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[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。
[Objective] To prepare niclosamide ethanolamine self-microemulsion drug delivery system to improve the water-solubility of the drug. [Method] According to the solubility of drugs in different solvents, the composition of the formulation was preliminarily determined. The pseudo-ternary phase diagram, the determination of the maximum drug loading of the blank formulation and the stability of the microemulsion after hydration of the drug formulation were further optimized. Determination of the particle size of the optimal formula, Zeta potential and other parameters, morphological observation, and investigate its stability. [Result] The optimal formula was ethyl butyrate as oil phase, Tween 20 as emulsifier, polyethylene glycol 200 as emulsifier, mass ratio of 1:6: 3, drug loading of 51.6 mg / g, The average particle size was 37.1 nm and the zeta potential was -38.6 mV, which was approximately spherical. The stability was good under low temperature, heat storage and room temperature. [Conclusion] The niclosamide ethanolamine salt self-microemulsifying drug delivery system has the advantages of simple preparation process, stable property and significant solubilization on the drug.