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目的:研制多西他赛自微乳化释药系统(DTX-SMEDDS)。方法:通过溶解度试验、处方配伍和伪三相图的绘制,以自微乳化时间、色泽和粒径的大小为指标,筛选油相、表面活性剂、助表面活性剂的最佳搭配和处方配比,制备获得DTXSMEDDS,并对DTX-SMEDDS的分散粒径、电位和体外溶出度等进行了测定。结果:DTX-SMEDDS自微乳化稀释后的粒径为96.9 nm,自微乳化时间<1 min,其在水中2 h累积溶出百分率为82.39%,是原料药(2.35%)的约35倍。结论:所制备的DTX-SMEDDS大大提高了多西他赛的溶解和溶出,为进一步研发多西他赛新制剂提供了理论和试验依据。
Objective: To develop docetaxel self-microemulsifying drug delivery system (DTX-SMEDDS). Methods: According to the solubility test, prescription compatibility and the pseudo-three-phase diagram, the optimal mix and prescription of oily phase, surfactant and cosurfactant were screened by the time, color and size of self-microemulsification The DTX-SMEDDS was prepared and the dispersion size, potential and in vitro dissolution of DTX-SMEDDS were determined. RESULTS: The self-microemulsified DTX-SMEDDS had a particle size of 96.9 nm and a self-microemulsification time of less than 1 min. The cumulative dissolution rate of DTX-SMEDDS in water at 2 h was 82.39%, about 35 times of that of raw drug (2.35%). CONCLUSION: The prepared DTX-SMEDDS greatly improves the dissolution and dissolution of docetaxel, and provides the theoretical and experimental basis for further research and development of new formulations of docetaxel.