西罗莫司自乳化给药系统及其固体化研究

发布时间：2018-02-15 04:25

本文关键词： 西罗莫司自微乳化给药系统固体化星点设计微丸　出处：《药学实践杂志》2016年02期 　论文类型：期刊论文

【摘要】：目的筛选西罗莫司自微乳给药系统处方,并制备微丸。方法通过溶解度试验确定助乳化剂、油相和乳化剂的选择范围;采用三元相图法、星点设计和效应面法对该体系优化制备工艺及处方。采用挤出-滚圆法制备不同处方的西罗莫司自微乳化微丸。结果西罗莫司自微乳微丸的最终处方为:西罗莫司0.4%、油酸聚乙二醇甘油酯9.3%、聚氧乙烯-35-蓖麻油15.9%、二乙二醇单乙基醚8.0%、微晶纤维素49.8%、乳糖13.3%、羧甲基淀粉钠3.3%。溶出度试验显示,西罗莫司固体自微乳微丸在水中的溶出度远大于市售西罗莫司片,在0.4%SDS溶液中,两制剂的溶出度相当。结论自微乳化给药系统可用于提高西罗莫司的体外溶出度。
[Abstract]:Objective to screen the prescription of sirolimus self-microemulsion delivery system and prepare pellets. Methods the selection range of co-emulsifier, oil phase and emulsifier was determined by solubility test, and the ternary phase diagram method was used. Star design and effect surface method were used to optimize the preparation process and formulation of the system. Different formulations of sirolimus self-emulsified pellets were prepared by extrusion-roller method. Results the final formulation of sirolimus self-emulsion pellets was as follows: sirolimo. The amount of polyethylene glycol oleate was 9.3%, polyoxyethylene 35 castor oil 15.9%, diethylene glycol monoethyl ether 8.0, microcrystalline cellulose 49.8%, lactose 13.3%, carboxymethyl starch sodium 3.3%. Dissolution test showed that, The dissolution of sirolimus solid self-emulsion pellets in water was much higher than that of sirolimus tablets sold on the market. In 0.4SDS solution, the dissolution rates of the two preparations were similar. Conclusion the self-microemulsified drug delivery system can be used to improve the dissolution of sirolimus in vitro.
【作者单位】：南京军区福州总医院药学科;
【基金】：福建省科技计划重点项目(2013Y0074) 福建省自然科学基金(2010J01218)
【分类号】：R943

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