PHARMACOKINETICS OF RAPAMYCIN - SINGLE-DOSE STUDIES IN THE RABBIT

被引：22

作者：

HONCHARIK, N

FRYER, J

YATSCOFF, R

机构：

[1] UNIV ALBERTA, DEPT LAB MED & PATHOL, EDMONTON T6G 2E1, ALBERTA, CANADA

[2] UNIV MANITOBA, HLTH SCI CTR, DEPT PHARMACEUT SERV, WINNIPEG R3T 2N2, MANITOBA, CANADA

[3] UNIV MANITOBA, HLTH SCI CTR, DEPT SURG, WINNIPEG R3T 2N2, MANITOBA, CANADA

来源：

THERAPEUTIC DRUG MONITORING | 1992年 / 14卷 / 06期

关键词：

RAPAMYCIN; PHARMACOKINETICS; RABBIT;

D O I：

10.1097/00007691-199212000-00007

中图分类号：

R446 [实验室诊断]; R-33 [实验医学、医学实验];

学科分类号：

1001 ;

摘要：

The pharmacokinetics of rapamycin was investigated in five New Zealand white rabbits following intravenous administration of 0.05 and 0.5 mg/kg rapamycin in a randomized crossover fashion. Whole blood concentrations of rapamycin were analyzed by high-performance liquid chromatography (HPLC). Model-dependent and -independent parameters were calculated. The volume of distribution at steady state and total body clearance increased significantly as the dose increased. Rapamycin pharmacokinetics appear to be nonlinear. The whole blood volume of distribution, especially at the higher dose, indicated distribution out of the blood component. The drug is not cleared rapidly, with a terminal half-life of >13 hours as calculated by model-independent parameters. The 24-h whole blood trough concentrations of the drug are well within the analytical range of the HPLC procedure. This should permit trough level monitoring for therapeutic range studies involving the drug.

引用

页码：475 / 478

页数：4

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