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目的:测定妇炎康灌肠剂有效成分芍药苷的药动学参数,为临床合理用药提供科学依据。方法:分别单剂量ig与灌肠给予家兔妇炎康灌肠剂,用HPLC测定血浆中芍药苷的浓度,用3p97程序拟合药物浓度-时间曲线,计算药动学参数。结果:ig给药后,血浆中未能检出芍药苷;直肠给药后,芍药苷在家兔体内过程符合一室开放模型,药动学参数为:ka为3.190 9 h-1,ke为0.943 8 h-1,t1/2(ka)为0.217 2 h,t1/2(ke)为0.734 4 h,Tmax为0.542 1 h,Cmax为0.542 1 mg·L-1,AUC0-4 h为9.260 2 mg·L-1 h-1。结论:与ig给药比较,妇炎康灌肠剂经直肠给药后其主要有效成分在家兔体内吸收更加迅速、完全。
Objective: To determine the pharmacokinetic parameters of paeoniflorin, the active ingredient in Fuyankang enema, to provide a scientific basis for clinical rational drug use. Methods: Rabbits were given Fuyankang enema with single dose ig and enema. The concentration of paeoniflorin in plasma was determined by HPLC. Pharmacokinetic parameters were calculated by fitting the drug concentration - time curve with 3p97 program. Results: Paeoniflorin could not be detected in the plasma after ig administration. Paracetamol in rabbits was consistent with one-compartment open model after rectal administration. The pharmacokinetic parameters were as follows: ka = 3.190 9 h-1, ke = 0.943 8 h-1, t1 / 2 (ka) was 0.217 2 h, t1 / 2 (ke) was 0.734 4 h, Tmax was 0.542 1 h, Cmax was 0.542 1 mg · L-1 and AUC0-4 h was 9.260 2 mg · L-1 h-1. Conclusion: Compared with ig administration, Fu Yan Kang enema after rectal administration of the main active ingredients absorbed more rapidly and completely in rabbits.