摘要
大鼠经CCl_4损伤后,使醋酸甲地孕酮(Megestrol acetate,MA)的内在清除能力明显降低,清除半衰期(T_(1/2)β)显著延长,清除率(CL)明显下降,表观分布容积(Vd)无显著变化。大鼠经肝微粒体酶诱导剂苯巴比妥处理后,用MA静注给药,其药代参数与对照组比较无明显差异,而口服给药后血药浓度峰值(Cp)和药-时曲线下面积(AUC)与对照组相比明显下降,生物利用度显著降低,CL明显上升,而T_(1/2)β无明显变化。
Megegtrol acetate (MA) is widely used as a contraceptive agent in our country] In the present study, the pharmacokinetics of MA was investigated. The MA plasma conoentration was measured by radioimmunoassay (RIA).The pharmaobkinetios of MA in rats with hepatite injury showed: (1) Increased elimination phase half-life (T1/2β), (2) Decreased olearenee (OL) and rate constant (Ke), (3) No change in the volume of distribution (Vd).Phenobarbitone is a microsomal enzyme indnoer. In the rat, phenobarbitone pretreatment had little effect on the handling of MA given intravenously. There was no significant change in any of the pharmacokinetic parameters. In contrast, following oral administration, phenobarbitone pretreatmeat caused a signifioant reduction in the AUC and peak height (Op), a significant increase in OL, but no signifioant change in. T1/2β.
出处
《上海医科大学学报》
CSCD
1990年第3期205-210,共6页
Journal of Fudan University(Medical Science)
关键词
甲地孕酮
药代动力学
肝功能损伤
megestrol aoetate
mieiosomal enzyme induction
hepatic in injury
pharmaeokinetics
