Pharmacokinetics of UC-isotretinoin in healthy volunteers and volunteers with biliary T-tube drainage

Journal Article · Wed May 01 04:00:00 EDT 1985 · Drug Metab. Dispos.; (United States)

OSTI ID:6085642

Colburn, W A; Vane, F M; Bugge, C J; Carter, D E; Bressler, R; Ehmann, C W

The pharmacokinetics of isotretinoin and 4-oxoisotretinoin in blood, as well as the blood concentrations and urinary, biliary, and fecal excretion of carbon-14 were studied using liquid scintillation counting techniques and reverse phase HPLC methods following a single 80-mg oral suspension dose of UC-isotretinoin to four healthy male subjects and two patients with biliary T-tube drainage. Approximately 80% of the dose was recovered as UC in excreta during the course of the study of which about equal fractions were in the urine and feces. Secondary peaks in blood concentrations of UC were observed in the healthy subjects whereas they were not seen in the patients with T-tubes. The harmonic mean apparent half-life for isotretinoin in the blood of the healthy subjects was 13.6 hr, whereas the corresponding value for the UC was 90 hr. The data for isotretinoin and 4-oxoisotretinoin coupled with the total carbon-14 data suggest that the oral dose of UC-isotretinoin is absorbed to a similar extent by the healthy subjects and T-tube patients, whereas T-tube patients clear the drug more rapidly. The biliary excretion and possible enterohepatic circulation of isotretinoin and its metabolites may have significant impact on the pharmacokinetic profile of isotretinoin in man.

• Research Organization: Hoffmann-La Roche Inc., Nutley, NJ
• OSTI ID: 6085642
• Journal Information: Drug Metab. Dispos.; (United States), Journal Name: Drug Metab. Dispos.; (United States) Vol. 3; ISSN DMDSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
BILE
BILIARY TRACT
BIOLOGICAL MATERIALS
BIOLOGICAL WASTES
BODY FLUIDS
CARBON 14 COMPOUNDS
CHROMATOGRAPHY
DIGESTIVE SYSTEM
DRAINAGE
DRUGS
FECES
HALF-LIFE
KINETICS
LABELLED COMPOUNDS
LIQUID COLUMN CHROMATOGRAPHY
MATERIALS
PATIENTS
PHARMACOLOGY
SEPARATION PROCESSES
WASTES