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  • theophylline  (5)
  • quinidine  (3)
  • plasma concentrations  (2)
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  • 1
    Electronic Resource
    Electronic Resource
    Intraindividual variability in theophylline pharmacokinetics: Statistical verification in 39 of 60 healthy young adults (1982)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 123-134 
    Details
    ISSN: 1573-8744
    Keywords: theophylline ; pharmacokinetics ; variability ; disposition rate constant ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract After administering a single 300 mg dose of theophylline in oral solution to 12 healthy adults, the dose-normalized area under the plasma concentration-time curve was 97.2±20.1 % (mean±SD) of that after giving a 500 mg dose and statistically indistinguishable. Similarly, these areas multiplied by the individual's terminal disposition rate constant (β) were statistically indistinguishable between 300 and 500mg doses (99.1±10.3%), giving no evidence of dose-dependence for theophylline kinetics at the levels below 15 μg/ml observed in these individuals. After an intravenous dose, a shortlived distribution phase (t1/2α) is sometimes seen. An a phase, however, is hardly discernible in over 250 profiles arising from oral doses administered during five single dose bioavailability studies. Almost all such profiles appear to follow single-compartment model predictions. With precautions to avoid a potential a phase, a terminal log-linear slope can be fitted by least squares analysis with a relative standard error in the slope determination almost always less than 6%. Covariance analysis confirms statistically that 39 of the 60 participating individuals varied in their β on the different occasions each was required to take a dose during the course of a crossover bioavailability trial. In one study, even though each individual was observed on only two occasions, 9 out of 12 showed statistically identifiable variation in β. Fluctuations in β of 60% can be seen. Changes of 30% or greater are common and can occur within 3 or 4 days. Thus real, large, and potentially frequent changes in β of theophylline have been identified in a majority of normal subjects. These changes do not appear to be confined to either sex, to smokers or nonsmokers, or to heavier or lighter individuals. No chronological pattern has, as yet, been recognized in the intraindividual variability in β.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01062330
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  • 2
    Electronic Resource
    Electronic Resource
    Divergence in pharmacokinetic parameters of quinidine obtained by specific and nonspecific assay methods (1979)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 7 (1979), S. 303-311 
    Details
    ISSN: 1573-8744
    Keywords: quinidine ; pharmacokinetic parameters ; assay methods ; assay specificity ; area under the plasma concentration-time curve ; bioavailability ; clearance ; therapeutic window
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Previously published estimates of pharmacokinetic characteristics of quinidine can be shown to be dependent on whether the investigators have used analytical methods which are specific for quinidine. Areas under the plasma concentration-time curve and peak plasma concentrations after administration of the drug were higher and clearance values consequently lower in studies utilizing nonspecific assays unable to distinguish quinidine from its metabolites. The error introduced is larger after oral administration as a result of marked first-pass metabolism of quinidine. The absolute oral bioavailabilities from pharmaceutical preparations might therefore be estimated higher in studies with assays including metabolites in the determination. Although the pharmacodynamic response to quinidine is related to the plasma concentration, the therapeutic window of drug concentrations has been defined only using nonspecific assays. In light of the availability of newly developed specific assays, redefinition of the range of therapeutic plasma concentrations is opportune.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01060020
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  • 3
    Electronic Resource
    Electronic Resource
    Gastrointestinal absorption of quinidine from some solutions and commercial tablets (1980)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 243-255 
    Details
    ISSN: 1573-8744
    Keywords: quinidine ; bioavailability ; absorption ; solutions ; rapidiy releasing tablets ; humans
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The gastrointestinal absorption of quinidine from three commercially available tablet products has been compared to that from a quinidine sulfate solution previously found to have 70% of the systematic availability of an intravenous dose. Quinidine gluconate solution was included in the study to compare the absorption characteristics of the two quinidine salts. The tablets were given in a counterbalanced sequence preceded by one quinidine solution and followed by the other in a crossover design. The three tablets proved to be equivalent to one another with respect to extent and rate of absorption. The absorption properties of the two solutions were indistinguishable. The tablets were equivalent to the solutions in extent but not in rate of absorption.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01059645
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  • 4
    Electronic Resource
    Electronic Resource
    Evaluation of the absorption from some commercial enteric-release theophylline products (1980)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 151-164 
    Details
    ISSN: 1573-8744
    Keywords: theophylline ; absorption ; bioavailability ; enteric release ; tablets ; plasma concentrations ; dissolution data
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract In a single-dose bioavailability study, Wales, Robinson, Columbia, and Choledyl (Warner/Chilcott) enteric-coated tablets all allowed a bioavailability of theophylline (99%±25%, 102%±23%,103%±18%, and 98%±15%;mean±SD, n=12) statistically indistinguishable from that of the standard uncoated tablet (Searle 200 mg aminophylline). Only the Wales and Choledyl tablets (7.6, 4.2 hr) could be shown (p〈0.05) to generate a peak plasma theophylline concentration later than the standard (1.4 hr). All tablet brands demonstrated a significant lag time before appearance of theophylline in the plasma, and both Wales and Choledyl tablets also had a (t peak -t tag )statistically different from that of the standard. Despite misleading indications from the mean plasma profile (plasma concentrations at each sampling time averaged over all subjects), plasma data from the individual participants and in vitrodissolution data show that, while release of theophylline from the Wales tablet might be inordinately slow, this is not a sustained-release preparation. Of the enteric-coated tablets only the Columbia product allowed significant levels in the first sample after dosage. Five of the 18 Columbia doses gave rise to 40–99%of the peak concentration in the 1- hr sample. In vitro,it takes 39±14 min for 40% of the theophylline content of Columbia tablets to dissolve in simulated intestinal fluid. Surprisingly rapid delivery of an entericcoated tablet to the duodenum would appear to be required to allow a significant percentage of theophylline to be dissolved and absorbed before 1 hr. None of 12 Columbia tablets tested in vitro,however, allowed dissolution of more than 0.2% of their theophylline content during 1 hr immersion in simulated gastric fluid. Since once in intestinal fluid Columbia tablets appear to dissolve more rapidly than the other enteric products, it is not clear whether the five Columbia tablets in question had imperfections or whether, in fact, this tablet brand more closely than the others represents the ideal of immediate release once in the duodenum. Plasma samples should be taken as early as 15 min after dosage when evaluating the bioavailability of enteric release products.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01065190
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  • 5
    Electronic Resource
    Electronic Resource
    Evaluation of the absorption from 15 commercial theophylline products indicating deficiencies in currently applied bioavailability criteria (1980)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 229-242 
    Details
    ISSN: 1573-8744
    Keywords: theophylline ; absorption ; tablets ; oral solution ; intravenous ; bioavailability criteria
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The biovailability of theophylline from alcoholic and aqueous oral solutions was compared to that from an intravenous dose in 12 normal adults. The alcoholic elixir surprisingly gave rise to a significantly greater (114 ±14%, mean±sd amount absorbed than did the intravenous dose. The aqueous solution (99±8%) and intravenous dose were statistically indistinguishable in this respect, and, furthermore, the extent of absorption from a 300-mg dose of the aqueous solution was 99±10% of that from a 500-mg dose, and not statistically different. The aqueous solution was thus employed in three subsequent studies as a standard with which to compare 13 different types of theophylline tablets, all marketed in the United States. Of the 13 tablets, eight showed bioavailability statistically distinguishable from that of the standard. Nevertheless, for only two tablets could it be claimed with 95% confidence that the bioavailability was less than 95%. For none can it be stated at this confidence level that the bioavailability is less than 90%. Bioavailability studies should include criteria of clinical significance in addition to criteria of statistical significance. Contrary to the usual rationale behind choice of a bioavailability standard, nine of the 12 uncoated tablets appeared to allow more rapid absorption of theophylline than did the standard oral solution, an aqueous syrup. Increasing the dose of syrup decreased the rate of theophylline absorption. Orally administered drug solutions may have properties more absorption rate limiting than the disintegration of many brands of tablet.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01059644
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  • 6
    Electronic Resource
    Electronic Resource
    Evaluation of the absorption from some commercial sustained-release theophylline products (1980)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 8 (1980), S. 131-149 
    Details
    ISSN: 1573-8744
    Keywords: theophylline ; absorption ; bioavailability ; sustained release ; tablets ; plasma concentrations ; mean plasma concentrations ; steady-state projections
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Absorption of theophylline from three commercial products labeled as sustained release was compared to the absorption from a standard uncoated tablet (Searle 200-mg aminophylline tablet) in a single-dose study. Aminodur tablets (Cooper) and Slophyllin Gyrocap capsules (Dooner) had bioavailability (100.2%±19.8% and 98.5%±13.8%) statistically indistinguishable from that of the standard but showed significantly slower absorption (peak times of 10,4±2.8 and 4.36±1.35 hr) and lower peak plasma concentrations (13.9±4.5 and 22.6±3.5gmg/ml/g dose) than the standard (t peak ,1.52±0.45 hr; Cpeak,28.l±6.2μg/ml/g dose). The time of the plasma concentration peak (2.47±1.38 hr) after a dose of Tedral S.A. (Warner/Chilcott) was not statistically different from that after the standard, but both the peak concentration (16.0±3.9 gmg/ml/g dose) and bioavailability (76.0±18.4%) were. Multiple-dose projections from single-dose data indicate that of the three test products only Aminodur maintains reasonably constant interdose plasma levels during 12 hourly dosing. With an 8 hourly dosing schedule Gyrocaps also might be satisfactory. Reasonable predictions of the plasma concentrations arising from Aminodur doses have been made using a single-compartment body model and assuming input from an outer followed by an inner layer of the tablet. Typically a single dose of a preparation designed for constant release of drug over 12 hr should not produce a plasma concentration plateau in subjects with an average 6.1-hr drug half-life. The apparent plateau in the mean plasma profile (i.e., concentrations at each sampling time averaged over all subjects) for Aminodur doses is evaluated. The interpretation commonly being implied in the publication of mean profiles from bioavailability studies is misleading, particularly when applied to sustained-release preparations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01065189
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  • 7
    Electronic Resource
    Electronic Resource
    A method for estimating within-individual variability in clearance and in volume of distribution from standard bioavailability studies (1982)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 135-146 
    Details
    ISSN: 1573-8744
    Keywords: theophylline ; intraindividual variability ; within-individual variability ; clearance ; volume
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Bioavailability studies are commonly undertaken, and most, because they involve subjects taking repeated doses of a drug, contain information on intraindividual variability in pharmacokinetics. However, because in such studies bioavailability itself is unknown, it is difficult to resolve which pharmacokinetic parameters vary within individuals. A mathematical model is presented which permits estimation of variability in clearance and in volume of distribution. When applied to pooled data arising from five theophylline bioavailability studies, this model has given statistical evidence that clearance of theophylline is inherently more variable within individuals (coefficient of variation, 13%) than volume of distribution (8%). As a result, use of the measurement AUC ·β rather than AUCas a more precise index of bioavailability is justified in studies where β is measured with reasonable precision. The model could be applied to estimation of withinbatch within-person variability in bioavailability.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01062331
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  • 8
    Electronic Resource
    Electronic Resource
    Quinidine pharmacokinetics in man: Choice of a disposition model and absolute bioavailability studies (1979)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 7 (1979), S. 315-330 
    Details
    ISSN: 1573-8744
    Keywords: quinidine ; pharmacokinetic models ; curve fitting ; bioavalability ; absorption ; humans ; plasma ; intravenous ; oral
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Parameters describing disposition and absolute oral bioavailability of quinidine were determined in ten normal male volunteers using a specific assay. Various models were compared for their ability to describe the experimental data. An intravenous quinidine gluconate and an oral quinidine sulfate solution were administered (3.74 mg/kg quinidine base). In three subjects the intravenous and oral studies were repeated. One-, two-, and three-compartment models with zeroand first-order input were fitted to the plasma concentrations. The selection of the best model was made by the Akaike information criterion and by eye. After intravenous administration, plasma concentrationtime curves could be adequately described by a twocompartment model. Mean disposition constants (±SD) were obtained from individualized fits (V1: 0.398 ±0.336 liter/kg, Vdarea: 2.53±0.72 liter/kg, α: 0.316±0.294 min−1, Β: 0.00204 ± 0.00262 min1, k2: 0.0305 ±0.010 min−1). A clearance of 4.9 ±1.5 ml/min/kg was observed. After oral administration, threecompartment models were needed to describe the observed data in some cases. Absorption was in most cases best described by a zeroorder rather than by a firstorder process. The time to peak concentration varied from 23 to 121 min, the lag time was always less than 3 min, and the mean elimination rate constant was 0.00171 min−1. The mean oral bioavailability of quinidine was 0.70 ±0.17.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01062532
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