蒿甲醚自微乳化给药系统的制备及体外评价张亚红林凤云邱妍川.DOCVIP

蒿甲醚自微乳化给药系统的制备及体外评价 张亚红 林凤云 邱妍川 朱照静* （重庆医药高等专科学校 400030） 摘要：目的：制备蒿甲醚自微乳化给药系统（ARM-SMEDDS），优选其最佳处方，并对其进行初步的质量评价。方法：通过溶解度实验和伪三相图的绘制筛选ARM-SMEDDS并对其理化性质和体外溶出度进行。结果：蒿甲醚自微乳化油相为Lauroglycol 90 ()，乳化剂为Cremophor RH 40 ( ) , 助乳化剂为Gelucire 44/14 ( ) 。ARM-SMEDDS 的粒径为(61.5±8.66) nm， Zeta电位为?32.45±5.42) mV，自微乳化时间 2 min。体外溶出度考察结果显示ARM-SMEDDS在120 min即能达到＞9%的溶出率累积溶出百分率是原料药的7倍。结论：所制备的ARM-SMEDDS溶出度高，且稳定性良好，为蒿甲醚新剂型的进一步开发奠定了基础。 Preparation of the self-microemulsifying drug delivery system of Artemether and the solubility evaluation in vitro Zhang Yahong Lin Fengyun Qiu Yanchuan Zhu Zhaojing* ( Chongqing Medical and Pharmaceutical College，400030) Abstract: Aim: To prepare the self microemulsifying drug delivery system (SMEDDS) of artemether (ARM) and evaluate the physico-chemical property and dissolution in vitro. Methods: The solubility in different oils and surfactants were determined and pseudo-ternary phase diagrams were plotted. The formation of ARM-SMEDDS was optimized by using the orthogonal design. The properties such as self-microlisifying time and Zeta potentials, the stability and the dissolution in vitro were evaluated. Results: The optimized formation of ARM-SMEDDS were composed of artemether 80mg/g, Lauroglycol 90 ( 0.4g/g) as oil, Cremophor RH 40 ( 0.4g/g) as surfactant and Gelucire- 44/14 ( 0.2g/g) as co-surfactant. ARM-SMEDDS was indicated to have the mean potential size of (61.5±8.66) nm, Zeta potential of (?32.45±5.42) mV and the self-microemulsifying time were all less than 2 minutes. ARM-SMEDDS was found to be stable at room temprature up to 3 months. The percentage of accumulated dissolution was more than 99.5% at 120 min which was 7 fold when compared with the ARM powder. Conclusions: The ARM-SMEDDS has good dissolution and stability which provides a strong foundation for further studies. Keywords: artemether , self-microemulsifying drug delivery system (SMEDDS), pseudo-ternary phase diagrams, quality assessment. 课题来源：重庆市卫生局2012 年医学科