苦参碱的利胆作用与药代动力学的关系

Relationship of Cholagogic Action of Matrine and its Pharmacodynamics

苦参碱具有促进大鼠胆汁分泌的作用。在５０、１００和１５０ｍｇ／ｋｇｉｇ三个剂量组中以１００ｍｇ／ｋｇ组的利胆作用最强，持续时间也最长。三个剂量的最大效应时间均在给药后的６０ｍｉｎ左右。大鼠１５、３０、６０ｍｇ／ｋｇ的口服生物利用度分别为４３．７％、４７．４％和３１．６％，达峰时间ｔｍａｘ平均为５８ｍｉｎ（５８．０±１３．４ｍｎ）。结果显示当苦参碱的血药浓度达峰时其利胆作用最强，且随血药浓度的降低而减弱。同时，作用强度与其生物利用度呈正性相关。

Matrine possesses the action of promoting bile secretion of rat.Among 50,100 and 150mg/kg(ig )dosage groups the 100 dosage group has the strongest cholagogic action and longest unremirring time. The maximum effect-times of three dosage groups are all about 60 min after administration.The oral bioavailability of 15,30 and 60mg/kg rats ate 43.7%,47.4%and 31.6%,respectively with 58min of maximum avetage peak-reaching time(58.0±13. 4min).The results indicated that the cholagogic action will be the strongest when the blood-dtug concentration of matrine reachs the peak and will attenuate as the blood-drug concentration decrease. Meantime,the strength of cholagogic action shows positive correlation with bioavailability.