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目的:对丹参酮ⅡA自微乳制剂进行体外释放和在体肠吸收评价。方法:以反向透析法进行丹参酮ⅡA自微乳制剂的体外释放度考察;采用大鼠在体小肠单向灌流实验模型,比较丹参酮ⅡA自微乳制剂和混悬液在大鼠肠道的吸收差异。结果:丹参酮ⅡA自微乳制剂45min内的累积释放度可达85%以上,而混悬液在90min内溶出度小于30%。大鼠在体肠吸收结果显示,丹参酮ⅡA自微乳制剂的吸收速率常数(Ka)和表观吸收系数(Papp)显著高于混悬液(P<0.01)。结论:自微乳制剂可显著提高丹参酮ⅡA的体外溶出和体内肠吸收程度。
Objective: To evaluate the in vitro release and in vivo intestinal absorption of tanshinone Ⅱ A self-microemulsion. Methods: The in vitro release of tanshinone ⅡA self-microemulsion was investigated by reverse dialysis method. The rat intestine absorption of tanshinone ⅡA difference. Results: The cumulative release of tanshinone ⅡA self-microemulsion reached more than 85% within 45 min, while the dissolution of the suspension in less than 30% within 90 min. The rat intestinal absorption results showed that the absorption rate constant (Ka) and apparent absorption coefficient (Papp) of tanshinone ⅡA self-microemulsion were significantly higher than that of the suspension (P <0.01). Conclusion: Self-microemulsion preparation can significantly improve the dissolution of tanshinone Ⅱ A in vitro and the degree of intestinal absorption in vivo.