天钩降压胶囊中钩藤碱大鼠体内药动学研究

目的:研究天钩降压胶囊中钩藤碱在大鼠体内药动学及复方配伍对钩藤碱药动学的影响。方法:大鼠灌胃给予天钩降压胶囊(相当于钩藤碱18 mg·kg-1)及钩藤提取物(相当于钩藤碱18 mg·kg-1),于给药后不同时间采集大鼠血浆。血浆样品经乙醚提取,HPLC测定血浆中钩藤碱含量。各给药组钩藤碱平均血药浓度-时间数据用3P97药动学软件进行药动学分析,组间药动学参数用SPSS 16.0软件进行统计分析。结果:钩藤碱灌胃给药在大鼠体内符合一室模型,复方组钩藤碱的Ka、Cmax、Ke显著减小,t1/2(ka)、Tmax、t1/2(ke)显著增加,AUC、V/F(C)无显著性差异。结论:复方配伍延缓了钩藤碱的吸收,延长了体内滞留时间,但对其生物利用度及体内分布无显著影响。

Pharmacokinetics Study of Rhynchophylline from Tiangou Jiangya Capsule in Rats

Objective：To study the pharmacokinetics of rhynchophylline i？om Tiangou Jiangya capsule and The effect of the compound compatibility on the pharmacokineties of rhynehophylline in rat. Methods：Tian- gou Jiangya capsule（equivalent to rhynchophylline 18 mg-kg-1） and one dosage of uncaria extract（equivalent to rhynchophylline 18 mg.kg-1） were administered to rats by intragastric administration separately. Plasma samples were collected at different times and extracted with ethyl ether. The contents of rhynchophylline in plasma were determined by HPLC method. The mean plasma concentration-time curves of different medica- tion administration teams were processed with 3P97 pharmacokinetic software. Pharmacokinetic parameters between groups were statistically analyzed by SPSS 16.0. Results：After oral administration of rhynchophylline, rhynchophylline in rat was fitted to a one-compartment model,the significant decrease for Ka,Cmax,Ke,signif icant increase for t1/2（ka）,Tmax,t1/2（ke） and no significant difference for AUC,V/F（c） in compound Tiangou Jiangya capsule. Conclusions：Compound compatibility can delay the absorbtion of rhynchophylline and prolong the resident time in vivo. There is no effect on bioavailability and biodistribution.