0.025). First-pass metabolism of hydralazine could explain the difference in bioavailability of the drug between fast and slow acetylators, without any corresponding difference in the elimination rate of the drug in the post-distributive phase.
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  • 26
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    European journal of clinical pharmacology 10 (1976), S. 395-401 
    ISSN: 1432-1041
    Keywords: Hydralazine ; bioavailability ; polymorphic acetylation ; first-pass metabolism ; oral and intravenous dosing
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of orally administered hydralazine was assessed in 4 healthy subjects after separate administration of a single oral or intravenous dose (0.3 mg·kg−1). Comparison of the areas under the serum concentration-time curves showed that 26 – 55 % of the oral dose was available to the systemic circulation as unchanged drug. The O - 24 h excretion of the drug in urine was rapid: 11.4 – 14.1 % of the dose after intravenous administration, and 2.0 – 3.6 % after an oral dose. Acetylation of hydralazine leads to formation of 3-methyl-s-triazolo-3,4,a-phthalazine (MTP) and a gas-liquid-chromatographic method for its measurement in urine was developed. After oral and intravenous administration, 0.8 – 1.2 % and 1.4 – 2.3 % of the dose, respectively, were recovered within 24 hours from urine as MTP. After oral administration there was a relative increase in the amount of MTP in every subject, which indicates route-dependent metabolism. The lower bioavailability of oral hydralazine could be explained in terms of first-pass metabolism.
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  • 27
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    European journal of clinical pharmacology 16 (1979), S. 335-340 
    ISSN: 1432-1041
    Keywords: cimetidine ; enterohepatic circulation ; irregular absorption ; bioavailability ; pharmacokinetics ; volunteers
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability and pharmacokinetics of cimetidine have been studied in healthy volunteers after administration of single intravenous (100 mg) and oral doses (100, 400 and 800 mg). After i.v. administration, the kinetics of cimetidine could be described by a linear, two compartment open model. Substantial variation in half-life was observed between subjects, with a mean value of 2.1 h (range 0.9–4.7). Cimetidine had a low hepatic extraction ratio and a high total plasma clearance, due to extensive urinary excretion of unchanged drug. After oral administration, the plasma concentration vs time curves in most subjects exhibited two marked peaks, an observation that seemed to be constant within individuals and was independent of dose. Bioavailability, estimated as the area under the plasma concentration vs time curves (AUC), after oral doses as compared to the intravenous dose, in most cases exceeded 100%. There was no correlation between bioavailability estimated as AUC and as urinary excretion of unchanged drug. These observations may indicate an enterohepatic circulatory mechanism, predominantly after oral administration. Both unchanged drug and its sulphoxide metabolite appear to be excreted in bile. The latter was shown in vitro to be reduced to cimetidine by fecal bacteria.
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  • 28
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    European journal of clinical pharmacology 13 (1978), S. 267-274 
    ISSN: 1432-1041
    Keywords: Chlordiazepoxide ; benzodiazepines ; pharmacokinetics ; bioavailability ; intramuscular injection ; alcohol withdrawal
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption of oral and intramuscular (i. m.) chlordiazepoxide hydrochloride (CDX · HCl) was compared in two pharmacokinetic studies. In Study One, single 50-mg doses of CDX · HCl were administered orally and by i. m. injection to 14 healthy volunteers using a crossover design. Whole-blood concentrations of chlordiazepoxide (CDX) and its first active metabolite, desmethylchlordiazepoxide (DMCDX), were determined in multiple samples drawn after the dose. Mean pharmacokinetic variables for CDX following oral and i. m. administration, respectively, were: highest measured blood concentration, 1.65 vs 0.87 µg/ml (p〈0.001); time of highest concentration, 2.3 vs 7.6 h after dosing (p〈0.001); apparent absorption half-life, 0.71 vs 3.39 h (p〈0.001). Biphasic absorption after i. m. injection, consistent with precipitation at the injection site, was observed in 9 of 14 subjects. Based upon comparison with previous intravenous data, the completeness of absorption was 100% for oral vs 86% for i. m. CDX · HCl (p〈0.1). In Study Two, 28 male chronic alcoholics with clinical manifestations of the acute alcohol withdrawal syndrome were randomly assigned to one of four treatment conditions: 50 or 100 mg doses of CDX · HCl, by mouth or by i. m. injection. Concentrations of CDX and DMCDX, determined in plasma samples drawn every 20 min for 5 h following the dose, were significantly higher after oral administration of a given dose than at corresponding points in time after i.m. injection after the same dose. Thus absorption of oral CDX is reasonably rapid and complete, whereas the absorption rate of i. m. CDX is slow.
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  • 29
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    European journal of clinical pharmacology 15 (1979), S. 269-274 
    ISSN: 1432-1041
    Keywords: phenytoin ; food-intake ; bioavailability ; pharmacokinetics
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of food intake on the absorption of phenytoin was examined in eight healthy volunteers, by study of single-dose kinetics following ingestion of phenytoin 300 mg either with a standardized breakfast or on an empty stomach. Blood samples were collected at regular intervals from 0 to 48 h, and serum concentrations of unmetabolized phenytoin were determined by gas chromatography. Serum concentrations of the major metabolite of phenytoin, 4-hydroxyphenytoin, were measured by mass fragmentography. Concurrent intake of food and phenytoin appeared to accelerate absorption of the drug from the formulation used, and the peak concentrations were significantly higher (mean increase 40%) in the postprandial than in the preprandial state. As reflected by the AUC (area under the curve), the amount of drug absorbed was increased during postprandial conditions, although the difference only reached borderline significance. It is suggested that phenytoin should always be taken in a defined relation to meals.
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  • 30
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    European journal of clinical pharmacology 16 (1979), S. 107-112 
    ISSN: 1432-1041
    Keywords: quinidine ; enteric-coated tablets ; bioavailability ; gastric emptying ; pH
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption of quinidine from single and multiple doses of an enteric-coated preparation (Systodin®) was studied in seven healthy subjects, and was compared with the pharmacokinetics of intravenously administered quinidine and the results of in vitro dissolution tests of the tablets. Absorption of quinidine began after a variable delay, 2–8 h (mean 4.8) after fasting and 3–10 h (mean 6.1) after food. The rate of absorption varied both in and between individuals. It appeared to be lower when the drug was administered after food. Multiple doses after food gave a pattern of plasma concentration-time curves similar to that found on administration of single doses after food. The delay prior to absorption was prolonged at night. The ratio between the maximum and minimum concentration of quinidine during a dose interval varied from 1.3 to 3.2 (mean 2.0). Bioavailability of quinidine in fasting subjects ranged from 69 to 95% (mean 83); variation was greater when doses were administered after food. The release of quinidine from the enteric-coated preparation was pH dependent and was sustained at low pHs as may be found in the intestines. The results indicate that the absorption of quinidine from the enteric-coated formulation was dependent on the highly variable rate of gastric emptying and the pH of intestinal fluid, and it varied greatly both within and between individuals.
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  • 31
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    European journal of clinical pharmacology 16 (1979), S. 141-147 
    ISSN: 1432-1041
    Keywords: prazepam ; N-desmethyldiazepam ; bioavailability ; pharmokinetics ; electron-capture gasliquid chromatography
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An original electron-capture gas chromatographic assay was developed for simultaneous measurement of plasma levels of the benzodiazepine derivative prazepam and of its principal unconjugated metabolite, N-desmethyldiazepam. The assay was used to study the pharmacokinetics of the drug and its comparative bioavailability from tablets and from a specially prepared solution. Nine healthy adult volunteers were studied. Each volunteer on one occasion took 30 mg of the drug in tablet form, and on another occasion 30 mg of the drug in solution. In all subjects, N-desmethyldiazepam appeared in plasma shortly after prazepam appeared and reached a peak within four hours of prazepam ingestion. Thereafter plasma N-desmethyldiazepam levels were much higher than plasma prazepam levels throughout. Prazepam became undetectable within six hours of intake, whereas its metabolite could still be measured in plasma fourteen days after dosage. Thus much of the pharmacological action of prazepam may be mediated through its metabolite, N-desmethyldiazepam. In five of the nine subjects, areas under the plasma level curves for the metabolite were not markedly different for the tablet and solution formulations studied. In the other four subjects the area under the curve for the tablets was 50% to 80% of the area under the curve for the solution. The time to reach peak plasma level for the metabolite was shorter after the solution formulation (mean 2.0±SD 1.2 h) than after the tablet formulation (mean 4.2±SD 1.7 h).
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  • 32
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    European journal of clinical pharmacology 10 (1976), S. 55-58 
    ISSN: 1432-1041
    Keywords: Penicillin V ; bioavailability ; pharmacokinetics ; dose ranging
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An absorption study was performed in ten healthy volunteers to test the bioavailability of various doses of two penicillin V-K preparations: Isocillin® (Hoechst AG, Federal Republic of Germany), — tablets of 600 000 and 1.2 Mega U; V-Cillin® (Eli Lilly, USA), — tablets of 200 000, 400 000 and 800 000 U. The serum concentrations and elimination of the active substance in urine were measured for six hours after administration. Independently of the source of the preparation, a strict linear relation between the dose and the area under the serum curve (AUC), or between the dose and the urinary elimination, was demonstrated by regression analysis. The dose-dependent increase in the AUC was highly significant (p〈0.01) in the range tested, i.e. between 200 000 and 1.2 Mega U. The relative elimination of active substance in urine lay within narrow limits for all doses (35.7–41.3%). Thus, both compounds proved to have the same bioavailability.
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  • 33
    ISSN: 1432-1041
    Keywords: Ampicillin ; bioavailability ; pharmacokinetics ; branded products ; proprietary preparations ; capsule formulation ; tablet formulation
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and bioavailability of three different brands of ampicillin were studied in 10 volunteers. After intravenous administration ampicillin can be described adequately by a two-compartment open pharmacokinetic model. The half-life during the α-phase was 9 min and the β-half-life was in the range 50–60 min, independent of the mode of administration. Absolute bioavailability was determined from the ratio of the areas under the serum concentration curves obtained after oral and intravenous administration of equal doses. Bioavailability was also estimated by analysis of variance. The results indicated absolute availability of the three products of 39–54%. One of the products, a capsule formulation, showed a significantly lower bioavailability than the others, which were tablet formulations.
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  • 34
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    European journal of clinical pharmacology 11 (1977), S. 277-281 
    ISSN: 1432-1041
    Keywords: Proscillaridin ; oral administration ; portal venous sample ; porto-peripheral concentration difference ; bioavailability ; 86Rb-uptake inhibition assay
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption of proscillaridin A was studied in four patients undergoing catheterization of the portal vein for diagnostic purposes. Proscillaridin 1.5 mg was given as a single oral dose and plasma glycoside activity was analyzed by the86Rb-uptake inhibition technique. Proscillaridin appeared rapidly in the portal blood, peak activity being found after 15 min in three and after 30 min in one patient. In peripheral blood the peak activity occurred after approximately 35 min. Despite rapid passage across the gut wall, porto-peripheral differences in glycoside activity were small; they were zero after 4 h. The mean amount absorbed as active proscillaridin during the first 4 h after the dose was calculated to be only 7.1% of the given amount. Late porto-peripheral differences, probably due to enterohepatic recycling, appeared after 6 h in three patients. The results suggest that proscillaridin undergoes first pass inactivation in the gut wall. Enterohepatic recirculation may contribute to the amounts of active glycoside that reach the systemic circulation.
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  • 35
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    European journal of clinical pharmacology 10 (1976), S. 49-54 
    ISSN: 1432-1041
    Keywords: Three-compartment open model ; intravenous infusion ; apparent volume of distribution ; renal insufficiency ; miconazole ; bioavailability
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic profile of miconazole has been studied in normal subjects and in patients suffering from severe renal insufficiency; one group of patients was undergoing intermittent haemodialysis. A three-compartment open model was fitted to the observed plasma concentrations obtained after intravenous infusion of miconazole 522 mg over fifteen minutes. The rate constants of elimination and exchange between compartments computed for the three groups were not significantly different. The apparent volumes of distribution in the cases of renal failure not undergoing haemodialysis were significantly smaller than the corresponding control values. A computational procedure is described which reduces observations obtained after infusion to the case of a single rapid intravenous administration.
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  • 36
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    European journal of clinical pharmacology 11 (1977), S. 207-212 
    ISSN: 1432-1041
    Keywords: Chlorpropamide ; hypoglycaemic agent ; bioavailability ; plasma concentrations ; bioequivalence ; dissolution tests
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of chlorpropamide from two new formulations (Melitase® tablets) has been compared to that from a reference formulation which is currently in clinical use as a hypoglycaemic agent. In both rate and extent of bioavailability, all three formulations may be considered equivalent, providing allowances are made for differences in drug content. With 95% confidence, the mean bioavailability of chlorpropamide from the new formulations was within about 16% of the mean from the reference formulation, and formulation-related differences were not statistically significant. Although all three formulations were shown to have similar dissolution profiles, dissolution of chlorpropamide was pH-dependent in vitro. Dissolution was almost complete during 30 min at pH 7.2, but only 40%–60% had dissolved during 90 min at pH 2.0. A peak mean concentration of 22.7 µg/ml was reached 3 h after administration of 2×100 mg tablets of the new formulation and peak mean concentrations of 26.8 µg/ml and 27.4 µg/ml were reached 3 h and 4 hours after administration of one 250 mg tablet of the new formulation and one 250 mg tablet of the reference formulation respectively. Formulation-related differences of mean plasma concentrations (after scaling for equal doses of 250 mg) were not significant and each formulation provided similar plasma concentrations at corresponding times after administration. Statistically significant subject-related differences in all the parameters of bioavailability were shown by analyses of variance.
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  • 37
    ISSN: 1432-1041
    Keywords: ergotamine ; migraine ; bioavailability ; radioimmunoassay ; plasma level ; CSF level ; continuous dosing
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma ergotamine concentrations were determined by radioimmunoassay in 10 healthy subjects after a 2 mg oral dose of ergotamine, administered at 24 h intervals on three consecutive days. After the first dose the mean peak plasma level of 0.35±0.05 (SEM) ng/ml was found 1–2 h after administration. In the samples obtained 2 h after the second and third doses, plasma ergotamine levels did not exceed the first peak value. On the other hand, after the third and last dose the plasma ergotamine began to rise slowly, reaching maximum of 0.70± 0.10 ng/ml on the 6th day after administration. This supports the concept of accumulation of the drug or of immunoreactive metabolites. CSF ergotamine was determined in 4 patients, who underwent lumbar puncture for other diagnostic purposes, 1 to 2 h after the 2 mg oral dose. A concentration of 0.40± 0.03 ng/ml was observed. In seven out of 18 migraine patients who were taking ergotamine preparations daily (mean 11.7 mg/week), ergotamine could not be detected in plasma 1 h after administration of the dose. In the remaining migraine patients, the pattern of plasma ergotamine after both the daily and the test doses was similar to that of the 10 healthy subjects. The results in volunteers and migraine patients suggest notable variation in bioavailability of the drug. It seems that in most subjects there is accumulation or tissue redistribution of ergotamine or its immunoreactive metabolites, although in a significant number of migraine patients who use the drug daily, ergotamine does not appear to be biologically available.
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  • 38
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    European journal of clinical pharmacology 16 (1979), S. 405-410 
    ISSN: 1432-1041
    Keywords: diclofenac ; plasma levels ; intravenous bolus administration ; oral administration ; enteric coating ; bioavailability
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of diclofenac were examined following single rapid intravenous injection and also following single oral doses to healthy female volunteers. After intravenous injection plasma levels of diclofenac fell rapidly and were below the limits of detection at 5.5 h postdosing. Individual drug profiles were described by a triexponential function and mean half-lives of the three exponential phases were 0.05, 0.26 and 1.1 h. After oral doses of enteric-coated tablets, the lag time between dosing and the appearance of drug in plasma varied between 1.0 and 4.5 h. However once drug absorption had commenced similar plasma drug profiles were obtained in different individuals. Peak plasma diclofenac levels ranged from 1.4 to 3.0 µg · ml−1. The mean terminal drug half-life in plasma was 1.8 h after oral doses. This value was not significantly greater than the value of 1.1 h following intravenous doses. Fifty percent of orally dosed diclofenac did not reach the systemic circulation due, predominantly, to first-pass metabolism.
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  • 39
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    European journal of clinical pharmacology 11 (1977), S. 219-224 
    ISSN: 1432-1041
    Keywords: Nortriptyline ; 10-OH-nortriptyline ; bioavailability ; plasma metabolites ; first pass metabolism ; oral dose ; intramuscular dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Nortriptyline was given orally and intramuscularly to six depressed patients. Plasma concentrations of parent drug and the unconjugated and conjugated principal metabolite, 10-hydroxynortriptyline, were determined by mass fragmentography. There was a significant decrease in the area under the nortriptyline plasma concentration — time curve after the oral route of administration, whilst the elimination rate was unchanged. With the oral dose, plasma concentrations of the metabolites were higher and peaked earlier than after intramuscular administration, whilst the opposite was true for the parent compound. This proves that the difference in bioavailability between the two routes of administration was due to first pass metabolism. As determined from the ratio between corresponding areas, the relative bioavailability of the oral dose was 66±21 S.D. per cent. This fraction is higher than that reported previously when intravenous nortriptyline was used as the reference dosage form.
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  • 40
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    European journal of clinical pharmacology 12 (1977), S. 281-284 
    ISSN: 1432-1041
    Keywords: Tetracycline ; bioavailability ; plasma levels ; nutritional state ; man
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Relative bioavailability after oral administration of a single dose and Cmin levels of tetracycline in plasma after multiple doses were determined in groups of well-nourished and undernourished subjects. The relative bioavailability of tetracycline, assessed by the area under serum concentration time-curves, did not differ in undernourished and well-nourished patients. The plasma levels were not different in the two groups after the conventional dose of tetracycline HCl 250 mg at 6 hour intervals. However, in these studies undernourished subjects received a higher dose per kg body weight, which could have compensated for any effect of a shortened half life of the drug. When the dose per kg body weight was reduced, the Cmin levels were lower. On the other hand, with the same dose per kg body weight at more frequent intervals, the plasma concentrations were similar to those in well-nourished subjects. These studies indicate that the dosage regimen should be based both on body weight and on the nutritional status of the individual.
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  • 41
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    European journal of clinical pharmacology 12 (1977), S. 65-68 
    ISSN: 1432-1041
    Keywords: Indomethacin ; antacids ; drug-drug interactions ; bioavailability ; drug combinations
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The biovailability of indomethacin from two indomethacin-antacid (aluminum hydroxide magnesium carbonate and magnesium hydroxide) combinations was compared with the bioavailability of oral indomethacin. Relative bioavailability was estimated by three methods: comparison of plasma concentrations at various times, comparison of areas under plasma concentration time curves, and comparison of the amount of drug excreted unchanged in the urine. A double blind three-way crossover study was conducted in twelve healthy volunteers. The combination with the slightly smaller amount of antacid (preparation A) showed significantly decreased bioavailability by all three methods in comparison with indomethacin alone (preparation C). The combination with the larger amount of antacid (preparation B) was also less bioavailable than preparation C. This effect was significant only for the comparison of areas under curves and not for plasma levels, although the mean plasma levels produced by preparation B at all times were lower than those for preparation C. These findings suggest that aluminum hydroxide magnesium carbonate and magnesium hydroxide decrease the bioavailability of indomethacin.
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  • 42
    ISSN: 1432-1041
    Keywords: Tolmetin ; pharmacokinetics ; bioavailability ; antacid ; oral dose
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The purpose of this study was to determine whether a concomitant single dose of antacid or multiple doses of antacid administered prior to, and with tolmetin, alter the pharmacokinetics of tolmetin when the drug was administered as a commercially available tablet containing tolmetin sodium. The possible effects of the antacid on plasma concentrations and urinary excretion of tolmetin and its major metabolite were evaluated following administration of: (a) tolmetin sodium alone; (b) antacid four time a day for three days prior to a single dose of tolmetin sodium, with continuation of the antacid during the day tolmetin was given; and (c) co-administration of single doses of tolmetin sodium and antacid. The twenty-four subject study was of the crossover type. There were no significant differences among treatment means for: (i) peak plasma concentrations of both tolmetin and metabolite, (ii) AUC 0–8 h and AUC 0-∞ for both tolmetin and metabolite, (iii) time to peak plasma concentration for both tolmetin and metabolite, (iv) plasma concentrations of both tolmetin and the metabolite at all sampling times (except for tolmetin at 2 h), (v) renal clearance of both tolmetin and its metabolite, and (vi) the amount of metabolite excreted in the 0–24 h urine. There were small, but significant, differences among amounts of tolmetin excreted in the 0–24 h urine. Semilogarithmic plots of both tolmetin and metabolite plasma concentrations past the peak concentrations were curved over the entire 8-h observation period; although the elimination half-life of tolmetin has been reported to be about one hour, the half-life most probably exceeds 2.6 h in most subjects. The results of this study indicate a lack of a significant drug-drug interaction between the non-steroidal anti-inflammatory agent, tolmetin sodium, and a commonly used antacid, which is a mixture of magnesium and aluminium hydroxides.
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  • 43
    ISSN: 1432-1041
    Keywords: Coumarin ; 7-Hydroxycoumarin ; drug disposition ; first-pass effect ; bioavailability
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of coumarin (C) upon i.v. and p.o. administration and its metabolites 7-hydroxy-coumarin (7-HC) and 7-hydroxy-coumarin glucuronide (7-HCG) have been studied. Six healthy volunteers were involved in this investigation. Four of the volunteers participated in a crossover study. Coumarin was administered i.v. and p.o. in dose sizes of 0.25 mg/kg and 0.857 mg/kg, respectively. Coumarin is rapidly absorbed p.o., however the availability to systemic circulation is less than 4%. The rest of the dose appears quantitatively as 7-HC and 7-HCG in systemic circulation suggesting an extensive firstpass effect. Coumarin and 7-HCG are best fitted to an open two-compartment model, whereas 7-HC is best fitted to an open one-compartment model. The biological half-life of both C (0.80 vs. 1.02 h) and 7-HCG (1.47 vs. 1.15 h) was not significantly different for the two routes of administration. The large total clearance of C again suggests a first-pass effect; while that of 7-HCG, which is nearly exclusively eliminated into urine, indicates active tubular secretion of the glucuronide.
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  • 44
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    European journal of clinical pharmacology 13 (1978), S. 35-39 
    ISSN: 1432-1041
    Keywords: Norethindrone ; bioavailability ; man ; competitive protein binding ; sex differences ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A competitive protein binding assay for norethindrone was developed to measure plasma levels in human subjects. The plasma levels were considerably higher in women than in men, especially at low dose levels. The plasma levels were directly related to the dose in men; but greater variations in the plasma levels were observed in women. The plasma half-life was about 5 h in both sexes with single oral doses of 5 to 20 mg. A comparative bioavailability study with norethindrone from 2 different manufacturers, formulated in the same manner, showed no significant differences in absorption characteristics and provided sufficient data for pharmacokinetic analysis.
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  • 45
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    European journal of clinical pharmacology 14 (1978), S. 261-265 
    ISSN: 1432-1041
    Keywords: Procainamide ; slow release formulations ; bioavailability
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Procainamide was given to 20 patients with normal renal function as an i.v. bolus of 500 mg followed by 1.0 or 1.5 g eight-hourly by mouth in the form of a slow release preparation (Durules). 97.6±27.1 (SD)% of the oral procainamide was absorbed, the absorption half life being 1.54 h. The elimination half life following the oral formulation was 6.0±0.8 h, compared to a mean of 3.4±0.4 h following i.v. administration. Elimination half life following i.v. administration was slightly related to acetylator status, being 2.75±0.9 h in fast acetylators, and 4.4±2.4 h in slow acetylators. This dependence on acetylator status was not seen in half life following oral administration. Total body clearance, steady state plasma procainamide and N-acetylprocainamide were not significantly dependent on acetylator status, although a few patients who are slow acetylators had unexpectedly low clearance and high steady state procainamide concentrations when given the higher dose.
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  • 46
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    European journal of clinical pharmacology 14 (1978), S. 357-360 
    ISSN: 1432-1041
    Keywords: Lanoxin tablets ; Lanoxicaps ; sorbitol ; bioavailability
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary (1) The mean cumulative urinary digoxin excretion over 8 days was compared in 8 healthy volunteers after single doses of digoxin administered as 3 Lanoxin tablets of 0.25 mg, 3 digoxin tablets of 0.2 mg, 12 Lanoxicaps without sorbitol of 0.05 mg, 6 Lanoxicaps without sorbitol of 0.1 mg digoxin, 3 Lanoxicaps without sorbitol of 0.2 mg and 3 Lanoxicaps with sorbitol of 0.2 mg. (2) There was no significant difference between the 8 day cumulative urinary excretion for any of the Lanoxicaps treatments. (3) Cumulative urinary excretion after 3 digoxin tablets of 0.2 mg was significantly (P〈0.05) lower than after all other treatments. (4) Cumulative urinary excretion after 3 Lanoxin tablets of 0.25 mg was not significantly different from that after any of the Lanoxicaps treatments except 0.1 mg Lanoxicaps without sorbitol, it was significantly (P〈0.05) lower after the latter. (5) Mean urinary excretion of digoxin was 60% of ingested dose for all Lanoxicaps treatments and was significantly (P〈0.05) higher than the mean value of 50% for both tablet treatments. (6) Enhanced absorption of digoxin from Lanoxicaps was confirmed and shown to be unrelated to the sorbitol content of the capsule shell.
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  • 47
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    Journal of chemical ecology 1 (1975), S. 101-113 
    ISSN: 1573-1561
    Keywords: pheromone ; inhibition ; Scolytidae ; Ips ; pini ; paraconfusus ; ipsenol ; linalool
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The bark beetles,Ips pini andI. paraconfusus, are not cross-attractive in the field although they attack the same host material at the same time. Logs containing the pheromone-producing sex (males) of both species side by side attract significantly fewer beetles of each species than do males of either species alone. Ipsenol, a component of the maleI. paraconfusus pheromone, duplicates the activity of maleI. paraconfusus in inhibiting the response ofI. pini to maleI. pini. Linalool from maleI. pini also reduces the catch ofI. paraconfusus in response to maleI. paraconfusus. Simultaneous production of a specific attractant pheromone and an interspecific chemical inhibitor favors exclusive use of the host substrate by the first arriving species.
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  • 48
    ISSN: 1573-1561
    Keywords: Archips argyrospilus ; Archips mortuanus ; pheromone ; attractant ; Tortricidae ; (Z)-11-tetradecenyl acetate ; (E)-11-tetradecenyl acetate ; (Z)-9-tetradecenyl acetate ; dodecyl acetate
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    Notes: Abstract MaleArchips argyrospilus (Walker) were maximally attracted to a 60∶40∶4∶200 admixture of (Z)-11-tetradecenyl, (E)-11-tetradecenyl, (Z)-9-tetradecenyl and dodecyl acetates. The identification of (Z)-9-tetradecenyl acetate, in addition to the other 3 components reported previously, is the first report of a 4-component pheromone system in moths.Archips mortuanus Kearfoot, a sibling species, was maximally attracted to a blend of the same components, but in a 90∶10∶1 mix of the tetradecenyl acetates. Among a number of tortricine moths that co-occur on apples and other hosts in New York, British Columbia, and elsewhere, differences in diel rhythms of attraction and seasonal distribution are insufficient to maintain reproductive isolation. Although the attractant systems of these species often possess components in common, males are maximally attracted to a speciesspecific blend. In tortricine moths attraction specificity appears to be a paramount mechanism for species partitioning.
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  • 49
    ISSN: 1573-1561
    Keywords: pheromone ; inhibitor ; bark beetle ; Dendroctonus ; southern pine beetle ; slow-release formulations
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract A slow release formulation of the bark beetle pheromones,endo- andexo-brevicomin, significantly reduced landing of southern pine beetles on host trees. Beetle flight activity within the infestation was not affected by the pheromones. The pheromones were released at approximately 600 mg/ha/day via Conrel® hollow fiber controlled-release dispensers.
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  • 50
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    Journal of chemical ecology 3 (1977), S. 207-217 
    ISSN: 1573-1561
    Keywords: Black molly fish ; Mollinenesia latipinna ; pheromone ; thyroxine ; thiouracil ; general activity stimulus ; social contact
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The female black mollyMollinenesia latipinna emits a water-borne pheromone which increases general activity and social contacts among males. Two hormones, thyroxine and thiouracil, administered to the females increase these behaviors in males. Apparently the hormones do not functionally compete in this species, and both seem to elevate the emission of the male stimulant.
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  • 51
    ISSN: 1573-1561
    Keywords: stable fly ; Stomoxys calcitrans (L.) ; pheromone ; sex pheromone ; branched alkanes ; mating stimulant
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Each of 20 methyl-branched and 1,5-dimethyl-branched alkanes that comprise the active principle of saturated hydrocarbons of the female stable fly,Stomoxys calcitrans (L.), was synthesized and evaluated for mating stimulant activity. The compounds that showed the highest degree of activity in bioassays were 15-methyl- and 15,19-dimethyltritriacontanes.
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  • 52
    ISSN: 1573-1561
    Keywords: Fannia canicularis (L.) ; little house fly ; pheromone ; sex pheromone ; (Z)-9-pentacosene ; heneicosan-8-ol acetate
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Chromatograms of the cuticular lipids washed from recently emerged female and maleFannia canicularis (L.) flies were nearly identical, but by the time the flies were 5 days old, the cuticular components of the two sexes differed considerably. A monoolefin which constituted 66% of the cuticular lipid from 5-day-old females stimulated a copulatory response from males and was identified as (Z)-9-pentacosene. The cuticular lipid of the same age males contained only 1% of this compound. Although all the major constituents of the cuticular lipid from mature females were hydrocarbons, 27% of the lipid washed from 5-day-old males was a nonhydrocarbon material that was represented by a single GLC peak. This material was identified as heneicosan-8-ol acetate.
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  • 53
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    Journal of chemical ecology 3 (1977), S. 461-466 
    ISSN: 1573-1561
    Keywords: communication ; fish ; cichlid ; Cichlasoma citrinellum ; pheromone ; maternal ; development ; predation ; chemoreception ; fry
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract When placed in aY-maze, the 1–10-day-old free-swimming fry of the Midas cichlid can chemically distinguish between their mother and plain water and between another mother and plain water. They do not distinguish between the two mothers offered together or between their father and plain water. Predation pressures make these responses adaptive.
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  • 54
    ISSN: 1573-1561
    Keywords: Scolytus multistriatus ; Dutch elm disease ; pheromone ; Multilure ; mass-trapping ; Ulmus
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract We attempted to suppress a population ofScolytus multistriatus (Marsham), the principal vector of Dutch elm disease, by trapping flying beetles on sticky traps baited with synthetic pheromone. The estimated catch on 421 traps distributed throughout a 1-km2 plot in Detroit, Michigan, was nearly 1 million beetles. Because an estimated 5 million beetles emerged in the plot during the study period, we conclude that this preliminary trapping study had no appreciable effect on suppressing the population. Studies that employ improved materials and techniques are continuing.
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  • 55
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    Journal of chemical ecology 4 (1978), S. 409-423 
    ISSN: 1573-1561
    Keywords: Coleoptera ; Dermestidae ; diel behavioral patterns ; 14-methyl-8-hexadecenal ; pheromone ; reproductive isolation ; Trogoderma glabrum ; T. inclusum ; T. variabile ; trogodermal
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract AdultTrogoderma glabrum, T. inclusum, andT. variabile exhibit diel periods of exposure-concealment behavior, the frequency and duration of which are age-dependent, and the temporal placement of which is species-dependent. Exposure periods correspond with daily maxima in male sensitivity to the most active female-released sex pheromone component, 14-methyl-8-hexadecenal, and with respective periods of sex pheromone release in females. Exposure-concealment behavior may be a factor in reproductive isolation between these species, since potential communication distances are greatly reduced when either males or females are concealed.
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  • 56
    ISSN: 1573-1561
    Keywords: Neodiprion sertifer ; Pine saw-fly ; Hymenoptera ; Diprionidae ; pheromone ; trans-perillenal ; monoterpene
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Volatile constituents present in nanogram quantities in various body parts and glands of the males and females of the speciesNeodiprion sertifer Geoffr. (Hymenoptera: Diprionidae) have been investigated by GC-MS. A significant amount of a volatile constituent was detected in the lateral parts of the integument of abdominal segments II-III. The constituent was identified as the furanoid monoterpenetrans-perillenal (I) previously not known to occur in nature. The identification and synthesis of this compound is described.
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  • 57
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    Journal of chemical ecology 5 (1979), S. 353-361 
    ISSN: 1573-1561
    Keywords: Stable fly ; Stomoxys calcitrans (L) ; pheromone ; mating stimulants ; alkenes ; cuticular lipids ; copulatory behavior
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The cuticular alkenes of the female stable fly,Stomoxys calcitrans (L), which were responsible for inducing male fly copulatory behavior are (Z)-9-hentriacontene, (Z)-9-tritriacontene, 13-methyl-1-hen-triacontene and 13-methyl-1-tritriacontene. The identifications of the branched alkenes and the synthesis of these four compounds are described. Bioassays indicate that these materials in combination with previously described methyl branched alkanes are more active than the individual components.
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  • 58
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    Journal of chemical ecology 5 (1979), S. 565-574 
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Lasiocampidae ; Malacosoma americanum ; Malacosoma disstria ; Tortricidae ; Archips cerasivoranus ; trail marker ; pheromone ; interspecific response ; tent caterpillar
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Exploratory trails deposited on paper strips by the forest tent caterpillar (FTC),Malacosoma disstria Hubner, and the eastern tent caterpillar (ETC),M. americanum (Fabricius), as well as extracts of these trails, readily elicited interspecific trail-following behavior. In 2-choice tests involving simple Y mazes constructed from these paper strips, the caterpillars of both species preferred by approximately 3∶1 the trails of the FTC. Studies involving whole colonies of the ETC maintained under nearnatural conditions in the laboratory, however, indicated that the trails deposited by successful foragers of the ETC as they returned to their tent from feeding sites were more attractive than the exploratory trails of either the ETC or FTC. The pronounced interspecific response of these congeners to each other's trails suggests that they utilize either qualitatively similar or identical trail-marking chemicals. Both species preferred their own trails to those ofArchips cerasivoranus (Fitch) (Tortricidae), providing the first evidence that more distantly related lepidopterous larvae utilize distinct trails.
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  • 59
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    Journal of chemical ecology 5 (1979), S. 941-953 
    ISSN: 1573-1561
    Keywords: White peach scale ; Pseudaulacaspis pentagona ; pheromone ; attractant ; microtechniques ; enantiomer ; isomers ; (R,Z)-3 ; 9-dimethyl-6-isopropenyl-3 ; 9-decadien-1-ol propionate
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Micro techniques were used to obtain spectroscopic and degradative information from less than 5μg of the sex attractant of female white peach scale,Pseudaulascaspis pentagons (Targioni-Tozzetti) isolated from airborne collections. The pheromone was identified as (Z)-3,9-dimethyl-6-isopropenyl-3,9-decadien-1-ol propionate. Both enantiomers of theZ isomer and also the enantiomers of theE isomer were prepared from (R)-or (S)-limonene. Bioassays of material with minimum enantiomeric purity of 95% showed that at extreme dilution only theR,Z isomer attracted male white peach scale; however activity of theS,Z enantiomer could not be completely excluded.
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  • 60
    ISSN: 1573-1561
    Keywords: Coleoptera ; Dermestidae ; Trogoderma variabile ; pheromone ; isolation ; identification ; (Z)-14-methyl-8-hexadecenal ; aeration ; Porapak Q ; sex attractant
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Females of the dermestid beetle,Trogoderma variabile Ballion, exhibit a diel pattern of calling behavior. A potent sexual excitant and attractant for the male beetles can be collected on Porapak Q during aeration of female beetles, but cannot be detected in extracts of macerated females. The attractant has been identified as (Z)-14-methyl-8-hexadecenal. Of the five additional compounds previously identified as attractants in otherTrogoderma species, only two were found; (Z)-14-methyl-8-hexadecen-1-ol is present in extracts of macerated female beetles, but not in extracts of Porapak Q, and γ-caprolactone is present in extracts of Porapak Q. Three collection procedures were necessary to ensure that all the pheromone components had been isolated. Synthetic (Z)-14-methyl-8-hexadecenal elicits attraction and sexual arousal inT. Variabile males.
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    Journal of chemical ecology 3 (1977), S. 219-237 
    ISSN: 1573-1561
    Keywords: Attagenus elongatulus ; Dermestidae ; pheromone ; behavior ; calling ; bioassay
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Males ofAttagenus elongatulus Casey responded to a source of female odor with a characteristic sequence of actions which included: extension of the antennae, elevation of the body by leg extension, rapid zig-zag running, and intermittent bobbing up and down. The courtship sequence also consisted of several activities and was usually followed by a typical copulatory act of less than 1-minute duration. Virgin females exhibited calling behavior which was associated with pheromone release. Female calling activity, female pheromone content, and male responsiveness followed a diurnal cycle with peak values occurring during the earlier hours of the 16L∶8D photoperiod. Quantitative bioassay indicated that a 50% male response level (RD50) occurred at ca. 0.014 female equivalent (FE) exposure.
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  • 62
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    Journal of chemical ecology 3 (1977), S. 251-255 
    ISSN: 1573-1561
    Keywords: stable fly ; Stomoxys calcitrans (L.) ; pheromone ; sex pheromone ; polyene ; mating stimulant ; (Z,Z)-1,7,-13-pentacosatriene
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The major component of the cuticular lipids of male stable flies,Stomoxys calcitrans (L.), was identified as (Z,Z)-1,7,13-pentacosatriene. The identification was confirmed by synthesis. This material is of unknown biological function; it is apparently not produced by female stable flies.
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  • 63
    ISSN: 1573-1561
    Keywords: Coleoptera ; Dermestidae ; Trogoderma granarium (khapra beetle) ; T. variabile ; T. glabrum ; T. inclusum ; pheromone ; (Z)- and (E)-14-methyl-8-hexadecenal ; interspecific response
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    Notes: Abstract Interspecific responses among severalTrogoderma species have been correlated with their pheromone components. The most important component emitted by four of the species is (Z)- or (E)-14-methyl-8-hexadecenal, which is not detectable in extracts of macerated beetles. The response to macerated beetles is probably due to the corresponding alcohol and ester. The recency of common origin of seven species is discussed.
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    Fresenius' Zeitschrift für analytische Chemie 279 (1976), S. 208-208 
    ISSN: 1618-2650
    Keywords: Best. von Palladium mit 2-Chlorphenothiazin ; Spektralphotometrie
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    Fresenius' Zeitschrift für analytische Chemie 279 (1976), S. 364-364 
    ISSN: 1618-2650
    Keywords: Best. von Titan(IV) ; Spektralphotometrie ; Extraktion als Thiocyanat mit Mesityloxid
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    Fresenius' Zeitschrift für analytische Chemie 278 (1976), S. 127-127 
    ISSN: 1618-2650
    Keywords: Best. von Kobalt mit 6-Nitrochinoxalin-2,3-dithiol ; Spektralphotometrie ; Spuren
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    Fresenius' Zeitschrift für analytische Chemie 278 (1976), S. 285-286 
    ISSN: 1618-2650
    Keywords: Best. von Kupfer mit 4-(2-Pyridylazo)-resorcin ; Spektralphotometrie ; Untersuchung der Komplexe
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    Fresenius' Zeitschrift für analytische Chemie 298 (1979), S. 367-372 
    ISSN: 1618-2650
    Keywords: Best. von Lanthaniden, Europium, Dysprosium, Erbium, Samarium in Uran ; Spektralphotometrie ; Atomabsorption ; Graphitofen
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    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Summary Studies were conducted on the assay of Sm, Eu, Dy and Er separated from uranium using aqueous standards by electrothermal AAS with Massmann type graphite furnace. The working curves were found to be linear in the ranges Sm (1–10 μg/ml), Eu (0.05–0.6 μg/ml), Dy (0.1–0.8 μg/ml) and Er (0.1–1.0 μg/ml). The values obtained for synthetic samples agreed favourably with those obtained by emission spectrographic method. Experiments using pyrolytic carbon coated tubes with and without pretreatment by La, Ta and Y have shown an enhancement with treatment upto a maximum of 15% and improve the memory effect marginally. The effect of Ta treatment was found to be singularly useful in improving the general behaviour of Sm. The interference effects of lanthanides, other than the analyte, were found to be negligible. However, the presence of uranium was found to affect the absorbance. The absorbance of Eu was found to be nearly independent of uranium after an initial increase. On the other hand, the absorbance of other elements studied was found to drastically decrease after an initial enhancement. Detailed investigations of temperature dependence of absorbance were carried out using Eu, Dy and Er. The differences in the behaviour of these elements is attributed to probable differences in the modes of their atomization.
    Notes: Zusammenfassung Die Untersuchungen wurden mit Hilfe des Graphitrohrofens nach Maßmann durchgeführt. In folgenden Bereichen ergaben sich lineare Eichkurven: Sm 1–10 μg/ml, Eu 0,05–0,6 μg/ml, Dy 0,1–0,8 μg/ml, Er 0,1μ-1,0 μg/ml. Die aus synthetischen Proben erhaltenen Ergebnisse stimmten gut mit den durch Emissionsspektrographie erhaltenen überein. Versuche wurden mit Röhren mit pyrolytischen Kohlenstoffüberzug mit und ohne Vorbehandlung durch La, Ta und Y durchgeführt und ergaben eine bis 15%ige Steigerung durch die Behandlung sowie eine mäßige Besserung des Memoryeffektes. Eine Behandlung mit Ta war besonders für Sm vorteilhaft. Störungen durch andere Lanthanide waren vernachlässigbar. Uran beeinflußte jedoch die Absorption. Im Falle von Eu zeigte sich nach anfänglicher Zunahme fast eine Unabhängigkeit, während bei den anderen untersuchten Elementen nach anfänglicher Zunahme eine beträchtliche Abnahme auftrat. Mit Eu, Dy und Er wurde ebenfalls die Temperaturabhängigkeit der Absorption untersucht. Festgestellte Unterschiede im Verhalten werden auf unterschiedliche Atomisierung zurückgeführt.
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    Fresenius' Zeitschrift für analytische Chemie 293 (1978), S. 416-416 
    ISSN: 1618-2650
    Keywords: Best von Vitamin D2 ; Spektralphotometrie ; HCl, Tetrachloräthan
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    Fresenius' Zeitschrift für analytische Chemie 293 (1978), S. 416-416 
    ISSN: 1618-2650
    Keywords: Best. von Pikrinsäure ; Spektralphotometrie ; Zink und Ammoniumchlorid
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    Fresenius' Zeitschrift für analytische Chemie 294 (1979), S. 284-284 
    ISSN: 1618-2650
    Keywords: Best. von Uran(VI) mit Chlorphosphonazo III ; Spektralphotometrie ; Trioctylamin-Extraktion
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    Fresenius' Zeitschrift für analytische Chemie 294 (1979), S. 285-285 
    ISSN: 1618-2650
    Keywords: Best. von Phosphat in Ferrosilicium ; Spektralphotometrie ; Cer/Xylenolorange, indirekt
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    Fresenius' Zeitschrift für analytische Chemie 294 (1979), S. 413-413 
    ISSN: 1618-2650
    Keywords: Best. von Kobalt mit Pyridin und Azid ; Spektralphotometrie ; Aussalzungsmittel, Mischkomplex
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    Fresenius' Zeitschrift für analytische Chemie 292 (1978), S. 43-44 
    ISSN: 1618-2650
    Keywords: Best. von Uran(VI) mit Arsenazo III ; Spektralphotometrie ; starksaure Lösung
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    Fresenius' Zeitschrift für analytische Chemie 292 (1978), S. 46-47 
    ISSN: 1618-2650
    Keywords: Best. von Thallium(I), Dimethylthalliumverbindungen ; Spektralphotometrie
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    Fresenius' Zeitschrift für analytische Chemie 295 (1979), S. 270-270 
    ISSN: 1618-2650
    Keywords: Best. von Cer(IV) ; Spektralphotometrie ; indirekt, Fe(III)-Resacetophenonoximat-Komplex
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    Fresenius' Zeitschrift für analytische Chemie 299 (1979), S. 264-266 
    ISSN: 1618-2650
    Keywords: Best. von Kohlenhydraten in Huminsäuren ; Spektralphotometrie ; Anthronmethode
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    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Eine modifizierte Anthronmethode zur Bestimmung des Kohlenhydratgehaltes in Fraktionen von Huminsäure-Blei(II)-Chelatverbindungen, die mit chemischen und gelchromatographischen Methoden getrennt wurden, wird beschrieben. Um die Störung der Methode durch die Absorption der Huminsäuren, die mit abnehmender Wellenlänge ansteigt, gering zu halten, wird die Extinktion des Anthron-Kohlenhydrat-Reaktionsproduktes bei 620 nm gemessen. Die Huminsäurekonzentration darf 0,1 g/dl nicht überschreiten. Da die molare Extinktion des Anthron-Reaktionsproduktes von der Art des Kohlenhydrates abhängt, wird der Kohlenhydratgehalt auf das Hauptkohlenhydrat des Huminsäurehydrolysats berechnet (d.h. Glucose).
    Notes: Summary A modified anthrone method is described for the determination of carbohydrates in fractions of lead(II)-chelate compounds of humic acids separated with chemical as well as gel-chromatographic methods. To reduce the disturbance of the method by the absorption of humic acids increasing with the decrease of wavelength, the absorbance of the anthronecarbohydrate reaction products is measured at 620 nm and the humic acid concentration is not allowed to exceed 0.1 g/dl. Because the molar absorptivity of the anthrone reaction-products depends on the type of carbohydrate investigated, the content is calculated for the main carbohydrate of the humic-acid hydrolysate (i.e. glucose).
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    Fresenius' Zeitschrift für analytische Chemie 295 (1979), S. 366-370 
    ISSN: 1618-2650
    Keywords: Best. von Quecksilber, Silber mit Formazanen ; Spektralphotometrie ; chelatbildende Ionenaustauscher
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Die Darstellung substituierter Formazane und ihre chemische Fixierung an Cellulose, amino- und chlormethyliertem Polystyrol wird beschrieben. Die Kapazitäten der Austauscher liegen zwischen 0,05 mÄq/g (Cellulose) und 0,6 mÄq/g (Polystyrol). In neutralem Medium zeigen sie eine besondere Affinität zu Hg(II), Pd(II) und Ag(I), aber keine Affinität zu Cu(II). Weiterhin wurde eine spektrophotometrische Bestimmung von Hg(II) und Ag(I) mit dem wasserlöslichen Formazan (FII)-NO2 ausgearbeitet [Hg(II): ɛ546=23 000 l Mol−1 cm−1, Ag(I): ɛ546 =38 000 l Mol−1 cm−1].
    Notes: Summary The preparation of substituted formazans and their fixation on cellulose, amino- and chloromethylated polystyrene is described. The capacities of the exchangers vary from 0.05 meq/g (cellulose) to 0.6 meq/g (polystyrene). They show in neutral medium greater affinity to Hg(II), Pd(II) and Ag(I), but no affinity to Cu(II). Further, a spectrophotometric determination of Hg(II) and Ag(I) with the watersoluble formazan (FII)-NO2 has been worked out. [Hg(II): ɛ546=23 000 l Mol−1 cm−1, Ag(I): ɛ546=38 000 l Mol−1 cm−1].
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    Fresenius' Zeitschrift für analytische Chemie 292 (1978), S. 233-235 
    ISSN: 1618-2650
    Keywords: Spektralphotometrie ; Ableitungen höherer Ordnung, Analogdifferenzierer, Derivativverfahren
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Es wird über eine neu entwickelte Analog-Recheneinheit berichtet, mit der man Ableitungen von Spektren und anderen Meßsignalen erstmalig bis zur 7. Ordnung on-line verwirklichen kann. Wie die Prüfungen ergaben, ist die optimale Auflösung in den meisten Fällen mit der 4. Ableitung erreicht. Dann sind nämlich alle Schultern und Wendepunkte der Kurven in bipolare Signale übergeführt. Eine Aufstellung der wichtigsten bisherigen Anwendungsgebiete wird gegeben.
    Notes: Summary This report deals with a newly developed analogue computing accessory by which derivations of spectra and other electric signals up to the seventh order were realized on-line. A thorough study of this apparatus showed that in most cases fine-resolving is reached by the fourth derivation. In this case, all shoulders and points of inflections are resolved to bipolar signals. A number of examples for applying derivative spectrophotometry of higher order (DSHO-method) is also given.
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  • 80
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    Fresenius' Zeitschrift für analytische Chemie 292 (1978), S. 400-402 
    ISSN: 1618-2650
    Keywords: Bestimmung von Meclozin, Pyridoxin in pharmazeutischen Produkten ; Spektralphotometrie ; Orthogonalfunktion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Summary A rapid spectrophotometric method for the analysis of tablets containing the title compounds without preliminary separation is developed. Thus, pyridoxine is determined by measurement at λ max while the six-points quadratic orthogonal polynomial has been used to determine meclozine. The mean percentage recoveries (8 determinations) were found to be 101.71±0.64 and 99.77±0.62% (P=0.05) for meclozine and pyridoxine hydrochlorides, respectively. Neither the Vierordt's nor the absorbance ratio methods gave accurate results as the proposed method. The method was applied successfully to the analysis of market preparations.
    Notes: Zusammenfassung Es wurde ein Verfahren zur schnellen Bestimmung der beiden Verbindungen ohne Vortrennung ausgearbeitet. Pyridoxin wird durch Messung beim Absorptionsmaximum von 292 nm bestimmt, Meclozin wird mit Hilfe eines quadratischen Sechspunkte-Orthogonalpolynoms berechnet. Die Wiederfindungsrate (8 Bestimmungen) lag bei 101,71±0,64 bzw. 99,77±0,62% (P=0,05). Vergleichsbestimmungen nach der Methode von Vierordt und dem Verfahren der Extinktionsverhältnisse gaben weniger genaue Resultate. Die vorgeschlagene Methode wurde mit gutem Erfolg auf handelsübliche Präparate angewendet.
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  • 81
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    Fresenius' Zeitschrift für analytische Chemie 278 (1976), S. 364-364 
    ISSN: 1618-2650
    Keywords: Best. von Nickel mit Äthylxanthat ; Spektralphotometrie
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    Topics: Chemistry and Pharmacology
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  • 82
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    Fresenius' Zeitschrift für analytische Chemie 293 (1978), S. 220-221 
    ISSN: 1618-2650
    Keywords: Best. von Magnesium ; Spektralphotometrie ; Trimethin-Reagentien aus Aminochalkogenuracilen
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Bekanntlich werden Trimethinfarbstoffe, als Reagentien für die photometrische Magnesiumbestimmung, durch die Kondensation von Malonaldehyd und Barbitursäure bzw. ihren Derivaten hergestellt. Auf ähnliche Weise erhält man mit 4(6)-Amino(2)-chalkogeno-uracilen und Malonaldehyd die Ammoniumsalze der Trimethinfarbstoffe, die sich ohne weitere Aufarbeitung als Reagentien für die photometrische Bestimmung einsetzen lassen. Die Herstellung der Verbindungen wird beschrieben.
    Notes: Summary It is known that trimethine dyes used for the photometrie determination of magnesium ions can be prepared by the condensation of malonicaldehyde with barbituric acid or its derivatives; In a similar way it is possible to use 4(6)-amino-2-chalcogeno-uracils giving with malonicaldehyde ammonium salts of the trimethine dyes, which are suited for the photometric determination without further manipulations. The preparation is described.
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  • 83
    ISSN: 1618-2650
    Keywords: Best. von Nickel, Kobalt mit 2-Carboxy-2′-hydroxy-3′,5′-dimethylazobenzol-4-sulfonsäure ; Spektralphotometrie
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  • 84
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    Fresenius' Zeitschrift für analytische Chemie 294 (1979), S. 356-360 
    ISSN: 1618-2650
    Keywords: Spektralphotometrie ; Mechanisierung, Prinzip, Optimierung
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Das Prinzip der Automatisierung der photometrischen Analyse mit kontinuierlichem Reagentienfluß und die speziellen Vorteile der Verwendung von Bausteinen der Flüssigkeits-Chromatographie werden ausführlich diskutiert. Die Optimierung folgender Parameter wird besprochen: Verweilzeit (Reaktionszeit), Einspritzmenge, Pumpgeschwindigkeit, Säulenabmessungen, Partikeldurchmesser.
    Notes: Summary The principle of automation of photometric analysis by the continuous flow method and the particular advantages of the use of component parts of liquid chromatography are discussed in detail. The optimization of the following parameters is pointed out: residence (reaction) time, injection volume, pumping rate, column dimensions and particle diameter.
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  • 85
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    Fresenius' Zeitschrift für analytische Chemie 295 (1979), S. 47-47 
    ISSN: 1618-2650
    Keywords: Best. von Vanadium in Stahl ; Spektralphotometrie ; Hydroxyphenyl-p-tolylbenzamidin
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    Topics: Chemistry and Pharmacology
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  • 86
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    Fresenius' Zeitschrift für analytische Chemie 295 (1979), S. 393-397 
    ISSN: 1618-2650
    Keywords: Best. von Tensiden in Wasser ; Spektralphotometrie ; Aniontenside, Reinigungsstufen
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Aniontenside werden an Feststoffen der Gewässer wie auch der Kläranlagen adsorbiert und teilweise angereichert. Ihre analytische Bestimmung erfordert eine mehrstufige Vorarbeit. Sie führt über die Extraktion des Probengutes, die Abtrennung der Tenside von Störstoffen durch Ausblasen (grobe Vorreinigung) und die chromatographische Reinigung der Rohfraktion auf Kieselgelschichten. Die Konzentration der reinen Tensidfraktion kann colorimetrisch oder IR-spektrometrisch bestimmt werden.
    Notes: Summary Anion tensides are adsorbed on solids in surface waters and sewage treatment plants and enriched to some extent. Their analytical determination requires multi-stage preparations, including sampling, separation of the tensides from disturbing material by air stripping (rough preliminary cleaning), and chromatographic cleaning of the raw fraction on silica gel. The concentration of the pure tenside fraction can be determined colorimetrically or by way of IR spectrometry.
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    Fresenius' Zeitschrift für analytische Chemie 297 (1979), S. 159-160 
    ISSN: 1618-2650
    Keywords: Best. von Vanadium(V) mit p-Hydroxybenzaldehyd und Hydroxyamidin ; Spektralphotometrie
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
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  • 88
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    Fresenius' Zeitschrift für analytische Chemie 292 (1978), S. 302-303 
    ISSN: 1618-2650
    Keywords: Best. von Aldehyden, aromat. mit Barbitursäure ; Spektralphotometrie. Best. von Barbitursäure mit p-Dimethylaminobenzaldehyd ; Spektralphotometrie
    Source: Springer Online Journal Archives 1860-2000
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  • 89
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    Fresenius' Zeitschrift für analytische Chemie 292 (1978), S. 359-361 
    ISSN: 1618-2650
    Keywords: Best. von Uran in Wasser ; Spektralphotometrie ; Arsenazo, Fällg. mit Al-Phosphat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Zur schnellen und genauen Bestimmung von Uranspuren in natürlichen, auch salzhaltigen Wässern, wird Uran durch Spurenfällung mit Aluminiumphosphat abgetrennt. Durch Auflösen des mit Zinkpulver vermengten Niederschlages erfolgt Reduktion zu U(IV), das mit Arsenazo III bestimmt wird. Der Extinktionskoeffizient beträgt 97000 cm2/Mol.
    Notes: Summary For the precise and accurate determination of uranium in natural, even saline, waters, it is separated by coprecipitation with Al-phosphate. The precipitate is mixed with zinc powder, dissolved and thus reduced to U(IV), which is determined with Arsenazo III. The molar absorptivity is 97000 cm2/mol.
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  • 90
    ISSN: 1618-2650
    Keywords: Best. von Phosphat neben Silicium, Arsen, Germanium ; Spektralphotometrie ; Extraktion mit Benzophenon, Molybdatmethode
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Summary A new type of separation of phosphate ion, along with its spectrophotometric determination, was established by liquid-liquid extraction, where the yellow heteropoly acid formed by the reaction with ammonium molybdate in acid solution is quantitatively extracted into molten benzophenone at a temperature of about 60° C. When cooled down to room temperature, the benzophenone extract converts from the liquid state to the solid state. The resulting solidified extract is dissolved in methyl propionate, and the phosphate ion in the solvent is determined spectrophotometrically by the blue heteropoly acid method. Possible interference by Si, As and Ge is eliminated by the separation procedure.
    Notes: Zusammenfassung Bei dem beschriebenen Verfahren wird die mit Ammoniummolybdat in saurer Lösung gebildete gelbe Heteropolysäure bei 60° C in geschmolzenes Benzophenon extrahiert. Dieses wird durch Abkühlen verfestigt, in Methylpropionat gelöst und in dieser Lösung das Phosphat spektralphotometrisch als blaue Heteropolysäure bestimmt. Si, As und Ge, die ebenfalls mit Molybdat reagieren, werden durch die Extraktion abgetrennt.
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  • 91
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    Fresenius' Zeitschrift für analytische Chemie 298 (1979), S. 158-158 
    ISSN: 1618-2650
    Keywords: Best. von Palladium, Ruthenium ; Spektralphotometrie ; Isonitrosodibenzoylmethan
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  • 92
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    Fresenius' Zeitschrift für analytische Chemie 298 (1979), S. 160-160 
    ISSN: 1618-2650
    Keywords: Best. von Ruthenium(III) mit 3-Hydroxy-3-(p-dimethylaminophenyl)-1-phenyltriazen ; Spektralphotometrie
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  • 93
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    Fresenius' Zeitschrift für analytische Chemie 277 (1975), S. 125-125 
    ISSN: 1618-2650
    Keywords: Best. von Arylidenmalonnitrilen ; Spektralphotometrie ; Dinitrobenzol als Reagens
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    Topics: Chemistry and Pharmacology
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  • 94
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    Fresenius' Zeitschrift für analytische Chemie 277 (1975), S. 127-127 
    ISSN: 1618-2650
    Keywords: Best. von Kobalt mit Tiron ; Spektralphotometrie
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  • 95
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    Fresenius' Zeitschrift für analytische Chemie 277 (1975), S. 127-127 
    ISSN: 1618-2650
    Keywords: Best. von Kupfer neben Nickel und Kobalt ; Spektralphotometrie ; Girard-T-deriv. von Hydroxynaphthaldehyd
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  • 96
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    Fresenius' Zeitschrift für analytische Chemie 277 (1975), S. 128-128 
    ISSN: 1618-2650
    Keywords: Best. von Tellur in Stahl ; Spektralphotometrie ; Se-haltiger Automatenstahl
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  • 97
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    Fresenius' Zeitschrift für analytische Chemie 277 (1975), S. 206-206 
    ISSN: 1618-2650
    Keywords: Best. von Zirkonium ; Spektralphotometrie ; Reagentienvergleich
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  • 98
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    Fresenius' Zeitschrift für analytische Chemie 296 (1979), S. 45-45 
    ISSN: 1618-2650
    Keywords: Best. von o-Dichlorbenzol ; Spektralphotometrie ; UV
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  • 99
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    Fresenius' Zeitschrift für analytische Chemie 296 (1979), S. 46-46 
    ISSN: 1618-2650
    Keywords: Best. von p-Methylaminophenolsulfat, Metol ; Spektralphotometrie
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  • 100
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    Fresenius' Zeitschrift für analytische Chemie 296 (1979), S. 406-407 
    ISSN: 1618-2650
    Keywords: Best. von Ligninsulfonsäure, Huminsäure in Wasser ; Spektralphotometrie ; UV
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    Topics: Chemistry and Pharmacology
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