论文部分内容阅读
目的:研制尼莫地平(nimodipine,NM)自微乳化释药系统(SMEDDS)。方法:以溶解度,相容性试验、自乳化效率及伪三元相图法筛选最佳油相、表面活性剂及助表面活性剂;以星点设计-效应面法优化处方;对NM-SMEDDS分散后粒径、体外溶出度及初步稳定性进行考察。结果:经处方筛选和星点效应面法优化得出最佳处方为:Captex200P,Cremophor EL,Labrosol分别为油相,乳化剂和助乳化剂,比例为30∶47∶23;NM-SMEDDS的粒径分别为33.8±3.42 nm,1 h累积溶出百分率为98.83%,约为市售片剂的3.84倍;经高温(60℃)、低温(4℃)、强光(4 500±500)Lx考察10 d,除强光可引起NM含量降低外,其他各项指标均无明显变化。结论:该处方及工艺筛选、优化法简便可行,容易控制,制备得到的NM-SMEDDS体外溶出度显著增加,稳定性较好,为进一步研发尼莫地平新制剂提供了理论和试验基础。
Objective: To develop nimodipine (NM) self-microemulsifying drug delivery system (SMEDDS). Methods: The optimal oil phase, surfactant and co-surfactant were screened by solubility, compatibility test, self-emulsification efficiency and pseudo-ternary phase diagram method. After dispersion, particle size, in vitro dissolution and initial stability were investigated. Results: The optimal prescriptions were optimized by prescription screening and star-spot effect surface method: Captex200P, Cremophor EL and Labrosol were oil phase, emulsifier and co-emulsifier in the ratio of 30:47:23, NM-SMEDDS tablets (33.8 ± 3.42 nm, respectively). The cumulative dissolution rate at 1 h was 98.83%, which was about 3.84 times higher than that of the commercial tablets. After high temperature (60 ℃), low temperature (4 ℃) and bright light (4 500 ± 500) Lx On the 10th day, except for the glare, the content of NM was decreased, while the other indexes did not change significantly. Conclusion: The prescription and the process screening, the optimization method is simple and feasible, easy to control, NM-SMEDDS prepared in vitro dissolution significantly increased, the stability is good, and provides a theoretical and experimental basis for further research and development of new formulations of nimodipine.