苦参素片与苦参素胶囊的药动学和生物等效性研究

目的:比较苦参素片与苦参素胶囊的人体药动学参数,评价二者的生物等效性。方法:将18名健康志愿者分为2组,分别空腹口服苦参素片(受试制剂)或苦参素胶囊(参比制剂)各600mg。于给药前、后采用高效液相色谱法测定氧化苦参碱血药浓度,计算2种制剂的药动学参数(以氧化苦参碱计)。结果:苦参素片、苦参素胶囊的药动学参数t1/2分别为(1.51±0.62)、(1.53±0.54)h,tmax分别为(1.35±0.13)、(1.29±0.13)h,Cmax分别为(730.86±101.13)、(729.58±74.35)ng.mL-1,AUC0～8分别为(2 579.1±244.4)、(2 505.7±223.5)ng.h.mL-1,AUC0～∞分别为(2 754.1±331.8)、(2 659.4±253.5)ng.h.mL-1。苦参素片的相对生物利用度为(103.7±13.3)%。结论:苦参素片、苦参素胶囊的主要药动学参数无显著差异,个体间、周期间和剂型间符合生物等效的假设,二者是生物等效制剂。

Pharmacokinetics and Bioequivalence of Matrine Tablets and Matrine Capsules in Healthy Volunteers

OBJECTIVE： To compare the pharmacokinetic parameters between matrine tablets and matrine capsules in healthy volunteers and evaluate the bioequivalence of the two formulations. METHODS： 18 healthy volunteers were assigned to receive matrine tablets （test formulation, 600mg） and matrine capsule （reference formulation） respectively q.d on empty stomach. The plasma concentrations of oxymatrine before and after medication were determined by HPLC and the pharmacokinetic parameters （calculated by oxymatrine） were calculated. RESULTS： The pharmacokinetic parameters of matrine tablets vs.matrine capsules in healthy volunteers were as follows ： t 1/2： （ 1.51 ± 0.62）h vs. （ 1.53 ± 0.54） h ; Tmax： （ 1.35 ± 0.13） h vs.（1.29± 0.13） h; Cmax： （730.86± 101. 13） ng.mL^-1 vs. （729.58± 74.35） ng.mL^-1; AUC0-8：（2 579.1 ± 244.4） ng . h .mL^-1 vs.（2 505.7±223.5） ng .h.mL^-1; AUC0-∞： （2 754.1±331.8） ng.h.mL^1 vs.（2 659.4±253.5） ng.h.mL^-1.The relative bioavailability of matrine tablets（calculated by oxymatrine） was（103.7 ± 13.3）% . CONCLUSION： There are no significant di- fferences between matrine tablets and matrine capsule in main pharmacokinetic parameters, which were in conformity with the presumption of bioequivalence between different individuals, different periods or different dosage forms. The two formulations are bioequivalent.