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  • pharmacokinetics  (30)
  • Triticum aestivum  (9)
  • Lepidoptera  (8)
  • Bone
  • Springer  (52)
  • 2015-2019
  • 1980-1984  (52)
  • 1983  (41)
  • 1980  (11)
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  • Springer  (52)
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  • 2015-2019
  • 1980-1984  (52)
Year
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 17 (1980), S. 111-116 
    ISSN: 1432-1041
    Keywords: zimelidine ; norzimelidine ; antidepressants ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The systemic availability of a new antidepressant, zimelidine, and of its pharmacologically active metabolite, norzimelidine, was studied in six healthy male volunteers. Three single doses of zimelidine (25 mg and 100 mg orally and 25 mg i.v.) and two single doses of norzimelidine (25 mg orally and i. v.) were given to each volunteer allowing at least seven days between administrations. Plasma concentrations of zimelidine and norzimelidine were determined in serial blood samples by HPLC. Following oral zimelidine peak plasma concentrations of the metabolite were attained about 3 h after dosing. Oral administration of norzimelidine itself resulted in a plasma concentration profile for this compound that was similar to that observed after oral zimelidine. Utilising the plasma concentration data following intravenous infusion of each compound, the elimination half-lives for zimelidine and norzimelidine were calculated to be 5.1 h (range 4.3–6.0) and 15.5 h (range 10.6–22.9) respectively. The total body clearances of the 2 compounds were similar at 0.52 l · min−1 (range 0.26–0.70) for zimelidine and 0.56 l · min−1 (range 0.28–0.83) for norzimelidine. The substantially longer elimination half-life of norzimelidine was apparently the result of a larger volume of distribution (9.4 l · kg−1; range 7.8–11.4) for this metabolite, as compared to zimelidine (3.21 · kg−1; range 1.6–4.9). The calculated bioavailability of zimelidine was 26% (range 9.1–39) after the 25 mg oral dose, and 29% (range 14–46) after the 100 mg dose. The bioavailability of norzimelidine was 66% (range 36–91). However, oral administration of zimelidine resulted in as much or more norzimelidine reaching the systemic circulation, as the oral administration of norzimelidine itself. This is important as a large part of the activity of the drug may be due to the metabolite.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: cimetidine ; intravenous infusion ; pharmacokinetics ; peptic ulcer ; duration of infusion ; acute dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The use of cimetidine administered by bolus intravenous injection to critically ill patients has been associated with serious cardiac arrhythmias, due presumably to high initial plasma concentrations. The aim of this study was to determine the range of infusion times of a single 200 mg dose of cimetidine which would avoid high initial drug concentrations while maintaining a duration of effective concentrations no less than that resulting from bolus injection. Computer simulations of both maximum plasma cimetidine concentrations and duration of effective plasma cimetidine concentrations versus duration of infusion were based on mean pharmacokinetic date from 6 peptic ulcer patients who had received cimetidine 200 mg i.v. over 5 min. The simulations indicated that to reduce maximum plasma cimetidine concentrations by at least 50%, while maintaining the duration of effective plasma concentrations, the infusion time should be at least 30 min and no longer than 4.5 h. The validity of the simulations was subsequently tested in 4 of the patients, who received cimetidine 200 mg i.v. over 30 min. The mean maximum plasma concentration for the 30 min infusion (4.57±0.53 µg/ml) was, as predicted, approximately half that corresponding to bolus administration in these patients (8.97±1.96 µg/ml). Moreover, the duration of effective concentrations for the infusion (1.43±0.28 h) was significantly greater than that for the 5 min infusion (1.21±0.31 h). We suggest that where an acute intravenous dose of cimetidine (200 mg) is indicated, it should be administered over at least 30 min rather than as a bolus.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 567-568 
    ISSN: 1432-1041
    Keywords: astemizole ; ethanol ; antihistamine ; pharmacodynamics ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of astemizole (10 mg daily for 7 days) on the kinetics and CNS depressant activity of ethanol have been examined in a double-blind cross-over study agonist placebo in 7 volunteers. There was no significant change in the elimination rate or AUC of the plasma ethanol concentration-time curve after astemizole. Central nervous system effects of ethanol as monitored by visual analogues of sedation, visual discrimination, pursuit rotor and reaction time were also unaffected by astemizole pretreatment.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 24 (1983), S. 349-352 
    ISSN: 1432-1041
    Keywords: diltiazem ; pharmacokinetics ; intravenous dose ; oral dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetic profile of diltiazem, a novel calcium antagonist, was studied in 12 volunteers following oral (60 mg) and intravenous (15 mg) administration. After i.v. administration biphasic elimination was observed, with a distribution half-life of 0.3±0.2 h and an elimination half-life of 3.1±1.0 h; the apparent volume of distribution was 5.3±1.71/kg and the total clearance was 1.28±0.48 l/kg/h. After the oral dose the elimination phase had a half-life of 3.2±1.3 h. The absolute bioavailability of diltiazem ranged from 24 to 74% (mean 42±18%). The interindividual variation may be explained by a variable first pass effect.
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  • 5
    ISSN: 1432-2242
    Keywords: HMW glutenin subunit genes ; cDNA clones ; Tandem DNA repeats ; Chromosomal location ; Gene copy number ; Wheat ; Triticum aestivum
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary cDNA clones encoding wheat HMW glutenin subunits have been isolated from a cDNA bank made to poly A+ RNA from developing wheat endosperm var. Chinese Spring. One such clone, pTag 1290, has enabled us to identify the HMW glutenin mRNA species. The DNA sequence of this clone has been partially determined and it contains several tandem DNA repeats. The sequence is discussed in relation to the generation of the HMW glutenin subunit gene family. Analysis of the organization of the HMW glutenin sequences in the wheat genome revealed that the genes encoding HMW glutenin subunits exist in low copy number and are located on the long arm of each of the homoeologous group 1 chromosomes.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 11 (1983), S. 183-187 
    ISSN: 1573-8744
    Keywords: nonlinear regression ; parameter estimation ; invariance ; transformation ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract It is shown that when one nonlinear regression model is a reparametrization of a second model, the parameter estimates, and their standard errors, for one model can be obtained directly from those obtained from fitting the other model.
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  • 7
    ISSN: 1573-8744
    Keywords: naltrexone ; controlled release ; pharmacokinetics ; gas chromatography ; biodegradable copolymer delivery system ; release rate quantitationin vivo ; Loo-Riegelman method
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Naltrexone release rates from a controlled release delivery system have been quantitated over a time period greater than one month in the monkey. The method requires calibration of the pharmacokinetic parameters of each monkey utilizing an intravenous bolus dose and assay of unchanged naltrexone levels in plasma as a function of time after dosing. Also required are periodic plasma levels of unchanged naltrexone obtained subsequent to administration of the delivery system. Release rates are then calculated as well as the total amount released. Application of the methodology to a biodegradable copolymer naltrexone delivery system in three monkeys showed an initial release rate of 3– 8% of the dose per day over the first 3– 5 days followed by a slow, rather constant release rate of 1– 3% per day from day 5 to the time of the last measurable plasma sample (36– 43 days). Comparison of alternative calculation methods using both experimental and simulated plasma naltrexone data verified the accuracy of the release rate calculations. The sum of the calculated total amount of naltrexone released plus the assayed amount remaining in the delivery system after removal from the animal accounted for 91– 94% of the administered dose in the two monkeys in which complete data were obtained.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 32 (1980), S. 189-194 
    ISSN: 1432-0827
    Keywords: Bone ; Fluoride ; Strength ; Porosity ; Mineralization
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary Radiographically normal vertebral bone cylinders from 80 male subjects were tested mechanically by static compression and analyzed for porosity, fluoride and ash content. As a group, they had low fluoride content, suggesting little prior intake, consonent with this geographic area. Nevertheless, increasing levels of fluoride were associated with bulkier bone, less porosity, and less mineral per unit of bone, which in direction though not degree suggested changes similar to those of osteomalacia and opposite from those of osteoporosis without apparent threshold. The higher fluoride hard tissue was weaker in static tests than that with less fluoride, but the increased bulk apparently offset this, resulting in bones of unchanged static strength. Hence, water fluoridation should not alter static bone strength. There has, however, been a recent report suggesting that increased mineralization of bone renders it more brittle and thus more likely to fracture on impact. Therefore, the possibility that fluoridation may increase impact resistance by lessening mineralization can be entertained.
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  • 9
    ISSN: 1432-0827
    Keywords: Bone ; Osteosarcoma ; Matrix vesicles ; Alkaline phosphatase ; Aminopeptidase ; Naphthylamidase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary Extracellular matrix vesicles from bovine fetal alveolar bone and from a dog osteosarcoma were isolated by differential centrifugation and then fractionated on a discontinuous sucrose density gradient. The fractions were examined by electron microscopy and were analyzed for protein, alkaline phosphatase, aminotripeptidase, and four different β-naphthylamidase activities. The low-density peak of enzyme activities was shown by electron microscopy to be much more homogeneous than the crude matrix vesicle fraction. Two major peaks of protein and enzyme activities were present, one in the high and one in the low density layers. There was good correlation between the activities of alkaline phosphatase and the various peptidases in the fractions from the sucrose density gradient. These results indicate a coexistence of peptidase and alkaline phosphatase in matrix vesicles. On the other hand, there was generally no correlation between the peptidase and alkaline phosphatase activities in vesicular specimens from bovine liver obtained in the same way. Most of the peptidase activity and about half of the alkaline phosphatase activity were solubilized from bone matrix vesicles by detergents. The extracted alkaline phosphatase and alanyl β-naphthylamidase activities were separated from each other on a DEAE-cellulose column.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 30 (1980), S. 15-20 
    ISSN: 1432-0827
    Keywords: Bone ; Osteoclasts ; Macrophage ; Resorption ; Plutonium
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary Female rats were used to study the kinetics of plutonium transfer from the bone surfaces of the mandibular condyle to osteoclasts and macrophages. This study was made using autoradiographs prepared from plastic sections of the mineralized bones of animals which had been injected with241 Pu citrate. Measurements of the concentration of plutonium in the osteoclasts and macrophages at different times after the injection of plutonium showed that plutonium was concentrated by osteoclasts from bone surfaces and was retained with a half-time of ∼ 70 h. Subsequently, plutonium appeared to be transferred to macrophages. The results showed that plutonium was unlikely to be accumulated by macrophages as a result of their participation in bone resorption.
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