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  • 1
    ISSN: 1573-8744
    Keywords: chlordiazepoxide ; benzodiazepine ; two-compartment model, biopharmaceutics ; pharmacokinetics ; single dose ; routes of administration ; intravenous ; intramuscular ; oral
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Single 30- mg doses of chlordiazepoxide HCl were administered to six healthy human subjects by the intravenous, oral, and intramuscular routes. Plasma concentration- time curves following intravenous administration were satisfactorily described by a biexponential equation consistent with a two-compartment open model system. Mean values of half-lives for the so-called distribution and elimination phases were 0.252 and 9.39 hr, respectively. The mean values for the volume of the central compartment (V 1) and volume of distribution $$(V_{d_\beta } )$$ were 18.0 and 30.9% of body weight, respectively. Following oral administration, the drug was rapidly and completely absorbed. Absorption was first order (t1/2≈27 min), and three of the six subjects showed a discernible lag time of approximately 20 min. Drug absorption following intramuscular administration was comparatively slow. A two- compartment “muscle model” comprised of precipitated and solubilized drug in the muscle was found to satisfactorily characterize the absorption process following administration by this route.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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  • 2
    ISSN: 1573-8744
    Keywords: chlordiazepoxide ; benzodiazepine ; two-compartment model ; multiple dosing ; pharmacokinetics ; biopharmaceutics ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Eight healthy male volunteers received chlordiazepoxide HCl orally at a dosage of 10 mg every 8 hr over a period of 21 days. On day 22, the regimen was changed to 30 mg every 24 hr for an additional 15 days. Plasma concentrations of chlordiazepoxide and its metabolites desmethyl-chlordiazepoxide, demoxepam, and desoxydemoxepam were measured during 14 of the 36 treatment days. Chlordiazepoxide plasma concentration- time data were consistent with first-order absorption and complete bioavailability. The harmonic mean absorption half-life was 12.3 min. Disposition of chlordiazepoxide was described by a two-compartment open model with a harmonic mean terminal exponential half-life of 10.1 hr. Average steady — state plasma levels of chlordiazepoxide, desmethylchlordiazepoxide, and demoxepam were approximately 0.75, 0.54, and 0.36 μg/ml, respectively.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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