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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 the pharmacokinetics of active ingredients in brain microemulsions and tablets, and provide the basis for the design and rational evaluation of oral microemulsion formulations. Methods: SD rats were randomly divided into experimental group and control group. The rats were given intragastric oral microemulsion 1.8 mL · kg-1 · d-1 and brain-derived tablets 1.08 g · kg-1 · D-1, collecting and processing blood samples of rats, using HPLC method at different time points (5,10,20,30,45min, 1,1.5,2,4,6,8,12 h) were measured plasma brain The main active ingredients of hydroxy safflor yellow A (HSYA), ginsenoside Rg1, Puerarin (Puer), ligustrazine (TMP) concentration. Non-compartmental model was used to calculate the main pharmacokinetic parameters, and SPSS13.0 statistical software was used for statistical analysis. RESULTS: Compared with naïve tablets, the area under the plasma concentration-time curve (AUC0-12, AUC0-∞) and peak concentration (Cmax) of HSYA, Rg1, Puer and TMP in oral microemulsion were significantly higher (P <0.05). Puer’s elimination half-life (t1 / 2) also significantly prolonged (P <0.05). Conclusion: Nansheng Oral Microemulsion can effectively increase the absorption and bioavailability of HSYA, Rg1, Puer and TMP, and is a successful exploration of the formulation modification of traditional Chinese medicine preparation.