脑得生口服微乳制剂与片剂在大鼠体内药动学比较

Comparison of pharmacokinetics of Naodesheng oral microemulsion and tablets

目的:比较脑得生口服微乳制剂与片剂中有效成分的药动学特征,为脑得生口服微乳剂型设计及合理性评价提供依据。方法:选用清洁SD大鼠,随机分为实验组和对照组,分别灌胃给予脑得生口服微乳制剂1.8mL·kg-1·d-1和脑得生片剂1.08g·kg-1·d-1,收集处理大鼠血液样本,采用HPLC法于不同时间点(5,10,20,30,45min,1,1.5,2,4,6,8,12h)测定血浆中脑得生主要活性成分羟基红花黄色素A(HSYA)、人参皂苷Rg1、葛根素(Puer)、川芎嗪(TMP)的浓度。采用非房室模型计算主要药动学参数,并利用SPSS13.0统计软件进行统计学分析。结果:相比脑得生片剂,口服微乳制剂中HSYA、Rg1、Puer、TMP在大鼠体内的血药浓度-时间曲线下面积(AUC0-12、AUC0-∞)和峰浓度(Cmax)均明显增加(P<0.05),Puer的体内消除半衰期(t1/2)也明显延长(P<0.05)。结论:脑得生口服微乳制剂可有效增加有效成分HSYA、Rg1、Puer、TMP的吸收和生物利用度,是对中药制剂剂型改造的一次成功的探索。

OBJECTIVE To compare pharmacokinetic characteristics of Naodesheng oral microemulsion and tablets,provide a reference for formulation design and the reasonable evaluation of Naodesheng oral microemulsion.METHODS SD rats were selected and randomly divided into test group and control group.Naodesheng oral microemulsion 1.8mL·kg^-1·d^-1 and tablets1.08g·kg^-1·d^-1 were administered by oral route,respectively.Then rats were killed to collect blood and detect concentrations of HSYA,Rg1,Puer and TMP at different time points（5,10,20,30,45 min,1,1.5,2,4,6,8and 12h）.Finally,pharmacokinetic parameters were calculated by non-compartment model and analyzed by statistical software SPSS 13.0.RESULTS Compared with control group,AUC0-12,AUC0-∞and Cmax of HSYA,Rg1,Puer and TMP were all significantly increased and t1/2of Puer was longer in test group（P〈0.05）.CONCLUSION Naodesheng oral microemulsion can increase absorption and bioavailability of effective components of HSYA,Rg1,Puer and TMP.It is a successful exploration for reform of Chinese traditional medicine preparation.