多西他赛自微乳化释药系统的研究  

Study on Self - microemulsifying Drug Delivery System of Docetaxel

作　　者：陈鹰[1] 陈戈[1] 史琼枝[1,2] 余爱荣[1] 符旭东[1] 刘辉[1] 

机构地区：[1]广州军区武汉总医院,武汉430070 [2]咸宁学院药学院

出　　处：《中国药师》2009年第11期1507-1510,共4页China Pharmacist

基　　金：湖北省科技攻关课题(NO.2007AA301B15);湖北省自然科学基金计划重点项目(NO.2007ABA071)

摘　　要：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 study on self- emulsifying drug delivery system for docetaxel （DTX-SMEDDS）. Method： The optimum formulations of DCT-SMEDDS were screened by solubility experiments, compatibility tests and pseudo-ternary phase diagrams, with the time of formulating emulsion, the consequence of visual examination and particle size as parameters. And the physic-chemical characters and dissolution in vitro of DTX-SMEDDS were also determined. Result： The particle diameter of DTX-SMEDDS was 96.9 nm, the time of self-microemulsifying was less than 1 min. The percent of accumulated dissolution of docetaxel in SMEDDS in simulated intenstinal fluid was up to 82.39% at 2 h, which was 35 times as much as that of DTX crude powder. Conclusion： The solubility and dissolution of DTX was widely improved by the new DTX-SMEDDS. It could provide reference for the new dosage form of Docetaxel.

关 键 词：多西他赛 自微乳化 处方研究 理化性质 体外溶出度 

分 类 号：R944.9[医药卫生—药剂学]