地氯雷他定自乳化释药系统的制备及质量评价

Preparation and quality evaluation of desloratadine self-microemulsifying drug delivery system

目的研究地氯雷他定(DL)自微乳的制剂处方与制备工艺,并对其质量进行评价。方法通过溶解度实验,伪三元相图实验,油相、乳化剂及助乳化剂配伍实验,筛选出DL自微乳制剂的处方组成;以乳滴平均粒径,载药量及包封率为指标,采用单纯形网格法优化制剂处方,并对DL自微乳的理化性质,溶出度以及稳定性进行评价。结果 DL自微乳处方中油相为中碳链三甘酯(MCT)(35%),乳化剂为聚乙二醇-12羟基-硬脂酸酯(HS15)(45%),助乳化剂为1, 2-丙二醇(20%)。所得自微乳制剂外观均一透明,略带黏性,自乳化后平均粒径为20.21 nm,平均载药量为20.95 mg/g,包封率为76.56%。溶出度实验结果表明,DL 60 min累积溶出率达到93.78%。稳定性实验表明,高温、光照影响自微乳制剂的稳定性,制剂应低温避光保存。结论 DL自微乳制剂制备工艺简单,质量稳定,能显著增加药物的溶解度,进而提高DL的口服生物利用度。

Objective to study the formulation, preparation and quality evaluation of DL self-microemulsion preparation. Methods through solubility test, pseudo-ternary phase diagram test, oil phase, emulsifier and co-emulsifier compatibility test, the formulation of DL self-microemulsion preparation was screened out. Through particle size determination, drug loading and encapsulation rate determination, simplex mesh method was used to optimize the formulation, and the physical and chemical properties, dissolution and stability of self-microemulsion preparation of DL were evaluated. Results the oil phase of DL from the formulation of microemulsion was medium c-triglyceride(MCT)(35%),(HS15)(45%), and 1, 2-propylene glycol(20%). The dissolution test results showed that DL accumulated dissolution rate reached 93.85% after 60 min. The stability experiment shows that low temperature, high temperature, high humidity and illumination all affect the stability of self-microemulsion preparation, so the preparation should be kept dry in room temperature away from light. Conclusion the preparation process of DL self-microemulsion preparation is simple, the excient components are low toxic and the quality of the preparation is stable, which can significantly increase the solubility of the drug, thus improving the oral bioavailability of DL. It provides reference for the further research and development about the related preparations of this drug.