目的制备丹参酮Ⅱ_A自微乳,为其新制剂开发提供参考。方法采用伪三元相图法研究不同乳化剂、助乳化剂和油相形成微乳的能力和区域,绘制不同处方组成的相图,并制备丹参酮Ⅱ_A自微乳。利用高效液相色谱法测定丹参酮Ⅱ_A在自微乳中的溶解度,考察自微乳的稳定性,并对微乳后的粒径大小、Zeta电位进行测定。结果所制备的自微乳中丹参酮ⅡA的溶解度为2.5 mg/g,对离心、高温破坏等稳定性良好,对光稳定性欠佳,微乳后可得到平均粒径在20 nm以下、Zeta电位绝对值在60 mV以上的微乳。结论丹参酮ⅡA自微乳制备简单,性质稳定,可显著增加丹参酮ⅡA在水中的溶解度。

Objective The self-microemulsifying drug delivery system(SMEDDS) with tanshinone ⅡA was prepared in order to develop its new dosage forms.Methods Pseudo ternary phase diagrams were used to evaluate the self-microemulsification existence area under emulsifier,coemulsifer,and oil phase.The HPLC analysis in vitro was set up.Solubility in various vehicles was determined.The self-microemulsification efficiency was assessed,such as stability,particle size,and Zeta potential.Results The solubi-lity of tanshinone ⅡA in SMEDDS was about 2.5 mg/g,droplet size was within 20 nm,and the absolute value of Zeta potential was over 60 mV.The stability of SMEDDS with tanshinone ⅡA was better in centrifugal condition with high temperature but not good enough to the light.Conclusion The SMEDDS can make tanshinone ⅡA solublized in water,and is an optimum vehicle in new dosage forms of tanshinone ⅡA.

中山大学2006年度暑期科研项目