脑得生口服微乳制剂与片剂在大鼠体内药动学比较

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1.8 mL·kg^-1·d^-1和脑得生片剂1.08 g·kg^-1·d^-1,收集处理大鼠血液样本,采用HPLC法于不同时间点(5,10,20,30,45 min,1,1.5,2,4,6,8,12 h)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(AUC_0-12、AUC_0-∞)和峰浓度(C_max)均明显增加(P<0.05),Puer的体内消除半衰期(t_1/2)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。

Comparison of pharmacokinetics of Naodesheng oral microemulsion and tablets

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 1.8 mL·kg^-1·d^-1 and tablets 1.08 g·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, 8 and 12 h). Finally, pharmacokinetic parameters were calculated by non-compartment model and analyzed by statistical software SPSS 13.0. RESULTS Compared with control group, AUC_0-12, AUC_0-∞ and Cmax of HSYA, Rg1, Puer and TMP were all significantly increased and t1/2 of 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.