氯硝柳胺乙醇胺盐自微乳释药系统的研制

Preparation of Niclosamide Ethanolamine Salt Self-microemulsifying Drug Delivery System

[目的]制备氯硝柳胺乙醇胺盐自微乳释药系统,改善该药的水溶性。[方法]根据药物在不同溶媒中的溶解度初步确定配方组成,通过绘制伪三元相图、测定空白配方最大载药量和载药配方水化后微乳的稳定性等途径进一步优化。测定最优配方的粒径、Zeta电位等参数,进行形态观察,并考察其稳定性。[结果]最佳配方选择丁酸乙酯为油相,吐温20为乳化剂,聚乙二醇200为助乳化剂,质量比为1∶6∶3,载药量为51.6 mg/g,平均粒径为37.1 nm,Zeta电位为-38.6 m V,近似圆球状,在低温、热贮及室温条件下稳定性良好。[结论]氯硝柳胺乙醇胺盐自微乳释药系统制备工艺简单,性质稳定,对该药有显著增溶作用。

[Aims] The niclosamide ethanolamine salt self-microemulsifying drug delivery system（NES-SMEDDS） was prepared to improve the solubility of niclosamide ethanolamine salt（NES）. [Methods] The composition was preliminary studied based on the solubility of the drug, then the pseudo-ternary phase diagram was drew and the largest drug loading and the stability were tested. Finally, the optimum prescription of NES-SMEDDS was determined, and the particle size, Zeta potential and morphology were studied. [Results] The optimal NES-SMEDDS prescription consisted of 10% of butyric acid ethyl ester, 60% of Tween 20 and 30% of PEG 200（w/w）. The drug loading of NES was 51.6 mg/g,the particle size of the microemulsion was 37.1 nm with Zeta potential of-38.6 m V. The NES-SMEDDS consisted of small spherical drops under transmission electron microscope（TEM）, and the stability was good under low temperature,heat store and room temperature. [Conclusions] The process was simple, and the SMEDDS provided a promising delivery system for enhancing the solubility of NES.