具杀精作用的右旋普萘洛尔在家兔体内的药物动力学  

Pharmacokinetics of R-(+ )- Propranolol in Rabbits,-A Spermaticide Drug

作　　者：周慧君[1] 顾芝萍[1] 

机构地区：[1]中国科学院上海药物研究所,浙江医科大学药学系

出　　处：《生殖与避孕》1996年第1期49-54,69,共7页Reproduction and Contraception

摘　　要：本文采用ＨＰＬＣ－荧光检测法研究了右旋普茶洛尔在家兔体内的药物动力学。结果：药时曲线经静脉注射给药符合开放三房室模型，经阴道给药符合开放二房空模型。家兔在阴道给予５、１０、１５ｍｇ／ｋｇ右旋普萘洛尔后，剂量与ＡＵＣ、Ｃｍａｘ值线性相关（ｒ≥０．９９）；生物利用度分别为７９．４９％、５１．５８％、５５．３８％；两种给药途径的ｔ１／２ａ、ｔ１／２β均无显著差异，并且ｔ１／２β相当接近，静脉注射１０ｍｇ／ｋｇ剂量组为２．３１ｈ、阴道给药的三个剂量组分别为２．３１、２．６５、２．３２ｈ。表明右旋普茶洛尔在家兔体内的动力学过程为线性一级动力学过程，且吸收快、消除快、不易积蓄，无代谢饱和现象。The pharmacokinetic characteristics of R -(+ )- propranolol were studied by high pressure liquid chromatography with fluorescence detection. The plasma concentration - time curve of R (+ )- propranolol in New Zealand white female rabbits after a single vaginal administration was best fitted to a two - compartment open model,and that after a single intravenenous administration was best fitted to a three - compartment open model. The bioavailability of vaginal doses of 5、10 and 15mg/kg was 79. 49% .51. 58 % and 55. 38% and the t1/2β after the vaginal doses were 2. 31、2. 65 and 2. 32 h respectively,while that after iv 10mg/kg was 2. 31 h;AUC and Cmax were in proportion with the dose(r≥0. 99). The results suggested that the pharmacokinetics of R -(+)propranolol in rabbits are constant with lst order by linear kinetics and. rapidly eliminated from plasma,and thus cumulative doses would not result in me.tabolic saturation and cumulative intoxication of the drug.

关 键 词：右旋普萘洛尔 杀精作用 药物代谢动力学 

分 类 号：R979.21[医药卫生—药品] R969.1[医药卫生—药学]