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  • Lepidoptera
  • bioavailability
  • Springer  (31)
  • International Union of Crystallography
  • 1980-1984  (31)
  • 1940-1944
  • 1980  (31)
Collection
Publisher
  • Springer  (31)
  • International Union of Crystallography
Years
  • 1980-1984  (31)
  • 1940-1944
Year
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 17 (1980), S. 111-116 
    ISSN: 1432-1041
    Keywords: zimelidine ; norzimelidine ; antidepressants ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The systemic availability of a new antidepressant, zimelidine, and of its pharmacologically active metabolite, norzimelidine, was studied in six healthy male volunteers. Three single doses of zimelidine (25 mg and 100 mg orally and 25 mg i.v.) and two single doses of norzimelidine (25 mg orally and i. v.) were given to each volunteer allowing at least seven days between administrations. Plasma concentrations of zimelidine and norzimelidine were determined in serial blood samples by HPLC. Following oral zimelidine peak plasma concentrations of the metabolite were attained about 3 h after dosing. Oral administration of norzimelidine itself resulted in a plasma concentration profile for this compound that was similar to that observed after oral zimelidine. Utilising the plasma concentration data following intravenous infusion of each compound, the elimination half-lives for zimelidine and norzimelidine were calculated to be 5.1 h (range 4.3–6.0) and 15.5 h (range 10.6–22.9) respectively. The total body clearances of the 2 compounds were similar at 0.52 l · min−1 (range 0.26–0.70) for zimelidine and 0.56 l · min−1 (range 0.28–0.83) for norzimelidine. The substantially longer elimination half-life of norzimelidine was apparently the result of a larger volume of distribution (9.4 l · kg−1; range 7.8–11.4) for this metabolite, as compared to zimelidine (3.21 · kg−1; range 1.6–4.9). The calculated bioavailability of zimelidine was 26% (range 9.1–39) after the 25 mg oral dose, and 29% (range 14–46) after the 100 mg dose. The bioavailability of norzimelidine was 66% (range 36–91). However, oral administration of zimelidine resulted in as much or more norzimelidine reaching the systemic circulation, as the oral administration of norzimelidine itself. This is important as a large part of the activity of the drug may be due to the metabolite.
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  • 2
    Electronic Resource
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    Springer
    European journal of clinical pharmacology 18 (1980), S. 423-428 
    ISSN: 1432-1041
    Keywords: pyridostigmine ; myasthenia gravis ; pharmacokinetics ; bioavailability ; plasma levels
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of pyridostigmine was evaluated after intravenous injection in two healthy male volunteers and after oral administration to five subjects. Plasma concentrations of pyridostigmine were determined after ion pair extraction from plasma and analysis by gas chromatography — mass spectrometry with chemical ionization, using d6-pyridostigmine as internal standard. Degradation of pyridostigmine in vitro was compensated for by use of the deuterated internal standard and by rapid cooling and separation of plasma after blood sampling. After intravenous administration of pyridostigmine 2.5 mg the plasma elimination half-life was 1.52 h, the volume of distribution was 1.43 l/kg and the plasma clearance 0.65 l/kg × h. The pharmacokinetic constants were very similar after oral administration of pyridostigmine 120 mg; the elimination half-life was 1.78±0.24 h, the volume of distribution 1.64±0.29 l/kg and the plasma clearance was 0.66±0.22 l/kg × h. The bioavailability was calculated to be 7.6±2.4%. When pyridostigmine was taken together with food, the time to reach the peak plasma concentration was prolonged from 1.7 to 3.2 h. Bioavailability, however, was not influenced by concomitant food intake. “Steady-state” plasma concentrations of pyridostigmine were measured in myasthenic patients on their ordinary dose schedule of cholinesterase inhibitor drugs. More than a seven-fold difference in steady-state plasma concentration was found between patients taking approximately the same daily dose of pyridostigmine.
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  • 3
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    Springer
    European journal of clinical pharmacology 18 (1980), S. 415-418 
    ISSN: 1432-1041
    Keywords: diclofenac ; acetyl salicylic acid ; intravenous bolus administration ; oral administration ; interaction ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Previous studies have shown that aspirin interacts with orally administered diclofenac sodium, causing reduced peak concentrations, lower levels and decreased areas under curves. In this study, diclofenac sodium was administered orally and intravenously with and without aspirin, to 6 healthy female volunteers. After intravenous dosing both plasma levels and areas under curves were significantly reduced although none of the rate constants was affected. The volume of distribution of diclofenac was increased as was the plasma clearance. Oral administration with aspirin also resulted in lower plasma levels, particularly peak levels, and areas under curves. Comparison of AUC's for both modes of administration with and without aspirin suggested that lower levels after oral administration were not due to impaired absorption. These observations are best explained by decreased protein binding and increased biliary excretion of diclofenac in the presence of salicylate.
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  • 4
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    Springer
    European journal of clinical pharmacology 17 (1980), S. 309-315 
    ISSN: 1432-1041
    Keywords: valproic acid ; sodium valproate ; suppositories ; micro-enemas ; steady-state concentration ; absorption ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Rectal and oral absorption of valproic acid and its sodium salt by man were compared to explore the possibility of rectal administration of the drug. The plasma concentration of valproic acid was measured by gas chromatography after a single oral dose of sodium valproate 600 mg, and after single rectal doses of sodium valproate 600 mg and valproic acid 520 mg, in a cross-over study in 7 volunteers. The rectal dosage forms included fatty suppositories and aqueous solutions. Compared with oral administration, rectal absorption of sodium valproate from an aqueous micro-enema was fast and complete. The free acid was absorbed more rapidly from fatty suppositories than was the sodium salt. The absorption rate from the rectum increased with the dose of valproic acid. Both findings are consistent with a diffusion — absorption mechanism based on the pH-partition hypothesis. Differences in the chemical composition of the fatty suppository base were not reflected in differences in absorption rate and relative bioavailability. No essential difference in absorption rate was observed if volunteers remained lying or sitting during the experiment. Rectal dosing with valproic acid 520 mg dissolved in 4 ml suppositories, twice a day resulted in steady-state plasma concentrations of 50 to 100 µg · ml−1, within the therapeutic range.
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  • 5
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    Springer
    European journal of clinical pharmacology 17 (1980), S. 379-384 
    ISSN: 1432-1041
    Keywords: theophylline ; aminophylline ; obstructive lung disease ; microcrystalline ; bioavailability ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Variation in the systemic disposition of theophylline after ingestion of a new microcrystalline product (Theolair®) has been investigated in 7 hospitalized patients with generalized obstructive lung disease. Disposition (absolute bioavailability) was determined by comparing in the same patients the areas under the serum concentration-time curves after a single oral dose of microcrystalline theophylline and after an intravenous infusion of aminophylline. Oral absorption appeared to be fast. The half-life of absorption was 19±9 min (mean±SD). Maximal serum concentrations reached after 100±30 min were found to be in a rather narrow range: 9.8±2.5 mg · 1−1. The absolute bioavailability of the microcrystalline preparation was high and it showed only small variation: 102.7±10.2% of the dose. Relevant pharmacokinetic parameters (half-life of elimination, volume of distribution and total body clearance) were determined after both routes of administration. Individual dosage regimens required to obtain a therapeutic serum concentration were calculated for each individual patient on the basis of the observed pharmacokinetic parameters.
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  • 6
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    Springer
    European journal of clinical pharmacology 17 (1980), S. 375-378 
    ISSN: 1432-1041
    Keywords: mebendazole ; echinococcosis ; bioavailability ; absorption ; concomitant eating ; plasma level
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary High oral doses of mebendazole are used experimentally for the treatment of human alveolar and cystic echinococcosis. In order to assess bioavailability of this drug 1.5 g doses were given to 3 volunteers. Measurable plasma concentrations of 17 to 134 nmol/l were found only if mebendazole was given together with a fatty meal. In a patient with cholestasis plasma concentrations were higher than in the 3 normal subjects. In patients on long term treatment the increase in plasma concentration after administration of a 1 g dose varied between 0 and 500 nmol/l. It is concluded that systemic availability of mebendazole is enhanced by concomitant food intake. In view of the large intra- and interindividual variation in plasma concentration, monitoring plasma levels during long term therapy appears advisable.
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  • 7
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    European journal of clinical pharmacology 17 (1980), S. 465-468 
    ISSN: 1432-1041
    Keywords: paracetamol ; suppository ; tablets ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The relative bioavailability of a new paracetamol suppository (Panodil) and tablets in doses of 0.5 and 1 g was investigated in eight healthy subjects. The tablets were absorbed faster and higher peak plasma concentrations were obtained than after the suppositories. The bioavailability of the suppositories was approximately 80% of that of the tablets at both dose levels. There was no indication of capacity-limited elimination at either the two doses investigated.
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  • 8
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    European journal of clinical pharmacology 17 (1980), S. 209-213 
    ISSN: 1432-1041
    Keywords: disopyramide ; bioavailability ; controlled-release tablets ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma concentrations and bioavailability of disopyramide following repeated administration of standard capsules and controlled-release tablets have been compared. Ten patients were randomized into two groups; Group I received disopyramide capsules 150 mg every 6 h for five days and subsequently disopyramide controlled-release tablets 300 mg every 12 h for further five days. Group II received the same preparations in the reverse order. There was a more rapid rise in disopyramide concentration after the capsules: the maximum of 10.7±0.6 µmol/l (mean ± SEM) was reached within 1.8±0.4 h as compared to 10.6±0.4 µmol/l within 4.0±0.3 h after the controlled-release tablets. No significant difference in the fluctuations in individual plasma concentrations during each dose interval at steady state were observed after ordinary capsules compared to controlled-release tablets. The extent of bioavailability was the same. Eight patients reported some side-effects during the capsule period and nine during the controlled-release tablet period.
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  • 9
    Electronic Resource
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    Springer
    European journal of clinical pharmacology 17 (1980), S. 215-221 
    ISSN: 1432-1041
    Keywords: L-dopa ; elderly ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Previous studies have suggested that the absorption of L-dopa in the elderly Parkinsonian patient might be unusually efficient. In the present investigation, the systemic availability of L-dopa was examined in 5 elderly Parkinsonian patients (mean age=77 years) and 6 young, healthy volunteers (mean age=26 years) following a single oral 300 mg dose of L-dopa. Quantitation of plasma levels of intact L-dopa was effected by ion-exchange column chromatography and spectrofluorimetry. The L-dopa plasma concentration-time profiles obtained confirmed the considerable intersubject variability in the absorption of L-dopa previously reported in the literature. Maximum plasma concentrations of L-dopa generally occurred within 60 min of administration of the dose. The existence of more than one plasma peak of L-dopa concentration was displayed in 45% of the subjects studied. This characteristic was not confined exclusively to either subject group. There was a significantly larger (P〈0.02) area under the plasma L-dopa concentration-time curve (AUC o ∞ ) in the elderly Parkinsonian patients (mean=234.69 µg · min/ml; SD=84.70) compared to the young, healthy volunteers (mean=82.33 µg · min/ml; SD=31.00). A significant (P〈0.01) correlation existed between AUC o ∞ and age (r=0.7970; n=11) among the subjects studied. The apparent elimination phase plasma half-life of L-dopa in the elderly Parkinsonian patients (mean=66.0 min; SD=11.1) was not significantly different to that observed in the young, healthy volunteers (mean=74.0 min; SD=18.1). These results suggest that there may be an age-related alteration to the disposition of orally administered L-dopa in the elderly Parkinsonian patient.
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  • 10
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    European journal of clinical pharmacology 17 (1980), S. 385-391 
    ISSN: 1432-1041
    Keywords: sulpiride ; pharmacokinetics ; serum clearance ; renal clearance ; bioavailability ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of sulpiride was studied in 6 healthy volunteers after intravenous and oral (tablets) administration of 100 mg. An open two- and in two subjects a three-compartment model was applied following intravenous administration. The average total distribution volume during the terminal slope was 2.72±0.66 l/kg and total systemic clearance was 415±84 ml/min. The serum half-life of the terminal slope following intravenous administration averaged 5.3 h (range 3.7–7.1 h) according to the two-compartment model. In two subjects the half-lives were 11.0 and 13.9 h when the three-compartment model was applied. Determination of urinary excretion rates of unchanged sulpiride indicated a half-life of 7.15 h. Following intravenous administration, 70±9% of the dose was recovered unchanged in urine within 36 h; the mean renal clearance was 310±91 ml/min. Sulpiride was absorbed slowly, with peak concentrations appearing between 3 and 6 h after oral administration. The recovery of unchanged drug in urine following oral administration was 15±5% of the dose, with a mean renal clearance of 223±47 ml/min. The bioavailability determined from combined plasma and urine data was only 27±9%. The low bioavailability was probably due to incomplete absorption.
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  • 11
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    European journal of clinical pharmacology 18 (1980), S. 43-50 
    ISSN: 1432-1041
    Keywords: enteral drug absorption ; development ; bioavailability ; neonates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary There is little information about enteral drug absorption during development compared to that about drug distribution, metabolism and excretion. Therefore, the bioavailability, i.e. the amount and rate of absorption of various drugs (sulfonamides, phenobarbital, digoxin, β-methyldigoxin) and test substances (D(+)-xylose, L(+)-arabinose) was investigated in 580 children using pharmacokinetic methods. The amounts of the drugs absorbed, determined by Dost's law of corresponding areas, showed no age dependence. But the rate of absorption, ka, calculated from the concentration time curves using a digital approximation procedure (RIP), is low at the time of birth and reaches adult values after the neonatal period. This phenomenon is identical for all of the substances tested. A prolonged gastric emptying time in the neonate does not seem to be responsible for the delayed absorption since the lagtime is not related to age. Stimulation of intestinal motility with metoclopramide increases the absorption rates, both in neonates and older children, but the age dependent differences remain. Using various dosages of L(+)-arabinose the parameters of the saturation kinetics could be determined. In neonates Vmax values are significantly lower than in older children. Similarly, the affinity constant $$\mathop K\limits^ \star$$ indicates a decreased capacity of enteral absorption in neonates compared with older children. Bioavailability data from adults cannot be accepted without further investigation since the rate of enteral drug absorption depends on age.
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  • 12
    ISSN: 1573-1561
    Keywords: Oriental fruit moth ; orfralure ; sex pheromone ; traps ; air permeation with pheromone ; Lepidoptera ; Olethreutinae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Orfralure [93% (Z), 7% (E)-8-dodecen-1-ol acetate], the synthetic pheromone of the oriental fruit moth,Grapholitha molesta (Busck), was released into the air of orchard test plots either by hanging plastic laminated dispensers on trees or by aerial dispersal of microcapsules containing a solution of the lure. Trap catch was reduced 95% or more with the most effective formulations, but consistently higher reductions were produced by the dispensers. In tests as long as 28 weeks with dispensers, a single retreatment at midseason maintained an effective concentration.
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  • 13
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    Journal of chemical ecology 6 (1980), S. 213-220 
    ISSN: 1573-1561
    Keywords: Olfactory receptors ; chemoreception ; Lepidoptera ; Lasio-campidae ; plant volatiles ; tent caterpillars ; Malacosoma americanum
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Volatile constituents of leaves of acceptable and unacceptable plants evoke multiunit responses from the antennal olfactory sensilla of larvae of the eastern tent caterpillar. Electrophysiological investigation of the activities of three of the sixteen antennal olfactory receptors revealed that different combinations of the three responded to the various plants. In those instances where the same combination responded to more than one species of plant, the ratios of responses measured as frequency of action potentials were often different. Thus, discrimination of different plants theoretically could be based upon the absolute number of cells responding and/or the ratios of frequencies.
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  • 14
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    Journal of chemical ecology 6 (1980), S. 565-572 
    ISSN: 1573-1561
    Keywords: Armyworm ; Mythimna unipuncta ; Pseudaletia unipuncta ; Leucania unipuncta ; Cirphis unipuncta ; Lepidoptera ; sex pheromone ; sex attractant ; (Z)-11-hexadecen-1-ol acetate ; (Z)-9-hexadecen-1-ol acetate ; hexadecan-1-ol acetate ; (Z)-11-hexadecen-1-ol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract (Z)-11-Hexadecen-1-ol acetate (Z11–16∶Ac) free of theE isomer (〈1%), hexadecan-1-ol acetate (16∶ Ac), and a hexadecen-1-ol [the (Z)-11 isomer based on the retention time on a Carbowax capillary column] were identified in extracts of the sex pheromone glands of adult virgin female armyworms,Pseudaletia unipuncta. Also, gas Chromatographic retention times on polar and nonpolar columns indicated the possible presence of (Z)-9-hexadecen-1-ol acetate (Z9–16∶Ac). The ratioZ11–16∶Ac/16∶Ac/Z11–16∶OH/Z9–16∶Ac was 1∶0.15∶0.13∶0.02. Infield testsZ11–16∶ Ac was attractive alone, and the addition ofZ9–16∶Ac,Zll–16 ∶ OH, or 16 ∶ Ac singly or in combination in ratios found in the gland did not increase trap capture.
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  • 15
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    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 463-481 
    ISSN: 1573-8744
    Keywords: bioavailability ; absorption ; deconvolution ; computer program for deconvolution ; algorithm for deconvolution ; drug input evaluation ; input response in linear pharmacokinetic systems ; pentobarbital absorption ; cimetidine absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The procedure of deconvolution to evaluate the rate and the extent of input from absorption data and data from intravenous administration is the most fundamental and least assumptive method of accurately evaluating drug absorption in linear pharmacokinetics. It is shown for linear systems that if the absorption response and the response from an intravenous infusion or bolus administration are both well approximated by a polyexponential function, then the rate of absorption can be expressed as a sum of exponentials. An algorithm and computer program are presented whereby the absorption function is uniquely defined from the model-independent parameters of the polyexponential expressions fitted to the absorption data and data from intravenous administration. Fitting a sum of exponentials to data has become a routine procedure in pharmacokinetics. The method presented therefore makes the previously complex task of deconvolution a simple procedure. The deconvolution approach is discussed in relation to conventional methods of evaluating drug absorption and appears to have some distinct advantages over these methods. The method is tested using simulated data and demonstrated using pentobarbital and cimetidine data from human subjects.
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  • 16
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    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 243-255 
    ISSN: 1573-8744
    Keywords: quinidine ; bioavailability ; absorption ; solutions ; rapidiy releasing tablets ; humans
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The gastrointestinal absorption of quinidine from three commercially available tablet products has been compared to that from a quinidine sulfate solution previously found to have 70% of the systematic availability of an intravenous dose. Quinidine gluconate solution was included in the study to compare the absorption characteristics of the two quinidine salts. The tablets were given in a counterbalanced sequence preceded by one quinidine solution and followed by the other in a crossover design. The three tablets proved to be equivalent to one another with respect to extent and rate of absorption. The absorption properties of the two solutions were indistinguishable. The tablets were equivalent to the solutions in extent but not in rate of absorption.
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  • 17
    ISSN: 1573-8744
    Keywords: theophylline ; absorption ; bioavailability ; enteric release ; tablets ; plasma concentrations ; dissolution data
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract In a single-dose bioavailability study, Wales, Robinson, Columbia, and Choledyl (Warner/Chilcott) enteric-coated tablets all allowed a bioavailability of theophylline (99%±25%, 102%±23%,103%±18%, and 98%±15%;mean±SD, n=12) statistically indistinguishable from that of the standard uncoated tablet (Searle 200 mg aminophylline). Only the Wales and Choledyl tablets (7.6, 4.2 hr) could be shown (p〈0.05) to generate a peak plasma theophylline concentration later than the standard (1.4 hr). All tablet brands demonstrated a significant lag time before appearance of theophylline in the plasma, and both Wales and Choledyl tablets also had a (t peak -t tag )statistically different from that of the standard. Despite misleading indications from the mean plasma profile (plasma concentrations at each sampling time averaged over all subjects), plasma data from the individual participants and in vitrodissolution data show that, while release of theophylline from the Wales tablet might be inordinately slow, this is not a sustained-release preparation. Of the enteric-coated tablets only the Columbia product allowed significant levels in the first sample after dosage. Five of the 18 Columbia doses gave rise to 40–99%of the peak concentration in the 1- hr sample. In vitro,it takes 39±14 min for 40% of the theophylline content of Columbia tablets to dissolve in simulated intestinal fluid. Surprisingly rapid delivery of an entericcoated tablet to the duodenum would appear to be required to allow a significant percentage of theophylline to be dissolved and absorbed before 1 hr. None of 12 Columbia tablets tested in vitro,however, allowed dissolution of more than 0.2% of their theophylline content during 1 hr immersion in simulated gastric fluid. Since once in intestinal fluid Columbia tablets appear to dissolve more rapidly than the other enteric products, it is not clear whether the five Columbia tablets in question had imperfections or whether, in fact, this tablet brand more closely than the others represents the ideal of immediate release once in the duodenum. Plasma samples should be taken as early as 15 min after dosage when evaluating the bioavailability of enteric release products.
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  • 18
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    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 347-362 
    ISSN: 1573-8744
    Keywords: griseofulvin ; bioavailability ; HPLC assay ; plasma levels ; human study
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The relative bioavailability of ten marketed dosage forms of griseofulvin was evaluated in two separate crossover studies. Each study utilized 12 healthy subjects, with eight of the subjects being common to both studies. Plasma griseofulvin concentrations were determined 1, 2, 3, 4, 6, 8, 10, 25, 34, 49, and 73 hr after dosing, using a high-pressure liquid chromatographic method. The “high-dose” study compared four microsize dosage forms administered as 500-mg doses and two ultramicrosize formulations given as 250-mg doses. The “low-dose” study employed four 250-mg microsize products and two 125-mg ultramicrosize products. The individual plasma level-time profiles for the majority of doses suggested prolonged absorption of microsize griseofulvin. The ultramicrosize dosage forms exhibited peak concentrations which were not significantly different (p〉0.05) from those of the microsize products administered as twice the dose. In the high-dose study, the two 250-mg ultramicrosize dosage forms exhibited areas under the plasma level-time curve (AUC) which were significantly (p〈0.05) less than the AUCs for all but one of the 500-mg microsize products. In the low-dose study the AUCs for the ultramicrosize products were significantly lower than the AUCs for all of the microsize dosage forms. Significant differences were also noted among the AUCs for the microsize products, although the maximum difference was less than 20% in both studies. A comparison of the AUCs observed in the high- and low-dose studies revealed that the AUCs for two of the 500-mg microsize dosage forms were only approximately 75% the AUC predicted from the 250-mg dose for the eight subjects common to both studies. All other formulations exhibited a dose proportionality for AUC.
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  • 19
    ISSN: 1573-8744
    Keywords: theophylline ; absorption ; bioavailability ; sustained release ; tablets ; plasma concentrations ; mean plasma concentrations ; steady-state projections
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Absorption of theophylline from three commercial products labeled as sustained release was compared to the absorption from a standard uncoated tablet (Searle 200-mg aminophylline tablet) in a single-dose study. Aminodur tablets (Cooper) and Slophyllin Gyrocap capsules (Dooner) had bioavailability (100.2%±19.8% and 98.5%±13.8%) statistically indistinguishable from that of the standard but showed significantly slower absorption (peak times of 10,4±2.8 and 4.36±1.35 hr) and lower peak plasma concentrations (13.9±4.5 and 22.6±3.5gmg/ml/g dose) than the standard (t peak ,1.52±0.45 hr; Cpeak,28.l±6.2μg/ml/g dose). The time of the plasma concentration peak (2.47±1.38 hr) after a dose of Tedral S.A. (Warner/Chilcott) was not statistically different from that after the standard, but both the peak concentration (16.0±3.9 gmg/ml/g dose) and bioavailability (76.0±18.4%) were. Multiple-dose projections from single-dose data indicate that of the three test products only Aminodur maintains reasonably constant interdose plasma levels during 12 hourly dosing. With an 8 hourly dosing schedule Gyrocaps also might be satisfactory. Reasonable predictions of the plasma concentrations arising from Aminodur doses have been made using a single-compartment body model and assuming input from an outer followed by an inner layer of the tablet. Typically a single dose of a preparation designed for constant release of drug over 12 hr should not produce a plasma concentration plateau in subjects with an average 6.1-hr drug half-life. The apparent plateau in the mean plasma profile (i.e., concentrations at each sampling time averaged over all subjects) for Aminodur doses is evaluated. The interpretation commonly being implied in the publication of mean profiles from bioavailability studies is misleading, particularly when applied to sustained-release preparations.
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  • 20
    ISSN: 1573-1561
    Keywords: Sex attractant ; trapping ; redbacked cutworm moth ; Euxoa ochrogaster ; Lepidoptera ; Noctuidae ; (Z)-5- and (Z)-7-dodecenyl acetates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Mixtures of (Z)-5- and (Z)-7-dodecenyl acetates in ratios 〉100∶1 are powerful, specific sex attractants for redbacked cutworm male moths. Bioactive lures were produced by admixture of these pure compounds or through syntheses involving catalytic bond shifting. Best field trapping was obtained with 200∶1 (Z)-5∶(Z)-7 ratio, at lure doses (on rubber) of 0.1–2.0 mg, using cone swivel traps with 10- to 13-mm orifices, or Pherocon® 1-CP sticky traps, at a height of 50–90 cm. The pheromone traps were more efficient than large blacklight traps and captured the various morphological forms of the moth in similar ratios.
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  • 21
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    Journal of chemical ecology 6 (1980), S. 797-804 
    ISSN: 1573-1561
    Keywords: Sex pheromone ; Sparganothis ; Lepidoptera ; Tortricidae ; (E)-11-tetradecen-1-ol ; (Z)-11-tetradecen-1-ol ; (E)-11-tetradecen-1-ylacetate ; (Z)-11-tetradecen-1-ylacetate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The sex pheromone of the woodbine leafroller,Sparganothis sp., includes (E)-11-tetradecen-1-ol, (Z)-11-tetradecen-1-ol, and (E)-11-tetradecen-1-yl acetate, based on chemical analysis of gland extracts, electroantennogram tests, and field trapping. Highest trap catches were obtained when these compounds were dispensed in the relative proportions observed in the female gland. (Z)-11-Tetradecen-1-yl acetate also was found in gland extracts, but significantly reduced trap catches. The saturated compounds tetradecan-1-ol and tetradecan-1-yl acetate were found in gland extracts as well, but were not tested. The amounts of these compounds per female gland were 127, 93, 17, 20, 25, and 3 ng, in the order named.
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  • 22
    ISSN: 1573-1561
    Keywords: Sex pheromone ; attractance ; behavioral threshold ; Plodia interpunctella ; Indian meal moth ; Lepidoptera ; Pyralidae ; orientation ; chemical communication
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Methods are presented for mathematically determining dispersal of a vapor in still air, in turbulent air of zero average velocity, and in turbulent or laminar air currents of constant, nonzero average velocity. The methods are combined with several assumptions about insect behavior to derive an insect attraction model that predicts: (1) In a warehouse a searching insect is likely to be attracted to a calling insect if it comes within an attraction sphere, 0.4–2.5 m in radius. (2) The attraction spaces of typical sex pheromone-baited traps that emit pheromone at rates greater than 0.01 ng/sec extend beyond the boundaries of a 10 × 10 × 10-m warehouse. (3) The searching behavior of an attracted insect is likely to be altered from an extensive to an intensive pattern if it comes within an altered-behavior sphere, 6–60 cm from a calling insect or within 10 m of a trap emitting 0.76 ng/sec. (4) Pheromone does not sink unless it is emitted along with a large amount of a high-vapor pressure solvent. The model is used in support of several hypotheses, including: (1) The effect of an adsorptive surface on the vapor concentration after an extended period of emission is negligible except at positions near the surface. (2) Sex pheromone-baited traps with sources of small dimensions have greater trapping efficiency than otherwise identical traps with sources of large dimensions.
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  • 23
    ISSN: 1573-1561
    Keywords: Electroantennographic detector ; Euxoa ochrogaster ; Lepidoptera ; identification ; mass chromatograms ; mass spectrometry ; redbacked cutworm ; sex pheromone ; (Z)-5-dodecenyl acetate ; (Z)-7-dodecenyl acetate ; (Z)-9-dodecenyl acetate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Pheromone washes from calling female moths of redbacked cutworm,Euxoa ochrogaster (Guenée), contained the following acetates that are structurally similar to those of known lepidopteran pheromones (%): decanyl (8.7), dodecanyl (8.5), (E)-5-dodecenyl (3.3), (Z)-5-dodecenyl (76.4), (Z)-7-dodecenyl (3.1), and (Z)-9-dodecenyl (trace〈0.5%). This is the first time that (Z)-5-dodecenyl acetate has been identified as a pheromone component. Three types of specific receptor cells were found in the male antennae, and they responded to (Z)-5-decenyl acetate, (Z)-5- and (Z)-7-dodecenyl acetates, respectively. Strong electroantennographic detector responses were also recorded for these three acetates and for (Z)-5-undecenyl acetate. The evidence for the presence of (Z)-5-decenyl acetate in the pheromone washes was inconclusive. The presence of (Z)-7- and the absence of (Z)-8-dodecenyl acetates were confirmed by a special electroantennographic detector technique in which the detector antennae were from males of other species that were known to have strong responses to these acetates. This is a very useful technique. Field results show that low concentrations (0.1–1.3%) of (Z)-5-decenyl acetate were synergistic when tested in a previously reported blend, but 6% was inhibitory. Similarly, (Z)-7-dodecenyl acetate at 2% or less may be essential for the attraction of males, but in previous tests at 14% it also was inhibitory. Species-specific attractant blends for redbacked cutworm males are described.
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  • 24
    Electronic Resource
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    Journal of chemical ecology 6 (1980), S. 867-873 
    ISSN: 1573-1561
    Keywords: Male scent ; Atrophaneura alcinous ; Lepidoptera ; Papilionidae ; benzaldehyde ; phenylacetaldehyde ; 2-phenylpropenal ; n-heptanal ; 6-methylhept-5-en-2-one ; linalool
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Benzaldehyde, phenylacetaldehyde (major component), 2-phenylpropenal,n-heptanal, 6-methylhept-5-en-2-one, and linalool were identified as compounds responsible for the male scent ofAtrophaneura alcinous alcinous. These substances were present predominantly in the wings, and the quantity of them was largest at the inner margin of the hind wing. Female wings also contained some of them in much smaller (except a few components) amounts. The relative proportion of each component exhibited manifests sexual differences.
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  • 25
    ISSN: 1573-1561
    Keywords: Sex pheromone ; anemotaxis ; Plodia interpunctella ; Lepidoptera ; Pyralidae ; behavioral threshold ; behavioral alteration threshold ; (Z,E)-9,12-tetradecadien-1-ol acetate ; Indian meal moth
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The effect of different concentrations of the sex pheromone (Z,E)-9,12-tetradecadien-1-ol acetate on the upwind anemotactic behavior of the malePlodia interpunctella (Hübner) was measured at 23 ± 1 ° C and 34 ± 1 ° C. The stimulus-response regression lines were analyzed by a new procedure that accounts both for control responses in the absence of pheromone and also for peak responses below 100% in the presence of concentrations considerably above the normal physiological levels. From the regression line for each temperature, the upwind anemotactic thresholds were calculated to be 1.34 × 106 molecules/cm3 at 23 ° C and 1.65 × 104 molecules/cm3 at 34 ° C, similar to other thresholds reported in the literature. Since departures from the two lines occurred at the highest concentrations tested, near 108 molecules/cm3, the upwind anemotactic behavior may change qualitatively above an altered-behavior threshold that is about two orders of magnitude higher than the upwind anemotactic threshold. The lower response at 23 ° C suggests that cool temperatures inhibit flight in response to pheromonal stimulation.
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  • 26
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    Journal of chemical ecology 6 (1980), S. 13-26 
    ISSN: 1573-1561
    Keywords: Butterfly ; Colias philodice ; chemical communication ; Lepidoptera ; Pieridae ; male scent ; courtship ; sex brands
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract During successful courtship in sulfur butterflies, virgin females respond to males by assuming a stationary posture and extending the abdomen ventrally from between the hindwings, thereby permitting copulation. In the clouded sulfur,Colias philodice Godard, this response was used in a laboratory bioassay to confirm the existence of a male chemical signal demonstrated by a previous worker and to document the signal's behavioral function and source. The male scent is shown to be required, in part, to reliably elicit abdominal extension and to be emitted from a patch of cells and scales associated with the dorsal surface of the male hind wing near the wing base. Experiments also show that evaporation of the signal is reduced when the source is covered by the forewing as it is at rest and in flight. These data, coupled with other information on male chemical signals in sulfur butterflies and other Lepidoptera, suggest that in sulfurs the morphology and chemistry of the scent glands along with the behavior of the male are structured in a way that minimizes the evaporative loss of scent from the wings when the male is not courting females.
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  • 27
    ISSN: 1573-1561
    Keywords: Sex attractant ; sex pheromone ; lesser peachtree borer ; field test design ; Synanthedon pictipes ; clearwing moths ; Lepidoptera ; Sesiidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Trap capture data from Ohio and Wisconsin show that (E,Z)-3-13-octadecadien-1-ol acetate alone is an effective trap bait for maleSynanthedon pictipes (Grote and Robinson). Attractiveness increased by increasing attractant concentration but not by adding theZ,E geometrical isomer.S. pictipes males partitioned themselves in a linear fashion among traps baited with 10–100 μg of attractant in 10-μg increments. Furthermore, they discriminated between 50- and 100-μg baits placed in the same tree. These and other results indicate that, in clearwing experiments involving noninhibitory compounds and blend tuning, high trap density can be used successfully.
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  • 28
    ISSN: 1573-1561
    Keywords: Cardenolides ; monarch butterfly ; Danaus plexippus L. ; Lepidoptera ; Danaidae ; storage ; regulation ; metabolism ; uscharidin ; calactin ; calotropin ; uzarigenin ; digitoxigenin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Adult monarch butterflies,Danaus plexippus L. (Lepidoptera: Danaidae), store only some of the cardenolides present in the larval milkweed (Asclepiadaceae) host. Feeding known doses of individual cardenolides to 4th instar monarch larvae led to more efficient larval tissue incorporation at low doses than at high ones, and favored storage of cardenolide glycosides over genins. A qualitative regulation also occurs during larval feeding; calactin and calotropin were stored as such but uscharidin was rapidly converted to a mixture of calactin and calotropin which were the forms stored by the larvae. Two genins, uzarigenin and digitoxigenin, were stored by larvae as polar cardenolide metabolites.
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  • 29
    ISSN: 1573-1561
    Keywords: Range caterpillar ; Hemileuca oliviae ; Lepidoptera ; Saturniidae ; trail pheromone ; aggregation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Methylene chloride-extractable chemical(s) from range caterpillar larval silk facilitates trail-following and aggregation by early-instar larvae, but late-instar larvae are less responsive to the pheromone. Larval aggregation does not reduce water loss when larvae are exposed to low humidity, nor does aggregation prevent predation by the antFormica neoclara Emery. Grouped larvae gain weight and complete early stadia more rapidly as compared to solitary larvae. Aggregation may provide increased visibility to herbivores and increase the impact of urticating spines, thereby decreasing inadvertant predation.
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  • 30
    ISSN: 1573-1561
    Keywords: Dodecyl acetate ; sex pheromone ; Trichoplusia ni ; Lepidoptera ; Noctuidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Dodecyl acetate was identified as a second component of the sex pheromone ofTrichoplusia ni (Hübner). Dodecyl acetate comprised 9.6% by weight of the total pheromone [(Z)-7-dodecenyl acetate plus dodecyl acetate] extracted from glands and 7.3% by weight of the total pheromone evaporated from the surfaces of glands. Dodecyl acetate appears to function as a short-range pheromone component. Evaporation at female release rates of a 10∶90 mixture of dodecyl acetate and (Z)-7-dodecenyl acetate in the field caused a significantly greater percentage of males to land on the pheromone source, increased significantly the time they spent on the source, but decreased significantly the time they spent searching for the source when within 50 cm, as compared to (Z)-7-dodecenyl acetate alone.
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  • 31
    ISSN: 1573-1561
    Keywords: Release rate ; polyethylene ; formulations ; controlled release ; (Z)-9-tetradecen-1-ol formate ; Heliothis zea ; Lepidoptera ; Noctuidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The release rates of (Z)-9-tetradecen-1-ol formate (Z9TDF) from four sizes of polyethylene tubing were measured periodically for 50 days by collecting the Z9TDF vapors on a polymeric adsorbent. The resulting release rate curves had shapes that were determined by the tubing's diameter and wall thickness. One tubing size that combined good longevity with adequately high release rates was tested in the field to determine whether it could disrupt pheromone communication of the corn earworm,Heliothis zea (Boddie). We observed a low percentage of disruption, but release rate measurements made concurrently showed that the tubing was releasing Z9TDF normally. In a second field test, a larger quantity of Z9TDF was released, and 87% disruption was attained for 66 days.
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