丹参酮Ⅱ_A自微乳制剂的体外释放和在体肠吸收评价

Assessment of tanshinone Ⅱ_A self-microemulsifying preparation with drug release in vitro and intestinal absorption in situ

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 drug release characteristics in vitro and the intestinal absorption behavior in situ of tanshinone ⅡA self-microemulsifying preparation（TA-SMP）.Methods：In vitro release studies were conducted by reverse dialysis technique.Rat single-pass intestinal perfusion technique was employed and the absorption properties of TA-SMP were evaluated by comparison with the suspension.Results：The dissolution of TA-SMP at 45 min was much higher（more than 85%） than that of the suspension（less than 30%）.The values of the absorption rate constant（Ka） and the intestinal apparent permeability coefficient（Papp） of Tan-SM were significantly higher than that of the suspension（P〈0.01）.Conclusion：The self-microemulsifying delivery systems can significantly increase the dissolution of tanshinone ⅡA in vitro and absorption rate in rat intestine in situ.