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  • bioavailability  (33)
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  • Springer  (61)
  • Annual Reviews
  • Nature Publishing Group
  • 1980-1984  (61)
  • 1982  (61)
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  • Springer  (61)
  • Annual Reviews
  • Nature Publishing Group
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  • 1980-1984  (61)
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 21 (1982), S. 373-377 
    ISSN: 1432-1041
    Keywords: propranolol ; sotalol ; thyrotoxicosis ; bioavailability ; serum tri-iodothyronine ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The elimination and bioavailability of two beta-blocking agents, propranolol and sotalol, were studied in 10 thyrotoxic patients, both before and after treatment with iodine-131. Each subject received in random order propranolol 160 mg and sotalol 160mg as single oral doses both while hyperthyroid and after euthyroidism had been achieved. The pharmacokinetics of sotalol was not affected by hyperthyroidism, whereas serum propranolol concentrations were significantly lower during hyperthyroidism than in the euthyroid state. During hyperthyroidism, the bioavailability of propranolol was significantly reduced (p〈0.05) and its clearance was increased (p〈0.005), whereas there was no difference in its serum t1/2. This indicates that the bioavailability of propranolol in hyperthyroidism is reduced by a mechanism which may depend on increased first-pass metabolism in the liver, or on an increased distribution volume of the drug. Both propranolol and sotalol caused a slight decrease in serum tri-iodothyronine concentration. As the effects of beta-blocking agents on the symptoms of hyperthyroidism are correlated with the serum concentration of the drugs, sotalol, with its long half-life and unaltered elimination in hyperthyroidism, has certain advantages over propranolol in the treatment of thyrotoxicosis.
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  • 2
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    European journal of clinical pharmacology 22 (1982), S. 309-314 
    ISSN: 1432-1041
    Keywords: acetylsalicylic acid ; salicylic acid ; dipyridamol ; bioavailability ; kinetics ; rapid- and slow-release formulations
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Acetylsalicylic acid (ASA) is a strong, irreversible inhibitor of platelet aggregation, but loses this activity following first-pass deacetylation to salicylic acid (SA). In order to compare the bioavailability of unchanged ASA from rapid- and slow-release formulations, the single-dose concentration profiles of ASA and SA were studied in healthy volunteers following intake of two different rapid-release (conventional and effervescent tablets) and three different slow-release (microencapsulated ASA in tablets and in capsules, and enteric-coated tablets) formulations of ASA, and of one slow-release formulation of sodium salicylate. Since anti-platelet therapy with ASA is often combined with dipyridamol, the influence of this drug was also examined. The concentrations of ASA and SA were measured by high-pressure liquid chromatography. While the bioavailability of SA from the 5 ASA formulations was essentially equal and similar to that of the salicylate formulation, the bioavailability and peak concentrations of ASA appeared to be the much greater after rapid-release than after slow-release formulations. Indeed, ASA was only rarely detected in systemic blood following intake of slow-release ASA. Co-administered dipyridamol did not significantly influence the kinetics of ASA or SA. It appears that rapid-release formulations of ASA should be prefered in anti-platelet therapy, either alone or in combination with dipyridamol.
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  • 3
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    European journal of clinical pharmacology 22 (1982), S. 85-90 
    ISSN: 1432-1041
    Keywords: lignocaine ; verapamil ; propranolol ; bioavailability ; predictions ; first pass effect ; oral clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary For drugs with a high hepatic clearance, bioavailability is low due to the so-called “first pass effect”. Prediction of the bioavailability for these drugs has been only lossely tested. It is proposed that by plotting the reciprocal of bioavailability versus the oral clearance, a straight line with intercept of unity and slope of reciprocal of hepatic blood flow should ensue. For lignocaine and verapamil, this relationship was found to be strong and gave good predictability, whereas for propranolol this relationship was weak and gave poor predictability. The proposed method may be of value in determining whether the low bioavailability of a drug is due to hepatic first pass metabolism.
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  • 4
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    European journal of clinical pharmacology 23 (1982), S. 59-64 
    ISSN: 1432-1041
    Keywords: morphine ; rectal administration ; i.m. administration ; gas chromatographic mass spectrometric analysis ; bioavailability ; plasma levels
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 21 healthy women undergoing gynaecological operations received rectal premedication with morphine 0.3 mg/kg body weight. Plasma concentrations of morphine were followed for 4 h by a GC/MS technique. In most patients the peak plasma concentration was reached after 30 min; the mean peak plasma level of morphine was 18 ng/ml (range 8.5–57 ng/ml). The bioavailability of rectal morphine was determined in 6 patients, who received an i.m. injection of morphine at a second operation. The mean bioavailability of rectal morphine was 31% (range 12%–61%). None of the patients showed any clinical sign of respiratory depression, and there was no increase in end-tidal carbon dioxide tension measured in 5 patients operated under spinal block.
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  • 5
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    European journal of clinical pharmacology 23 (1982), S. 235-240 
    ISSN: 1432-1041
    Keywords: ergotamine ; pharmacokinetics ; migraine ; plasma drug levels ; i.v. administration ; i.m. administration ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of ergotamine has been investigated in migrainous patients using a new, specific, sensitive HPLC assay (detection limit 100 pg/ml plasma). 10 patients were given ergotamine tartrate 0.5 mg i.v. and 5 of them received the same dose i.m. 2–3 weeks later. Blood samples were collected for up to 54 h following administration and the plasma concentration were analysed. After intravenous administration the plasma ergotamine declined rapidly, with an initial distribution half-life of 3 min followed by a mean terminal half-life of 1.86 h (range 90–155 min). The mean total plasma clearance was 11.0 ml kg−1 min−1, and the volume of distribution (Vdβ ) was 1847.6 ml kg−1. Individual t1/2β showed a positive linear correlation with the individual Vdβ . The intramuscular absorption of ergotamine was rapid and maximum plasma levels were usually obtained 10 min following administration. The biological availability was incomplete and variable at 46.6% (range 28.3–60.8%).
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  • 6
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    European journal of clinical pharmacology 23 (1982), S. 249-252 
    ISSN: 1432-1041
    Keywords: mecillinam ; bacmecillinam ; pivmecillinam ; pharmacokinetics ; pro-drug ; healthy volunteers ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of bacmecillinam and pivmecillinam were studied in healthy fasting volunteers given tablets in a cross-over, randomized order. The mean (±SD) peak levels of plasma mecillinam were 1.43±0.34, 2.73±0.43, and 4.62±1.41 mg/l after bacmecillinam 100, 200, and 400 mg and 2.38±0.65 mg/l after pivmecillinam 400 mg. The corresponding areas under plasma Vs time curves (AUC) were 2.21±0.19, 3.99±0.63, and 7.74±1.38 mg·h·l−1 for bacmecillinam and 5.35±0.93 mg·h·l−1 for pivmecillinam. The elimination half-lives were 0.8–1.1h for bacmecillinam and 0.7h for pivmecillinam. The 12 h urinary recovery of unchanged mecillinam after the 400 mg doses was 41% for bacmecillinam and 30% for pivmecillinam. The 400 mg dose of bacmecillinam gave a significantly higher plasma peak (p〈0.001), AUC (p〈0.001) and urinary recovery (p〈0.001) than did pivmecillinam 400 mg. The plasma peaks appeared earlier and the rate of absorption was higher after bacmecillinam than after pivmecillinam (p〈0.05). In conclusion, bacmecillinam had a better bioavailability than pivmecillinam in the tablet formulations studied. The AUC increased linearly with increasing doses of bacmecillinam.
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  • 7
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    European journal of clinical pharmacology 22 (1982), S. 265-272 
    ISSN: 1432-1041
    Keywords: pharmacokinetics ; variation of absorption ratios ; bioavailability ; dissection of variation due to absorption and intermediate processes ; oral drug application
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Differences in the plasma concentrations of drugs after oral administration are caused by two main factors: variation in absorption ratios and in the distribution processes in the body. A new method for the dissection of both types of factors is discussed. The method uses a reference regression of the AUC-values to the corresponding values after intravenous infusion of graded doses. The reference regression is estimated from an appropriate trial. Deviation of the determined AUC-values from the regression curve afford an estimate of the residual variance due to varying distribution volumes or similar random biological effects. For the estimation of absorption ratios after oral administration the drug is given orally to another sample of subjects and their AUC-values are calculated. The deviation of these AUC values due to the above mentioned random effects are simulated using the residual variance of the reference regression, and are subtracted from the observed AUC-values. Then, the differences in the corresponding absorbed doses are transformed by inverting the reference regression. From these doses the empirical distribution function and statistical parameters (e.g. quantiles) are determined. The method has the advantage that no restrictive assumptions are required, such as first order processes, dose linearity, homogeneity of variance or normal distribution of absorption ratios. Its applicability to substances with qualitative differences in their pharmacokinetics is demonstrated by appropriate examples.
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  • 8
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    European journal of clinical pharmacology 21 (1982), S. 343-350 
    ISSN: 1432-1041
    Keywords: orphenadrine ; single dose ; multiple doses ; bioavailability ; pharmacokinetics ; N-demethylorphenadrine ; metabolism ; dog ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma concentrations of orphenadrine were measured by a specific gaschromatographic method in 5 healthy male volunteers after a single oral dose of orphenadrine hydrochloride 100mg. The single dose pharmacokinetic profile of orphenadrine was evaluated from these data. The elimination half-life ranged from 13.2–20.1 h after the commercial tablet formulation. Plasma concentrations, determined in volunteers and patients under different conditions of repeated oral administration of the same formulation of orphenadrine hydrochloride exceeded the theoretical values, predicted from the single dose pharmacokinetics, by a factor 2 to 3. The elimination half-lives after discontinuation of treatment showed a 2 to 3-fold increase over the single dose values. This demonstrates a clear discrepancy between the multiple and single dose pharmacokinetics of orphenadrine. Experiments in dogs suggested competition for biotransformation between orphenadrine and its metabolite N-demethylorphenadrine. Product inhibition of this type could explain the observed discrepancy.
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  • 9
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    European journal of clinical pharmacology 22 (1982), S. 63-69 
    ISSN: 1432-1041
    Keywords: pivmecillinam ; avicel ; gastroscopy ; comparison of different tablets ; in vitro disintegration ; gastric irritation ; plasma mecillinam ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Three different pivmecillinam preparations, a conventional 200 mg tablet (P tablet) and two new formulations containing respectively pivmecillinam 200 mg and 400 mg plus Avicel® (microcrystalline cellulose) as a disintegrator (PA tablet), were compared in vitro and in a gastroscopic study in 8 healthy volunteers. Disintegration of the PA tablet was significantly more rapid both in vitro and in the stomach. Following disintegration, the content of the PA tablet was spread over a larger area of the gastric mucosa (1088 mm2) than was observed with the P tablets (408 mm2). Three of the 8 volunteers taking the P tablet developed hyperaemia, interstitial bleeding or erosions of the mucosa of the stomach. No such reactions were seen with the PA tablets. Serum concentrations of mecillinam following ingestion of pivmecillinam tablets were determined in three groups of subjects; fasting volunteers, both supine and ambulant, and in ambulant subjects who took the preparation with a light meal. There was a tendency for the new PA tablets to produce a higher peak serum level as well as greater bioavailability of mecillinam. Administration of the PA tablets with a meal significantly increased the peak serum level and total bioavailability of the drug. On the basis of our observations we recommend adoption of the new PA tablet, because of its quick passage through the oesophagus and its more rapid and complete disintegration in the stomach.
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  • 10
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    European journal of clinical pharmacology 22 (1982), S. 77-84 
    ISSN: 1432-1041
    Keywords: allopurinol ; oxipurinol ; benzbromarone ; hydrochlorothiazide ; pharmacokinetics ; bioavailability ; interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An high-pressure liquid chromatographic method was used to measure allopurinol and oxipurinol in plasma and urine in 6 healthy volunteers after a single intravenous or oral dose of allopurinol. The influence of coadministrated benzbromarone and hydrochlorothiazide on the pharmacokinetics of allopurinol and oxipurinol was also investigated. After intravenous injection of allopurinol 300 mg the plasma disappearance was biexponential, with a mean distribution half-life of 2.32±1.08 min $$(\bar x \pm SD)$$ and an elimination half-life of 47.8±10.6 min. The total clearance of allopurinol was 11.37±2.70 ml/min/kg, whereas its renal clearance was only 1.73±0.79 ml/min/kg. Oxipurinol disappeared monoexponentially from plasma ith a mean half-life of 12.2±2.6 h. Its renal clearance was 0.42±0.091 ml/min/kg. After oral administration of allopurinol 300 mg the peak plasma concentration of 2.1±0.6 µg/ml (1.5×10−5 M) was reached within 30 to 120 min. The peak level of oxipurinol of 5.8±1.5 µg/ml (3.8×10−5 M) was found within 2 to 5 h after intravenous and oral allopurinol. The bioavailability of oral allopurinol computed from plasma data was 90.4±8.7%. The total recovery from urine was 77% (allopurinol 8%, oxipurinol 69%) after oral and 88% after i.v. administration. It was concluded that about 10% of the oral dose was not absorbed and that 12% was eliminated by an unknown mechanism, presumably as riboside. The pharmacokinetics of allopurinol and oxipurinol were not significantly influenced by coadministration of benzbromarone or hydrochlorothiazide.
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  • 11
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    European journal of clinical pharmacology 22 (1982), S. 171-173 
    ISSN: 1432-1041
    Keywords: theophylline ; neonates ; bioavailability ; food intake ; premature infants
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 16 premature infants suffering from neonatal apnoea received orally an aqueous solution of theophylline 5 mg/kg bodyweight under fasting conditions and immediately before a milk feed. Bioavailability up to 7 h after administration was determined from the serum concentration-time course. The rate of absorption was significantly decreased if the drug was given with food; mean maximum serum concentrations were reached after 4.7 h instead of 1.6 h under fasting conditions. The area under the curve did not differ between the two patient groups which indicates that only the rate but not the amount of absorption was affected by food intake. The influence of feeding on the rate of absorption of theophylline by premature infants, which is more pronounced than in adults, can be related to particular functional factors in the gastrointestinal tract during the neonatal period.
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  • 12
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    European journal of clinical pharmacology 22 (1982), S. 535-539 
    ISSN: 1432-1041
    Keywords: noscapine ; pharmacokinetics ; absorption ; bioavailability ; intravenous application ; oral application ; ion exchange resin tablet
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Noscapine was administred to five healthy volunteers in a randomized crossover design, as an intravenous infusion of 66 mg, and as an oral 150 mg dose of either rapidly dissolving tablets or a tablet containing ion exchange resin-bound noscapine. After i.v. administration, the disposition of noscapine was bi-exponential with an elimination half-life of 2.6 h; the total plasma clearance was 22 ml/min/kg and the volume of distribution (Vdarea) was 4.7 l/kg. The absolute oral bioavailability was 30%, with a 3.6-fold interindividual variation. There was no pharmacokinetic evidence to support a prolonged action of the ion exchange resin tablet.
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  • 13
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    European journal of clinical pharmacology 22 (1982), S. 459-462 
    ISSN: 1432-1041
    Keywords: tolbutamide ; diabetes ; food intake ; blood glucose ; blood insulin ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of food on the rate and extent of absorption of tolbutamide in diabetic patients was studied by varying the time of drug administration in relation to the ingestion of a standard meal. Serum levels of tolbutamide, insulin and glucose and related bioavailability parameters were compared following the administration of a single dose of tolbutamide 0.5 g to diabetic patients 30 min prior to and immediately before a standardized meal. A placebo dosage form was also administered to determine baseline glucose and insulin response to the meal. The 700 calorie standard meal was composed of 41% carbohydrate, 18% protein, and 41% fat. Administration of the drug with the meal resulted in a 6% (statistically significant) decrease in the extent of absorption, as determined by measurement of the area under the tolbutamide serum level-time curve from zero to infinity. Serum levels of tolbutamide were also significantly higher 0.5 h after drug administration when the drug was taken with the meal. Except for these two minor effects, no other differences between the drug treatments were observed in any other parameters of tolbutamide absorption or in the postprandial glucose and insulin serum levels. Therefore, the small differences found were judged to be clinically meaningless. These findings demonstrate that administration of tolbutamide 0.5 g tablets 30 min prior to or with a standard meal results in equivalent therapeutic actions.
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  • 14
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    European journal of clinical pharmacology 23 (1982), S. 267-270 
    ISSN: 1432-1041
    Keywords: terodiline ; human volunteers ; pharmacokinetics ; serum clearance ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of terodiline HCl was studied in nine healthy volunteers given 12.5 mg i.v. and p.o. or 20 mg i.v. and 25 mg p.o. on two different occasions. The serum concentrations were measured by gas chromatography — mass spectrometry, using deuterated terodiline HCl as the internal standard. After i.v. administration the kinetics could be described by a two-compartment model with a mean distribution half life of 0.3 h and a mean elimination half life of 63 h. The serum clearance and apparent volume of distribution varied about 4-fold with mean values of 4.8 l/h and 417 l, respectively. After oral administration, the mean half life of absorption was 0.7 h and that of elimination 65 h. The absolute bioavailability varied between 64% and 105% with a mean of 92%. The long serum half life of terodiline should permit its once daily administration.
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  • 15
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    European journal of clinical pharmacology 21 (1982), S. 335-341 
    ISSN: 1432-1041
    Keywords: phenylephrine ; pharmacokinetics ; bioavailability ; first-pass metabolism ; phenolic conjugates ; m-hydroxymandelic acid ; intravenous ; oral
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 7-3H-phenylephrine was given to 15 volunteers by a short-infusionn=4) or p.o. (10 volunteers, 1 patient with porto-caval anastomosis). Analysis of serum for free3H-phenylephrine and fractionation of urinary radioactivity was performed by ion-exchange and thin-layer chromatography. As almost the same3H-activity was excreted in urine after i.v. and p.o. administration, 86% and 80% of the dose respectively, complete enteral absorption can be assumed. A considerable difference was seen in the fraction of free phenylephrine, i.v. 16% of the dose versus p.o. 2.6%, which suggested reduced bioavailability. This was confirmed by comparison of the areas under the serum curve, which showed a bioavailability factor of 0.38. The result for the patient with porto-caval anastomosis was comparable to that in the normal volunteers. The biological half-life of 2 to 3h was comparable to that of structurally related amines, as were the total clearance of 2 1/h, and the volume of distribution of 340l. Metabolism to phenolic conjugates mainly after oral ingestion, and tom-hydroxymandelic acid after i.v. injection, again demonstrated thatm-hydroxylated amines are predominantly conjugated during the “first-pass” metabolism.
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  • 16
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    European journal of clinical pharmacology 22 (1982), S. 463-467 
    ISSN: 1432-1041
    Keywords: orthostatic hypotension ; etilefrine ; dihydroergotamine ; bioavailability ; combination therapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Etilefrine undergoes considerable first-pass metabolism through conjugation in the gut wall. In six volunteers bioavailability was reduced to 35% for a fast release tablet and to 17% for a sustained release preparation. The addition fo dihydroergotamine (DHE) to the sustained release preparation surprisingly increased bioavailability to 61%. The plasma levels of the main metabolite formed during the passage through the gut wall indicated an increase in the rate of enteric absorption and therefore also in bioavailability by DHE. This might be due to the influence of DHE upon the vascular resistance of the vessels in the gut wall or a change in gastro-intestinal motility with a prolongation of drug contact time within the absorbing gut segment.
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  • 17
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    European journal of clinical pharmacology 21 (1982), S. 293-301 
    ISSN: 1432-1041
    Keywords: metipranolol ; deacetyl metipranolol ; pharmacokinetics ; bioavailability ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic parameters of deacetyl metipranolol were determined after i.v. infusion of increasing doses (6–25 mg) in 17 normal volunteers. In a second cross-over trial, deacetyl metipranolol 10 and 20 mg were infused in a further 10 subjects, and in a third trial another 20 volunteers received metipranolol 40 mg orally. Metipranolol is very rapidly and completely deacetylated in man, so all pharmacokinetic data refer to deacetyl metipranolol, which was assayed by gas chromatography-mass spectrometry. The pharmacokinetic analysis was performed using a recently developed model, using a volume of distribution which is variable with time. The following data were obtained after oral administration: (mean values); lag-time 7.3 min; tmax 50 min, invasion half-life 6.3 min; elimination half-life 3 h; urinary excretion of unchanged drug approximately 4% of the dose. The experiments with infusion of increasing doses, as well as the cross-over study with 10 and 20 mg i.v., showed dose-linearity of the kinetics. The respective mean half-lives of elimination were 2.6, 2.9 and 2.8 h. The mean total, renal and extra-renal clearances amounted to 1237 ml/min, 149 ml/min and 1068 ml/min, respectively. The distribution coefficient was 3.5 l/kg, and protein binding amounted to 70% within the range of therapeutic concentrations. Absolute bioavailability was found to be approximately 50% by several different evaluation procedures. Thus, the pharmacokinetic profile of metipranolol shares features of both the lipophilic and the hydrophilic groups of β-blocking agents.
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  • 18
    ISSN: 1432-1041
    Keywords: indomethacin ; bioavailability ; plasma concentrations ; dissolution ; enteric-coated ; pellets ; controlled release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Two multiple-units controlled-release indomethacin capsule formulations containing enteric-coated pellets were bioequivalent to a standard capsule formulation (taken as the reference) in respect of extent of bioavailability in a crossover study with normal human subjects. However, drug absorption from the enteric-coated pellet formulations was slower, when compared to that from the standard reference capsule. The standard reference capsule released 85% of its drug content in vitro during 10 min at pH 6.5 and 98% during 1 h at pH 7.5. One enteric-coated pellet capsule formulation (I) released 77% during 1 h at pH 6.5 and the other (II) released 10% during 1 h at pH 6.5. Release of drug from each capsule of enteric-coated pellets was complete during 1 h at pH 7.5. Although differences in areas under the plasma indomethacin concentration-time curves were not significantly different, the peak plasma levels and the times of their occurrence indicated that the absorption rates of indomethacin decreased in the order, reference formulation 〉 pellet formulation I 〉 pellet formulation II, which was the same rank order as that of their dissolution rates in vitro. The data indicated that multiple units controlled-release formulations represent a reliable and reproducible source of indomethacin, which by avoiding extremes of local or systemic drug concentrations also should be better tolerated by individuals susceptible to unwanted gastrointestinal and centrally-mediated side-effects.
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  • 19
    ISSN: 1432-1041
    Keywords: indapamide ; bioavailability ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Two formulations of indapamide tablets (2.5 mg) were given as a 5.0 mg dose and the subsequent blood levels were compared to those obtained after administration of a 5.0 mg solution. The study was conducted as a randomized three-way crossover design using healthy male volunteers. The drug was well tolerated by all the subjects involved. The area under the blood concentration versus time curve, extrapolated to infinity was essentially the same for all three formulations (4.2, 4.7, and 4.4 µg-h/ml). Statistical comparison of the blood levels from the two tablets showed that one tablet had a significantly greater maximum blood concentration (263 vs 231 ng/ml) and a significantly shorter time of maximum blood concentration (2.3 vs 3.5 h). Cmax (333 ng/ml) and tmax (0.7 h) values for the solution were significantly higher than either tablet. The average half-life (β-phase) for all three formulations was 15 h, while the average systemic clearance was 20 ml/min. Indapamide has a low clearance rate and there was no evidence that the drug undergoes a first-pass effect.
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  • 20
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    European journal of clinical pharmacology 22 (1982), S. 359-365 
    ISSN: 1432-1041
    Keywords: chlorpheniramine ; pharmacokinetics ; oral absorption ; half-life ; bioavailability ; volume of distribution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma and urinary levels of chlorpheniramine (CPM) and its 2 demethylated metabolites were measured by HPLC after i.v. and oral dosing. In 5 mg (maleate) i.v. bolus studies in 2 subjects, plasma CPM levels were fitted to triexponential equations with terminal half-lives (t 1/2) of 23 and 22 h and area of 3.6 and 3.21/kg, respectively. Intravenous data predicted hepatic blood extraction ratios for the 2 subjects to be 0.06 and 0.07, respectively. Absolute bioavailability from oral solution (10 mg) was 59 and 34%, and from tablets (8 mg) 44 and 25%, respectively, indicating extensive gut first-pass metabolism. Mean t 1/2 from 7 oral fasting studies in 5 subjects was 28 h (19–43 h). Mean absorption lag time was 0.7 h (0.4–1.3 h), and mean peak time was 2.8 h (2–4 h). In 2 subjects, 6 mg solutions were given every 12 h for 9 doses; good correlation between single and multiple dose kinetics was found. Significant accumulation was demonstrated in simulation studies with frequent daily dosing. Estimated accumulation ratios vary from 4.1 to 9.4 (mean 6.5). The t 1/2 from urinary data (collected for 12 days) was consistent with plasma data. The above results suggest the need to reexamine the current practice of frequent daily dosing and the use of sustained or controlled release dosage forms of this drug. The possible cause of reduced plasma clearance of CPM in renal patients is discussed.
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  • 21
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    European journal of clinical pharmacology 23 (1982), S. 87-92 
    ISSN: 1432-1041
    Keywords: phenobarbital ; epilepsy ; kinetics ; bioavailability ; epileptic patients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of phenobarbital (PB) were evaluated in six normal subjects and six epileptic patients treated with phenytoin or carbamazepine. Each normal subject received three single doses of PB: PB-sodium 130 mg i.v. (IV), PB sodium 130 mg i.m. (IM), and PB acid 100 mg orally (PO), in random order at least one month apart. After IV PB distributive half-lives varied from 0.13 to 0.70 h, disposition half-lives were 75 to 126 h, steady state volume of distribution (Vss) was 0.54±0.03 l/kg, and clearance (CL) was 3.8±0.77 ml/h/kg. Absolute bioavailability of IM PB was 101±13%, of PO PB (corrected for dose) 100±11%. Peak serum PB concentrations were achieved from 2 to 8 h after IM administration, and from 0.5 to 4 h after PO administration. Epileptic patients exhibited similar PB kinetics: disposition half-lives were 77 to 128 h, Vss 0.61±0.05 l/kg, and Cl 3.9±0.76 ml/h/kg. Phenobarbital appears to represent an exception among antiepileptic drugs, in that pharmacokinetic data obtained in normals can reasonably be extrapolated to the epileptic population.
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  • 22
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    European journal of clinical pharmacology 23 (1982), S. 271-273 
    ISSN: 1432-1041
    Keywords: chloroquine ; bioavailability ; gastrointestinal absorption ; food effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of chloroquine in 7 healthy adult male volunteers was assessed with and without a standard breakfast. Chloroquine (600 mg base) was administered orally and timed blood samples were obtained for determination of plasma concentrations. The results suggest that the AUC and peak plasma levels were significantly higher when chloroquine was administered together with food, although the rate of absorption was not different. It appears, therefore, that food facilitates chloroquine absorption and the extent of absorption is significantly modified. Hence administration of chloroquine together with food appears to be an advisable clinical practice.
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  • 23
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    Journal of chemical ecology 8 (1982), S. 31-39 
    ISSN: 1573-1561
    Keywords: Malacosoma americanum ; eastern tent caterpillar ; Lepidoptera ; Lasiocampidae ; trail pheromone ; pheromone secretory site ; silk trail
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract A new site of secretion of a chemical trail marker was found on the sternum at the tip of the last abdominal segment of the larva of the eastern tent caterpillarMalacosoma americanum. Larvae marked from this site by drawing their sterna along the substrate when they extended existing trails in search of food and again when they established recruitment trails to food-finds. Differences in the quantity or quality of the marker deposited by exploring and recruiting caterpillars may account for the greater activity of the recruitment trails.
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  • 24
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    Journal of chemical ecology 8 (1982), S. 267-273 
    ISSN: 1573-1561
    Keywords: Fall armyworm ; Spodoptera frugiperda ; Lepidoptera ; Noctuidae ; (Z)-9-dodecen-1-ol acetate ; (Z)-9-tetradecen-1-ol acetate ; pheromone ; mating behavior
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Two components of the fall armyworm,Spodoptera frugiperda (J.E. Smith), sex pheromone, (Z)-9-dodecen-1-ol acetate (DDA) and (Z)-9-tetradecen-1-ol (TDA), were tested alone and in combination to determine their effects on male sexual response and inhibition of mating in the laboratory. The threshold response for FAW males was lower for TDA than for DDA, and males responded to TDA over a wider range of dosages. Although TDA is not attractive to FAW males in the field, this compound was highly effective in reducing mating under laboratory conditions.
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  • 25
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Noctuidae ; Pseudaletia separata ; male scent ; repellent pheromone ; repellent allomone ; nonspecificity ; sexual selection
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Air movement around a malePseudaletia separata Walker, observed using the smoke of an incense stick during wing-fanning, showed that the air moves away from the female and backwards. Moths moved or flew away immediately when vaporized benzaldehyde was blown over their antennae in a screen cage set in a greenhouse. This repellency lacked species, sex, or individual specificity. Male scent acts as an inhibitor to conspecific males and, at the same time, to other moths if they approach the male in courtship. Inhibition of ovipositional and larval locomotory behavior by benzaldehyde was also demonstrated.
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  • 26
    ISSN: 1573-1561
    Keywords: Agrotis segetum ; turnip moth ; Lepidoptera ; Noctuidae ; sex pheromone ; straight-chain acetates ; single-cell recordings ; electroantennography ; behavior ; gas chromatography-mass spectrometry ; entrainment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Analysis of female abdominal tips ofAgrotis segetum by means of GC-MS showed the presence of 13 aliphatic acetates and alcohols. (Z)-7-Dodecenyl acetate was found to be the main component in the extracts at amounts of about 1 ng/female. (Z)-9-Tetradecenyl acetate and (Z)-7-dodecenol were present to the extent of 49 and 19%, respectively, of the main component. Minor components could be identified as decyl acetate, (Z)-5-decenyl acetate, dodecyl acetate, (Z)-9-dodecenyl acetate, tetradecyl acetate, a tetradecenyl acetate, hexadecyl acetate, a hexadecenyl acetate, (Z)-5-decenol, and (Z)-9-tetradecenol. The presence and biological activity of decyl acetate, (Z)-5-decenyl acetate, and (Z)-7-dodecenyl acetate in the extracts could be detected by GC-EAD. Tested by EAG (Z)-5-decenyl acetate evoked the highest response among pheromone candidates, followed by (E)-5-decenyl acetate and (Z)-7-dodecenyl acetate. Single-cell recordings from 100 male antennal sensilla trichodea revealed receptorcells highly sensitive to (Z)-5-decenyl, (Z)-7-dodecenyl, (Z)-8-dodecenyl, and (Z)-9-tetradecenyl acetate as well as (Z)-5-decenol. The (Z)-5-decenyl, (Z)-7-dodecenyl, and (Z)-9-tetradecenyl acetate receptors were activated significantly also by female extracts. When tested in a tube olfactometer, a blend of decyl, (Z)-5-decenyl, (Z)-7-dodecenyl, and (Z)-9-tetradecenyl acetate evoked the same male response as did female glands. Tested in the field, this blend was more attractive than virgin females. Other authors previously reported many of the compounds identified in the present study. However, both quantitative and qualitative discrepancies exist among the various investigations, possibly due to the existence of geographical races.
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  • 27
    ISSN: 1573-1561
    Keywords: Smaller tea tortrix moth ; Adoxophyes sp. ; Lepidoptera ; Tortricidae ; asymmetric induction ; 10-methyl-1-dodecanol acetate ; ester ; chirality
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract A new route to (±)-10-methyl-1-dodecanol acetate, a minor component of the smaller tea tortrix moth (Adoxophyes sp.), is described. An optional sequence that permits the generation of the chiral center with enantiomeric excesses (ee's) as high as 74% (R) or 80% (S) employing the available (S)-(−)-prolinol as a chiral auxiliary may be included. High-performance liquid chromatography of diastereomeric intermediates allows preparation of products with greater ee's.
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  • 28
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    Journal of chemical ecology 8 (1982), S. 233-239 
    ISSN: 1573-1561
    Keywords: Choristoneura fumiferana ; Lepidoptera ; Tortricidae ; carbohydrates ; sucrose ; feeding preference ; behavior
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Spruce budworm larvae reared on an artificial diet were tested for preference of twelve carbohydrates over a water control. A strong preference for sucrose was seen, followed by fructose, inositol, and glucose. Male and female larvae do not differ in their responses to sucrose. The behavioral threshold for sucrose is at 10−4 to 10−3 M, with a peak response in the range of 0.01 to 0.05 M sucrose.
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  • 29
    ISSN: 1573-1561
    Keywords: Western avocado leafroller ; Amorbia cuneana ; sex pheromone ; Tortricidae ; (E,E)- and (E,Z)-10,12-tetradecadien-1-ol acetate ; Lepidoptera
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The major volatile components in the extract of the female sex pheromone gland ofAmorbia cuneana consisted of (E,E)- and (E,Z)-10,12-tetradecadien-1-ol acetates. The identification was based on electroantennogram bioassay of gas Chromatographic effluent from sex pheromone gland extract, relative retention times on polar and nonpolar gas chromatographic columns, chemical degradation (ozonolysis, saponification), mass spectrometry, chemical synthetic methods, and field tests. Based on mass spectrometry and retention times by capillary gas chromatography, traces of (E)-10-tetradecen-1-ol acetate and 1-tetradecanol acetate were also present in the extract. Traps baited with a combination of synthetic (E,E)- and (E,Z)-10,12-tetradecadien-1-ol acetates caught more males than did traps baited with females.
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  • 30
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    Journal of chemical ecology 8 (1982), S. 1251-1262 
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Tortricidae ; Adoxophyes orana ; pheromone traps ; attraction ; interaction ; trap spacing ; wind ; monitoring ; mass trapping
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract In a spindle-tree apple orchard, sex pheromone traps for the summerfruit tortrix moth were distributed at different spacings. From the captures, information was derived about influence of prevailing wind direction and of trap spacing on interactions between traps. Prevailing wind direction in the experimental area had no appreciable influence on trap interaction, perhaps because of eddying within the planting. The relationship between density and capture of traps was first considered theoretically and interaction by overlap of active-space areas was distinguished from that by overlap of mere capturing areas, which depend also on distance of dispersal. The actual results were in accordance with these considerations and indicated that the diameter of the active-space areas averaged 15 m. The variation in the captures of the wider-spaced traps was too large to be conclusive about the average width of the capturing areas, but the diameter of these seemed to be more than about 45 m. These data have been related to adequate trap distances for monitoring and mass trapping.
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  • 31
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    Journal of chemical ecology 8 (1982), S. 1429-1436 
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Noctuidae ; Heliothis zea ; bioassay ; host plant resistance mechanisms ; allelochemicals
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Maysin, a flavone glycoside from corn silks, inhibits ingestion, and thus growth, ofHeliothis zea (Boddie) larvae. Pinitol from soybeans inhibitedH. zea growth by the same mechanism. Despite the widely held assumption that tannins inhibit growth by inhibiting assimilation, cotton condensed tannin inhibitedH. zea growth by reducing ingestion; no evidence was found for a reduction in assimilation. Neonate larvae are shown to be much more sensitive to allelochemics than larvae that have fed on control diet before being transferred to diet containing plant allelochemics.
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  • 32
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    Hydrobiologia 91-92 (1982), S. 111-119 
    ISSN: 1573-5117
    Keywords: phosphorus ; bioavailability ; point source ; diffuse source ; Great Lakes ; bioassay ; eutrophication
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Control of phytoplankton production in the Great Lakes can be achieved most efficiently by limiting inputs of biologically available P. We report the results of studies performed to characterize the chemical forms and availability of particulate P in wastewater and tributaries which enter the lower Lakes, the eroding bluffs which border Lake Erie, and bottom samples from the near-shore of western Lake Erie. Rates of release of available P were estimated from a simple first-order model of the process, as observed during algal bioassays. Available P in wastewater samples, as a fraction of total particulate P, was affected minimally by wastewater treatment, including chemical precipitation and filtration; it correlated well with levels of total particulate P. Available particulate P levels in fluvial suspended sediments showed regional uniformity, but appeared to be strongly dependent on levels of both NaOH-P and CDB-P. Rates of release of available P decreased during wastewater treatment to values which were similar in magnitude to those observed for fluvial sediments. Release rates, however, were not related to any of the particulate P fractions which were measured. Analysis of the bluff and bottom samples indicated that P availability in the former was negligible, but the latter contained levels which approached those of wastewater particulates, though available P was released from the bottom sediments at relatively low rates.
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  • 33
    ISSN: 1573-5117
    Keywords: mercury ; methyl mercury ; speciation and sediment-water partitioning ; rivers and lakes ; dissolved and suspended matter ; seasonal and site-specific variations ; biogeochemistry ; pollution ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Seasonal and regional variations in the speciation, sediment-water partitioning, and dynamics of mercury (Hg) were studied at selected sites along the Hg-polluted Wabigoon River, and at unpolluted headwater and tributary sites, during April–September, 1979. ‘Dissolved’ and ‘particulate’ forms of Hg in the water were separated by continuous-flow centrifugation in the field. The Hg and other pollutants such as wood chips and salt had been discharged from a chlor-alkali plant and paper mill at Dryden, Ontario. Concentrations and loadings of particulate methyl mercury (CH3Hg+) and total particulate Hg (and loadings of total ‘dissolved’ Hg) were greatest during the spring flood (April-May) owing to accelerated resuspension and transport of sediments. Concentrations of ‘dissolved’ CH3Hg+, however, were highest in the summer (July–September), probably reflecting stimulation of microbial methylating activity by elevated temperatures, together with factors such as reduced levels of metal-scavenging particulates and minimal dilution by runoff. Total dissolved Hg concentrations were relatively high in September at polluted sites only, possibly because of desorption from sediments due to elevated concentrations of Cl− ions. Loadings of dissolved CH3Hg+ tended to be high in the summer but were generally depressed (suggesting sorption by suspended particles) during the major spring-flood episode in May. During July–August dissolved CH3Hg+ was a function of total dissolved Hg, suggesting rapid biomethylation of desorbed inorganic Hg; but in general dissolved and suspended CH3Hg+ levels depended on environmental variables and were unrelated to total Hg concentrations. In the summer only, total dissolved Hg was a function of dissolved Cl−. Hg species in particulates were associated with sulfides, hydrated Fe and Mn oxides, organic matter (notably high molecular weight humic and humic-Fe components), and selenium (Se); but CH3Hg+ and total Hg differed in their specific preferences for binding agents, implying that binding sites discriminate between CH3Hg+ and Hg2+ ions. CH3Hg+ was associated with sulfide and (in the spring only) with Fe oxides, whereas total Hg was associated with organic matter and Se and with DTPA- and NaOH-extractable Fe in the spring but with Mn oxide and NaOH-extractable organics in the summer. Sulfides were most abundant in May, indicating that they were eroded from bottom sediments, but Fe and Mn oxides were most abundant in the summer, probably owing to activities of filamentous iron bacteria and other micro-organisms. Particulate Hg was 98–100% nonextractable by mild solvents such as Ca acetate, CaCl2, dilute acetic acid, and (at polluted sites only) DTPA solutions, suggesting that the particulate Hg mobilized in the spring may not be readily available to organisms; association with Se and high molecular weight humic matter also supports this hypothesis. Hg probably becomes more bio-available in the summer, as suggested by the upsurge in dissolved CH3Hg+ and total dissolved Hg levels, and by increases in the solubility of particulate Hg in acetic acid, DTPA, H2O2, and NaOH solutions, as well as an increase in the relative importance of lower molecular weight fractions of NaOH-extractable Hg (in September). Regional variations in Hg speciation and partitioning reflected a gradient in sediment composition from wood chips near Dryden to silt-clay mud further downstream. Hg in silt-clay mud relatively far (〉 35 km) downstream from the source of pollution or in unpolluted areas appeared to be more readily solubilized by Cl− ions or chelators such as DTPA, more readily methylated (as indicated by downstream increases in dissolved CH3Hg+ levels and CH3Hg+/total Hg ratios), and was to a greater degree organically bound (H2O2-extractable), and thus was probably more bio-available, than Hg in wood-chip deposits. Possible explanations include weaker binding of Hg by the mud, the more finely divided state of the mud, and improved microbial growth at lower concentrations of toxic pollutants. Owing to enrichment in sulfides and Fe oxides, resuspended wood-chip sediments were especially efficient scavengers of CH3Hg+. The results indicate that in any pollution abatement plan aimed at lowering the Hg levels in the biota of lakes fed by the Wabigoon River, immobilization, removal, or detoxification of dissolved as well as particulate forms of Hg in the river would probably have to be considered. Possibly, Hg species could be ‘scrubbed’ from the river water by increasing the suspended load and by sedimentation and treatment with Hg-binding agents in special receiving basins.
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  • 34
    ISSN: 1573-5117
    Keywords: mercury ; methyl mercury ; speciation and sediment-water partitioning ; rivers and lakes ; dissolved and suspended matter ; seasonal and site-specific variations ; biogeochemistry ; pollution ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Seasonal and regional variations in the speciation, sediment-water partitioning, and dynamics of mercury (Hg) were studied at selected sites along the Hg-polluted Wabigoon River, and at unpolluted headwater and tributary sites, during April–September, 1979. ‘Dissolved’ and ‘particulate’ forms of Hg in the water were separated by continuous-flow centrifugation in the field. The Hg and other pollutants such as wood chips and salt had been discharged from a chlor-alkali plant and paper mill at Dryden, Ontario. Concentrations and loadings of particulate methyl mercury (CH3Hg+) and total particulate Hg (and loadings of total ‘dissolved’ Hg) were greatest during the spring flood (April-May) owing to accelerated resuspension and transport of sediments. Concentrations of ‘dissolved’ CH3Hg+, however, were highest in the summer (July–September), probably reflecting stimulation of microbial methylating activity by elevated temperatures, together with factors such as reduced levels of metal-scavenging particulates and minimal dilution by runoff. Total dissolved Hg concentrations were relatively high in September at polluted sites only, possibly because of desorption from sediments due to elevated concentrations of Cl− ions. Loadings of dissolved CH3Hg+ tended to be high in the summer but were generally depressed (suggesting sorption by suspended particles) during the major spring-flood episode in May. During July–August dissolved CH3Hg+ was a function of total dissolved Hg, suggesting rapid biomethylation of desorbed inorganic Hg; but in general dissolved and suspended CH3Hg+ levels depended on environmental variables and were unrelated to total Hg concentrations. In the summer only, total dissolved Hg was a function of dissolved Cl−. Hg species in particulates were associated with sulfides, hydrated Fe and Mn oxides, organic matter (notably high molecular weight humic and humic-Fe components), and selenium (Se); but CH3Hg+ and total Hg differed in their specific preferences for binding agents, implying that binding sites discriminate between CH3Hg+ and Hg2+ ions. CH3Hg+ was associated with sulfide and (in the spring only) with Fe oxides, whereas total Hg was associated with organic matter and Se and with DTPA- and NaOH-extractable Fe in the spring but with Mn oxide and NaOH-extractable organics in the summer. Sulfides were most abundant in May, indicating that they were eroded from bottom sediments, but Fe and Mn oxides were most abundant in the summer, probably owing to activities of filamentous iron bacteria and other micro-organisms. Particulate Hg was 98–100% nonextractable by mild solvents such as Ca acetate, CaCl2, dilute acetic acid, and (at polluted sites only) DTPA solutions, suggesting that the particulate Hg mobilized in the spring may not be readily available to organisms; association with Se and high molecular weight humic matter also supports this hypothesis. Hg probably becomes more bio-available in the summer, as suggested by the upsurge in dissolved CH3Hg+ and total dissolved Hg levels, and by increases in the solubility of particulate Hg in acetic acid, DTPA, H2O2, and NaOH solutions, as well as an increase in the relative importance of lower molecular weight fractions of NaOH-extractable Hg (in September). Regional variations in Hg speciation and partitioning reflected a gradient in sediment composition from wood chips near Dryden to silt-clay mud further downstream. Hg in silt-clay mud relatively far (〉 35 km) downstream from the source of pollution or in unpolluted areas appeared to be more readily solubilized by Cl− ions or chelators such as DTPA, more readily methylated (as indicated by downstream increases in dissolved CH3Hg+ levels and CH3Hg+/total Hg ratios), and was to a greater degree organically bound (H2O2-extractable), and thus was probably more bio-available, than Hg in wood-chip deposits. Possible explanations include weaker binding of Hg by the mud, the more finely divided state of the mud, and improved microbial growth at lower concentrations of toxic pollutants. Owing to enrichment in sulfides and Fe oxides, resuspended wood-chip sediments were especially efficient scavengers of CH3Hg+. The results indicate that in any pollution abatement plan aimed at lowering the Hg levels in the biota of lakes fed by the Wabigoon River, immobilization, removal, or detoxification of dissolved as well as particulate forms of Hg in the river would probably have to be considered. Possibly, Hg species could be ‘scrubbed’ from the river water by increasing the suspended load and by sedimentation and treatment with Hg-binding agents in special receiving basins.
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  • 35
    ISSN: 1573-5117
    Keywords: mercury ; methyl mercury ; speciation and sediment-water partitioning ; rivers and lakes ; dissolved and suspended matter ; seasonal and site-specific variations ; biogeochemistry ; pollution ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Seasonal and regional variations in the speciation, sediment-water partitioning, and dynamics of mercury (Hg) were studied at selected sites along the Hg-polluted Wabigoon River, and at unpolluted headwater and tributary sites, during April–September, 1979. ‘Dissolved’ and ‘particulate’ forms of Hg in the water were separated by continuous-flow centrifugation in the field. The Hg and other pollutants such as wood chips and salt had been discharged from a chlor-alkali plant and paper mill at Dryden, Ontario. Concentrations and loadings of particulate methyl mercury (CH3Hg+) and total particulate Hg (and loadings of total ‘dissolved’ Hg) were greatest during the spring flood (April-May) owing to accelerated resuspension and transport of sediments. Concentrations of ‘dissolved’ CH3Hg+, however, were highest in the summer (July–September), probably reflecting stimulation of microbial methylating activity by elevated temperatures, together with factors such as reduced levels of metal-scavenging particulates and minimal dilution by runoff. Total dissolved Hg concentrations were relatively high in September at polluted sites only, possibly because of desorption from sediments due to elevated concentrations of Cl− ions. Loadings of dissolved CH3Hg+ tended to be high in the summer but were generally depressed (suggesting sorption by suspended particles) during the major spring-flood episode in May. During July–August dissolved CH3Hg+ was a function of total dissolved Hg, suggesting rapid biomethylation of desorbed inorganic Hg; but in general dissolved and suspended CH3Hg+ levels depended on environmental variables and were unrelated to total Hg concentrations. In the summer only, total dissolved Hg was a function of dissolved Cl−. Hg species in particulates were associated with sulfides, hydrated Fe and Mn oxides, organic matter (notably high molecular weight humic and humic-Fe components), and selenium (Se); but CH3Hg+ and total Hg differed in their specific preferences for binding agents, implying that binding sites discriminate between CH3Hg+ and Hg2+ ions. CH3Hg+ was associated with sulfide and (in the spring only) with Fe oxides, whereas total Hg was associated with organic matter and Se and with DTPA- and NaOH-extractable Fe in the spring but with Mn oxide and NaOH-extractable organics in the summer. Sulfides were most abundant in May, indicating that they were eroded from bottom sediments, but Fe and Mn oxides were most abundant in the summer, probably owing to activities of filamentous iron bacteria and other micro-organisms. Particulate Hg was 98–100% nonextractable by mild solvents such as Ca acetate, CaCl2, dilute acetic acid, and (at polluted sites only) DTPA solutions, suggesting that the particulate Hg mobilized in the spring may not be readily available to organisms; association with Se and high molecular weight humic matter also supports this hypothesis. Hg probably becomes more bio-available in the summer, as suggested by the upsurge in dissolved CH3Hg+ and total dissolved Hg levels, and by increases in the solubility of particulate Hg in acetic acid, DTPA, H2O2, and NaOH solutions, as well as an increase in the relative importance of lower molecular weight fractions of NaOH-extractable Hg (in September). Regional variations in Hg speciation and partitioning reflected a gradient in sediment composition from wood chips near Dryden to silt-clay mud further downstream. Hg in silt-clay mud relatively far (〉 35 km) downstream from the source of pollution or in unpolluted areas appeared to be more readily solubilized by Cl− ions or chelators such as DTPA, more readily methylated (as indicated by downstream increases in dissolved CH3Hg+ levels and CH3Hg+/total Hg ratios), and was to a greater degree organically bound (H2O2-extractable), and thus was probably more bio-available, than Hg in wood-chip deposits. Possible explanations include weaker binding of Hg by the mud, the more finely divided state of the mud, and improved microbial growth at lower concentrations of toxic pollutants. Owing to enrichment in sulfides and Fe oxides, resuspended wood-chip sediments were especially efficient scavengers of CH3Hg+. The results indicate that in any pollution abatement plan aimed at lowering the Hg levels in the biota of lakes fed by the Wabigoon River, immobilization, removal, or detoxification of dissolved as well as particulate forms of Hg in the river would probably have to be considered. Possibly, Hg species could be ‘scrubbed’ from the river water by increasing the suspended load and by sedimentation and treatment with Hg-binding agents in special receiving basins.
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  • 36
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    Hydrobiologia 91-92 (1982), S. 111-119 
    ISSN: 1573-5117
    Keywords: phosphorus ; bioavailability ; point source ; diffuse source ; Great Lakes ; bioassay ; eutrophication
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Control of phytoplankton production in the Great Lakes can be achieved most efficiently by limiting inputs of biologically available P. We report the results of studies performed to characterize the chemical forms and availability of particulate P in wastewater and tributaries which enter the lower Lakes, the eroding bluffs which border Lake Erie, and bottom samples from the near-shore of western Lake Erie. Rates of release of available P were estimated from a simple first-order model of the process, as observed during algal bioassays. Available P in wastewater samples, as a fraction of total particulate P, was affected minimally by wastewater treatment, including chemical precipitation and filtration; it correlated well with levels of total particulate P. Available particulate P levels in fluvial suspended sediments showed regional uniformity, but appeared to be strongly dependent on levels of both NaOH-P and CDB-P. Rates of release of available P decreased during wastewater treatment to values which were similar in magnitude to those observed for fluvial sediments. Release rates, however, were not related to any of the particulate P fractions which were measured. Analysis of the bluff and bottom samples indicated that P availability in the former was negligible, but the latter contained levels which approached those of wastewater particulates, though available P was released from the bottom sediments at relatively low rates.
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  • 37
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    Journal of chemical ecology 8 (1982), S. 351-362 
    ISSN: 1573-1561
    Keywords: Choristoneura occidentalis ; western spruce budworm ; Lepidoptera ; Tortricidae ; pheromone chemistry ; Choristoneura fumiferana ; capillary GC-MS ; (E/Z)-11-tetradecenal
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract SCOT capillary Chromatographic and SCOT capillary chromatographic-mass spectrometic analyses of gland washes and effluvia of virgin femaleChoristoneura occidentalis Free, have been conducted with both a diapausing and nondiapausing strain of this insect. The following compounds were identified in gland washes and effluvia in both strains:E andZ11–14∶Ald,E andZ11–14∶Ac,E andZ11–14∶OH and 14∶Ald, 14∶Ac, and 14∶OH. The average aldehyde: acetate: alcohol ratio found by analysis of single glands by virgin females (nondiapausing strain) was 1∶7∶0.73. Analysis of virgin female effluvia gave this ratio as 10∶3∶8 (diapausing strain: %Z=8, 11, 15, respectively) and 10∶3∶6 (nondiapausing strain: %Z=8, 11, 12, respectively). The saturated components were generally 1–2% of theE isomer in each case. Comparisons of EAG responses of bothC. occidentalis andC. fumiferana toE11–14∶Ald,E11–14∶Ac andE11–14∶OH were made. Correlations with both laboratory and field data previously published were also made betweenC. fumiferana andC. occidentalis.
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  • 38
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    Journal of chemical ecology 8 (1982), S. 493-506 
    ISSN: 1573-1561
    Keywords: Choristoneurafumiferana (Clem.) ; Lepidoptera ; Tortricidae ; sex pheromone ; mating disruption ; sex attraction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Male spruce budworm [Chorisloneura fumiferana (Clem.)] moths were held for 3 hr in a wind tunnel and subjected to various concentrations of background synthetic pheromone. They were then exposed to calling females and their response was recorded. The background pheromone was presented either as discrete turbulent plumes or as a uniform permeation throughout the tunnel. The numbers of males wing-fanning and flying in response to the calling females decreased as the concentration of background pheromone increased. Of the males which flew, a higher proportion progressed upwind in the discrete plumes than in the uniform permeation, an indication that structure in the pheromone cloud is necessary for upwind progression. In both discrete plumes and uniform permeation fewer males were able to locate the females (i.e., disruption was greater) as the concentration of synthetic pheromone increased, but for the same total release rates, disruption was greater when the synthetic pheromone was released in discrete plumes rather than in a uniform permeation. This implies that disruption which involves luring males to sources of synthetic pheromone is more effective than masking female plumes by uniform permeation and suggests that it is more efficient to release pheromone from a few potent sources than from numerous low-potency sources.
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  • 39
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    Journal of chemical ecology 8 (1982), S. 731-754 
    ISSN: 1573-1561
    Keywords: Alkenylcompounds ; pheromones ; chemotaxonomy ; decenyl dodecenyl ; tetradecenyl ; hexadecenyl ; trapping ; Lepidoptera ; Noctuidae
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    Notes: Abstract Sex attractants known for 145 species of noctuid moths have many common features both as to chemical constituents and to their relationships in blends. The great majority of constituents are straight-chain (Z)-alkenols, -alkenals, or -alkenyl acetates of even carbon number (10 through 16). The unsaturation is nonterminal in odd-numbered positions (5 through 11). In effective lures, these components are blended in specific ratios and the components in a sex pheromone or sex attractant blend are structurally related by “one-change” steps. This means that any blend component differs from one or more other components by a single structural alteration, such as a change in double bond position, or a change in carbon chain length, or a change in the oxygen function. For the few multicomponent systems known in detail, the central place in the “one-change” framework is occupied by the predominant blend component. Different patterns of occurrence of lure components occur in the subfamilies Acronictinae, Noctuinae, Hadeninae, Cuculliinae, Amphipyrinae, Heliothidinae, Plusiinae, Acontiinae, and Pantheinae, and some subfamilies are as yet without known lures. Some guiding principles for elucidation of blend compositions for unstudied species are presented; these guidelines can also be used in improvement of some synthetic blends of unsatisfactory quality.
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  • 40
    ISSN: 1573-1561
    Keywords: Monarch butterfly ; Asclepias spp. ; monooxygenase ; induction ; cardenolide ; aldrin epoxidation ; p-chloro-N-methylanilme demethylation ; Lepidoptera ; Danaidae
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Monarch butterfly larvae were examined for NADPH-dependent monooxygenase activities. Midgut and fat body homogenates catalyzed aldrin epoxidation andp-chloro-N-methylanilineN-demethylation at consistently low rates compared to many other lepidopteran larvae. Homogenates from larvae collected from four different milkweeds (Asclepias spp.) with quite different cardenolide contents had similar levels of activity. There were no detectable variations in activity due to season or year of collection.
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  • 41
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    Journal of chemical ecology 8 (1982), S. 837-842 
    ISSN: 1573-1561
    Keywords: 2-Tridecanone ; structure-activity relationships ; Lycopersicon hirsutum f.glabratum C.M. Mull ; Heliothis zea (Boddie) ; Lepidoptera ; Noctuidae ; resistance
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Toxicity bioassays of the naturally occurring insecticide 2-tridecanone and a group of structural analogs against the tomato fruitworm (Heliothis zea) reveal a significant influence of chain length on toxicity of methyl ketones. This effect may be due to the differential ability of these compounds to penetrate lipid barriers and reach the active site, since a close relationship is seen between toxicity and lipophilicity. Congeners of chain lenths 15 and over are less active than predicted by this relationship, possibly due to steric effects.
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  • 42
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    Journal of chemical ecology 8 (1982), S. 1125-1132 
    ISSN: 1573-1561
    Keywords: Peachtree borer ; Synanthedon exitiosa (Say) ; Lepidoptera ; Sessiidae ; oviposition stimulant ; peach ; Prunus persica
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Peachtree borer (PTB) cocoons, peach tree bark, and a mixture of frass and gum obtained arount PTB wounds were extracted with organic solvents of increasing polarity. Female PTB moths,Synanthedon exitiosa (Say), laid the greatest number of eggs on filter paper substrates treated with acetone extracts of PTB cocoons, ethyl acetate extracts of peach tree bark and acetone extracts of frass and gum mixtures. The extracts of cocoons or frass and gum mixture were separated by liquid chromatography and thin layer chromatography.
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  • 43
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    Journal of chemical ecology 8 (1982), S. 1183-1191 
    ISSN: 1573-1561
    Keywords: Kairomone ; contact chemicals ; arrestant ; host seeking ; Eucelatoria bryani ; Diptera ; Tachinidae ; Heliothis ; Lepidoptera ; Noctuidae ; parasitoid
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Factors acting at contact or close range affected the behavior associated with host seeking of females, but not of males, of the tachinid,Eucelatoria bryani Sabrosky. Females were arrested by components of larvae ofHeliothis virescens (F.) and by a dichloromethane extract of okra leaves. A hexane extract ofH. virescens frass and a chloroform-methanol extract ofH. virescens larvae were both active. In addition to chemicals, shape and size were involved because females were arrested by small inert objects the size ofH. virescens larvae and frass.
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  • 44
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    Journal of chemical ecology 8 (1982), S. 1455-1462 
    ISSN: 1573-1561
    Keywords: Efficacy ; electroantennogram ; looplure ; response threshold ; sex attractant ; trapping ; Trichoplusia ni ; Pseudoplusia includens ; Rachiplusia ou ; pheromone ; Lepidoptera ; Noctuidae
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Source concentration differences of (Z)-7-dodecen-1-ol acetate, or looplure, were evaluated for field trapping efficiency and electrophysiological responses with malePseudoplusia includens (Walker),Trichoplusia ni (Hubner) andRachiplusia ou (Guenné) (Lepidoptera: Noctuidae). Sticky traps baited with 1000 μg of the lure captured a significantly greater (P 〈 0.05) number of maleP. includens andT. ni than any other concentration;R. ou males were caught at a greater rate in traps baited with 100 μg of looplure, significantly more (P 〈 0.05) than with 1000 μg. Electroantennogram (EAG) studies demonstrated that antennae of maleP. includens have a lower response threshold to looplure than eitherT. ni orR. ou antennae, the latter demonstrating the highest significant threshold of response. No differences in the stimulus-response functions of the three species were detected.
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  • 45
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    Journal of chemical ecology 8 (1982), S. 383-396 
    ISSN: 1573-1561
    Keywords: Insect sex pheromone ; fall webworm moth ; American white moth ; Hyphantria cunea ; salt march caterpillar moth ; Estigmene acrea ; Lepidoptera ; Arctiidae ; (Z,Z)-9,12-octadecadienal ; linolealdehyde ; (Z,Z,Z)-9,12,15-octadecatrienal ; linolenaldehyde ; (Z,Z)-3,6-cis-9,10-epoxyheneicosadiene
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    Notes: Abstract Three compounds have been identified as sex pheromone components produced by female fall webworm moths,Hyphantria cunea (Drury). These compounds are: (Z,Z)-9,12-octadecadienal (I), (Z,Z,Z)-9,12,15-octadecatrienal (II), and (Z,Z)-3,6-cis-9,10-epoxyheneicosadiene (III). The ratio of these compounds was approximately 5∶6∶13, respectively, in female tip extracts prepared from U.S.S.R, insects and approximately 1∶8∶21, respectively, in extracts from U.S. insects. The ratio in female effluvia trapped from U.S. insects was 1∶6∶27, respectively. Compound III plus either I or II is effective in eliciting upwind flight in a wind tunnel. Compounds I, II, and III are also components of the sex pheromone system of the saltmarsh caterpillar moth,Estigmene acrea (Drury).
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  • 46
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    Journal of chemical ecology 8 (1982), S. 397-408 
    ISSN: 1573-1561
    Keywords: Pea moth ; Cydia nigricana (F.) ; Lepidoptera ; Olethreutidae ; sex attractant ; (E)-10-dodecen-1-yl acetate ; (E,E)-8,10-dodecadien-1-yl acetate ; inhibitor ; Synergist ; lure
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    Notes: Abstract (E)-10-Dodecen-1-yl acetate (E10–12∶Ac) and (E,E)-8,10-dodecadien-1-ylacetate (E,E8,10–12∶Ac) are sex attractants for males of the pea moth,Cydia nigricana (F.). Thirty-two structurally related compounds with chain lengths of 9–14 carbon atoms were exposed withE10–12∶Ac orE,E8,10–12∶Ac in traps in the field to investigate their influence on the activity of the attractants. Only alchols and acetates unsaturated at C-8, -9, or -10 greatly influenced moth captures. (Z) and (E)-8-dodecen-1-ol were weak synergists forE10–12∶Ac but no synergists forE,E8,10–12∶Ac were found. (Z) and (E)-8-dodecen-1-yl acetate and (E,E)-8,10-dodecadien-1-ol inhibited bothE10–12∶Ac andE,E8,10–12∶Ac while (E)-10-dodecen-1-ol, 10-dodecyn-1-ol, (Z) and (E)-9-dodecen-1-yl acetate, (Z)-10-dodecen-1-yl acetate, and undecyl acetate inhibited only the former attractant.
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  • 47
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    Journal of chemical ecology 8 (1982), S. 507-515 
    ISSN: 1573-1561
    Keywords: Almond moth ; Ephestia cautella ; Lepidoptera ; Pyralidae ; stored products ; pest management ; behavior ; density ; flight
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The mating rate ofEphestia cautella (Walker) was inversely related to the level of pheromone permeating the air. However, permeation did not prevent mating by altering the number of females calling or the frequency, duration, or pattern of male flight. Instead, permeation probably prevented mating by reducing the distance from which a male can respond to a female. The pheromone level necessary to achieve a particular reduction in mating increases with moth density.
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  • 48
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    Journal of chemical ecology 8 (1982), S. 663-670 
    ISSN: 1573-1561
    Keywords: Pandemis heparana ; sex pheromone ; Lepidoptera ; Tortricidae ; gas chromatography ; mass spectrometry ; insect behavior ; (Z)-11-tetradecen-1-yl acetate ; (Z)-9-tetradecen-1-yl acetate ; (Z)-11-tetradecenl-ol ; tetradecyl acetate ; dodecyl acetate
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    Notes: Abstract 90% (Z)-11-tetradecen-1-yl acetate, 5% (Z)-9-tetradecen-1-yl acetate, 5% (Z)-11-tetradecen-1-ol, dodecyl acetate (〈1%), and tetradecyl acetate (〈1%) were identified from gland extracts ofPandemis heparana females by gas chromatography and gas chromatography-mass spectrometry analysis (including mass fragmentography studies), chemical characterization, total synthesis, laboratory and field bioassays. In the field, a mixture of (Z)-11-tetradecen-l-yl acetate and (Z)-9-tetradecen-l-yl acetate (95∶5) was found to be essential for attractiveness ofP. heparana males.
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  • 49
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    Journal of chemical ecology 8 (1982), S. 755-762 
    ISSN: 1573-1561
    Keywords: Sex pheromone ; Heliothis virescens ; tobacco budworm ; Heliothis zea ; bollworm ; virelure ; Lepidoptera ; Noctuidae
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract None of the isolated degradation products of (Z)-11-hexadecenal [(Z)-11-HDAL] affected the catches of either tobacco budworm [Heliothis virescens (F.)] or bollworm [H. zea (Boddie)] moths when dispensed with pheromone from cotton dental rolls in cone traps. Also, none of the degradation products of (Z)-9-tetradecenal [(Z)-9-TDAL] had an effect on trap catches of tobacco budworm moths. Two of the three chemicals that have previously been identified in ovipositor washes of tobacco budworms but that are absent in those of bollworms caused a reduction in capture of bollworms: (Z)-9-TDAL (1.0 μg/trap) caused a 96% reduction in trap catch and (Z)-11-hexadecen-1-ol (20.0 μg/trap) caused a similar reduction. Tetradencenal (40 μg/trap) had no effect on trap catch.
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  • 50
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    Journal of chemical ecology 8 (1982), S. 843-850 
    ISSN: 1573-1561
    Keywords: Kairomones ; 2-acylcyclohexane-1 ; 3-diones ; Ephestia keuhniella Zeller ; (syn.Anagasta kuehniella Zeller) ; Lepidoptera ; Pyralidae ; Nemeritis canescens (Grav.) (syn.Venturia canescens (Grav.)) ; Ephestia cautella (Wlk.) ; Ephestia elutella (Hubner) ; Hymenoptera ; Ichneumonidae ; Plodia interpunctella (Hubner) ; oviposition
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    Notes: Abstract 2-Acylcyclohexane-1,3-diones, a novel class of compounds in the larval mandibular glands ofEphestia(=Anagasta) kuehniella Zeller, act as kairomones. Their relative activities in eliciting oviposition responses from the larval parasiteNemeritis(=Venturia) canescens (Grav.) are reported.
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  • 51
    ISSN: 1573-1561
    Keywords: Antennae ; esterases ; pheromone degradation ; cuticle ; olfaction ; cabbage looper ; Trichoplusia ni ; Lepidoptera ; Noctuidae
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Examination was made of the hydrolytic activities of esterases obtained from the antennae, legs, and wings of 3-day-old cabbage looper moths,Trichoplusia ni (Hübner), by elution and by homogenation of those appendages. Pheromone hydrolysis in 1-min assays was monitored by use of tritium-labeled (Z)-7-dodecen-1-ol acetate and thin-layer chromatography to separate the reaction products. Listed according to the activities of the esterases obtained by homogenation, the organs were antennae 〉 legs 〉 wings. In contrast, the order according to the activities of the eluted esterases was wings 〉 legs 〉 antennae. Also, the eluted enzymes were less active than the esterases obtained by homogenization. The relatively high pheromone-hydrolyzing activity present in homogenized antennae suggests that the esterases originated inside the antennae and lends support to the hypothesis proposed in earlier investigations that pheromone-inactivating enzymes may play an important role in the olfactory process, possibly by clearing pheromone from the vicinity of the olfactory receptors. The esterases detected on the cuticle, on the other hand, may function by preventing surface accumulation of pheromone. The higher measured esterase activity in homogenates of prothoracic legs than of mesothoracic or metathoracic legs suggests that the prothoracic legs, which are used to clean the antennae of debris, may function by removing and degrading pheromone from the surface of antennae.
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  • 52
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    Journal of chemical ecology 8 (1982), S. 923-933 
    ISSN: 1573-1561
    Keywords: Aldehyde pheromone ; bioluminescence ; corn earworm ; Heliothis zea ; insect pheromone ; navel orangeworm ; Amyelois transitera ; western spruce budworm ; Choristoneura occidentalis ; spruce budworm ; Choristoneura fumiferana ; Lepidoptera ; assay for aldehydes ; Pyralidae ; Noctuidae ; Tortricidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Pheromone levels in the glands of individual female moths of the spruce budworm (Choristoneura fumiferana), the western spruce budworm (C. occidentalis), the navel orangeworm (Amyelois transitella), and the corn earworm (Heliothis zea) were quantitively measured by means of a new bacterial bioluminescence assay specific for aldehydes. The sensitivity and rapidity of the bioluminescent assay enabled studies to be conducted on the dependence of the pheromone levels in the spruce budworm on age and the effect of photoperiod on the pheromone levels in the corn earworm. The bioluminescence assay provides a rapid and sensitive approach for studying aldehyde pheromone levels and their regulation in insects.
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  • 53
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    Journal of chemical ecology 8 (1982), S. 935-945 
    ISSN: 1573-1561
    Keywords: Aldehydes ; bioluminescence ; insect pheromones ; Porapak Q ; spruce budworm ; Choristoneura fumiferana ; Lepidoptera ; (E)-11-tetradecenal ; trapping ; bioassay for aldehydes
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract A newly developed bioluminescent assay was used to measure quantitatively the amount of (E)-11-tetradecenal, the major component of the sex pheromone of the spruce budworm, trapped on Porapak Q®. The bioluminescent response was linearly related to the amount of aldehyde either deposited on the absorbent or trapped from an airstream. However, the recovery of pheromone from Porapak was dependent on whether the air was prefiltered (through Porapak) or taken directly from the atmosphere. Furthermore, pheromone on Porapak was lost with time during the flow of air through the absorbent, indicating that trapping of aldehyde pheromone should be conducted for short periods of time for optimal recoveries. The applicability of the assay system for the rapid and direct measurement of the release rates of aldehyde pheromone lures was demonstrated for pheromone lures used for baiting spruce budworm traps.
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  • 54
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    Journal of chemical ecology 8 (1982), S. 973-980 
    ISSN: 1573-1561
    Keywords: (E, Z)-7,9-Dodecadien-1-yl acetate ; European grapevine moth ; Lobesia botrana ; Lepidoptera ; Tortricidae ; sex pheromone ; photoisomerization ; conjugated diene
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Photo- and radical isomerization of (E, Z)-7,9-dodecadien-1-yl acetate (DDA) leads to an equilibrium mixture of all four possible geometric isomers of 7,9-DDA in the ratio ofE,E, 69–76%;Z,E, 11–13%;E, Z, 12–15%; andZ, Z, 1–3%. Iodine catalysis of the isomerization takes place even in dark at room temperature and is probably a radical reaction.
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  • 55
    ISSN: 1573-1561
    Keywords: Heliothis virescens ; Lepidoptera ; Noctuidae ; Z11-16:Ald ; 16:Ald ; Z9-14:Ald ; 14:Ald ; sex pheromone emission ; gland volatiles ; blend composition ; pheromone emission rates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Sex pheromone gland volatiles from individualHeliothis virescens (F.) females were collected and analyzed on an SP-2330 capillary gas-liquid chromatography column for identification and quantification of the compounds emitted. Only four of the seven compounds previously reported as pheromone components appeared consistently in the volatile collections: 14:Ald, Z9-14:Ald, 16:Ald, and Z11-16:Ald. The female glands did not emit the same amounts of these compounds throughout a 24-hr period; they emitted maximum quantities between 6 and 11 hr after the onset of scotophase with the remainder of the photoperiod having minimal emission rates. Although the absolute quantities fluctuated, the percent compositions of the compounds remained about the same throughout the 24-hr period.
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  • 56
    ISSN: 1573-8744
    Keywords: phenytoin ; bioavailability ; Michaelis-Menten parameters
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    Topics: Chemistry and Pharmacology
    Notes: Abstract The bioavailability of phenytoin from rapid release capsule and oral solution formulations relative to that of a slow release capsule formulation was assessed in five patients who had participated in a three-way crossover study performed at steady state. The subjects then underwent dosage adjustment utilizing the slow release formulation, and estimates of their Michaelis-Menten parameters thus obtained were utilized in calculating the relative bioavailabilities. In addition, expected changes in steady-state plasma phenytoin concentrations were calculated assuming initial levels of 15 mg/liter, with increases and decreases in bioavailability of 10%. The consequences of such alterations in the extent of phenytoin absorption or average content of the dosage form may be clinically significant, particularly where the initial phenytoin level is equal to or greater than the patient's operative Km.
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  • 57
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    Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 465-494 
    ISSN: 1573-8744
    Keywords: disopyramide ; pharmacokinetics ; bioavailability ; metabolite ; half-life ; protein binding ; disease states ; drug-drug interaction
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    Topics: Chemistry and Pharmacology
    Notes: Abstract Current information on the pharmacokinetics of disopyramide is reviewed with emphasis on the implications for antiarrhythmic therapy. The absolute bioavailability, the disposition half-life, the plasma clearance, and the renal clearance for normal subjects and patients are discussed. Drug-drug interactions are discussed, and a new flexible intravenous dosing schedule is proposed.
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  • 58
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    Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 157-172 
    ISSN: 1573-8744
    Keywords: sulfisoxazole ; pharmacokinetics—unbound drug ; pharmacokinetics—total drug ; bioavailability ; healthy volunteers ; protein binding
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    Topics: Chemistry and Pharmacology
    Notes: Abstract Plasma concentrations of total and unbound sulfisoxazole were followed after single intravenous and oral doses of 1 g sulfisoxazole and during a 500-mg, four-time-a-day dosing regimen in six healthy males, using a specific high pressure liquid Chromatographic assay method. Saturable plasma protein binding was observed at total concentrations above 80–100 mg/liter. The clearance of sulfisoxazole was 18.7±3.9ml/min for total drug and 232±64ml/min for unbound drug. Renal elimination, on the average, accounted for 49% of the clearance of sulfisoxazole. The apparent volume of distribution for total drug was 10.9±2.0 liters and 136±36 liters for unbound drug, indicating that sulfisoxazole is primarily distributed extracellularly. Accumulation of N4-acetyl-sulfisoxazole during multiple dosing did not affect the disposition of sulfisoxazole. Adjusting for variable renal clearances between oral and intravenous administration and using the unbound plasma concentrations, the bioavailability for an oral dose of sulfisoxazole was found to be 0.95±0.04.
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  • 59
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    Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 231-245 
    ISSN: 1573-8744
    Keywords: nitrazepam ; i.v. ; oral ; rectal administration ; protein binding ; pharmacokinetics ; bioavailability
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    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics and bioavailability of nitrazepam following intravenous, oral (tablet), and rectal (solution) administration were studied in seven healthy, young male volunteers. Nitrazepam plasma concentrations were determined by electron-capture GLC; pharmacokinetic evaluations were made by compartmental analysis (NONLIN) and compared with the results obtained by a less stringent modelling of the data. The plasma concentration-time profile was similar for all three routes of administration. Mean kinetic parameters as obtained by compartmental analysis of i.v. nitrazepam were: distribution half-life 17 min; volume of distribution after equilibrium 2.14 liters/kg; total plasma clearance 61.6 ml/min; elimination half-life 29.0 h. The mean protein unbound fraction of nitrazepam in plasma was 12.3% and the clearance of the unbound fraction was 506 ml/min. Absorption of oral nitrazepam started after the elapse of a lag time (mean value 12 min) and occurred as an apparent first-order process in all but one subject, with a mean absorption half-life of 16 min. Distribution and elimination half-lives were comparable with those following i.v. administration. Following rectal administration of the nitrazepam solution, rapid first-order absorption occurred with a mean lag time of 4 min and a mean absorption half-life of 9 min. Peak times (median 18 min) were significantly shorter than following oral administration (median 38 min), but there was little difference in peak concentrations. The distribution half-life was similar to i.v. and oral administration, but the elimination half-lives were longer with a mean value of 33.1 h. Following i.v. administration a good agreement was found between the results obtained by compartmental analysis using NONLIN and those obtained by a less stringent modelling of the data. Following oral and rectal administration, a good agreement between the two procedures was found for the elimination half-life; estimation of bioavailability, however, was higher by compartmental analysis. The mean bioavailability data showed that absorption is complete when nitrazepam is given orally and almost 20% lower when it is given rectally, but considerable interindividual differences were observed.
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  • 60
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    Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 335-348 
    ISSN: 1573-8744
    Keywords: pharmacokinetics ; bioavailability ; growth ; literature growth ; logistic function
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    Topics: Chemistry and Pharmacology
    Notes: Abstract The literature growth in pharmacokinetics and bioavailability between the years 1964 and 1980 is analyzed. During much of this period, the literature doubled approximately every 1.6 years. However, during the period 1978–1980, little or no growth was observed. During the period 1950–1967, the total chemical literature increased exponentially with a half-life of 8.28 years; between 1968 and 1980, the half-life was 12.4 years. Thus, the pharmacokinetic literature increased at a much more rapid pace than did the total chemical literature in general. The subject of growth is considered in a general context, particularly as influenced by psychological, sociological, political, and economic factors. It is concluded that while mathematical functions may adequately describe past literature trends, they have little if any utility in predicting future trends in specific research areas such as pharmacokinetics.
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  • 61
    ISSN: 1573-8744
    Keywords: chloramphenicol-3-monosuccinate ; chloramphenicol-1-monosuccinate ; chloramphenicol ; bioavailability ; pharmacokinetics ; intravenous administration ; adult patients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of chloramphenicol (CAP) and total chloramphenicol succinate (CAPS) were studied in eight hospitalized adult patients with normal renal and hepatic function receiving intravenous chloramphenicol sodium succinate therapy. The steady-state peak concentrations of CAP (8.4–26.0 μg/ml) occurred at an average of 18.0 min (range 5.4–40.2) after cessation of the chloramphenicol sodium succinate infusion. Unhydrolyzed CAPS prodrug, representing 26.0±7.0% of the dose, was recovered unchanged in the urine indicating that the bioavailability of CAP from a dose of intravenous chloramphenicol succinate is not complete. A pharmacokinetic model was developed for simultaneous fitting of CAP and CAPS plasma concentration data. Pharmacokinetic parameters determined by simultaneous fitting were: V, 0.81±0.18 liters/kg; t1/2, 3.20 ±1.02 hr; CLB, 3.21±1.27 ml/min/kg for chloramphenicol; and V, 0.38±0.13 liters/kg; t1/2, 0.57±0.12hr; CLB, 7.72±1.87 ml/min/kg for total chloramphenicol succinate.
    Type of Medium: Electronic Resource
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