Pharmacokinetics and absolute bioavailability of colchicine after i.v. and oral administration in healthy human volunteers and elderly subjects

Autor: Jean Michel Scherrmann, M. Rochdi, C. Girre, R. Venet, A. Sabouraud
Rok vydání: 1994
Předmět:
Zdroj: European journal of clinical pharmacology. 46(4)
ISSN: 0031-6970
Popis: The pharmacokinetics of colchicine were studied in six healthy male and four elderly female volunteers after i.v. and oral administration. Plasma samples were collected over 72 h and assayed for colchicine by a specific and sensitive radioimmunoassay. Plasma concentration-time curves were fitted using a three-compartmental model after i.v. administration of 0.5 mg (healthy volunteers) and 1 mg (elderly group) colchicine. The first distribution half-life (t1/2 lambda 1) was short: 9.2 min in healthy volunteers and 3.0 min in the elderly group; the second distribution half-life (t1/2 lambda 2) was of the same order for both groups, 1.2 h. Plasma elimination half-lives were also in the same range: 30 h for healthy volunteers versus 34 h for the elderly subjects. Mean residence time was also in the same range in the two groups: 27 h in healthy volunteers and 21 h for elderly subjects. The volume of distribution (Vz) was 6.7 l.kg-1 for the healthy group and 6.3 l.kg-1 for the elderly group, while Vss was smaller: 4.2 l.kg-1 for healthy volunteers and 2.9 l.kg-1 for elderly subjects. Total body clearance was 10.5 l.h-1 for healthy and 5.5 l.h-1 for elderly subjects. After oral administration of 1 mg, lag-time was 14 min in healthy volunteers and 11 min in elderly subjects. Maximal plasma concentration was 5.5 ng.ml-1 at 62 min in the healthy group, while in the elderly group Cmax was 12 ng.ml-1 at 87 min. Mean absolute bioavailability of the tablet was the same in both groups, 44% for healthy volunteers and 45% for elderly subjects.
Databáze: OpenAIRE
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