拉西地平自微乳的制备与体外评价

发布时间：2018-03-16 05:21

本文选题：拉西地平　切入点：自微乳　出处：《沈阳药科大学学报》2017年03期 　论文类型：期刊论文

【摘要】：目的设计和优化拉西地平自微乳处方,改善药物吸收,提高拉西地平的生物利用度和临床疗效。方法通过测定拉西地平在各种辅料的溶解度,对各类辅料进行初步筛选和配伍。并利用三元相图绘制不同处方的自乳化区域,星点设计-效应面法结合外观、乳化速度、粒径分布、Zeta电位等指标,综合考虑确定自微乳的最优处方。并进行体外评价,观察乳液的外观、乳滴形态,测定粒径分布和溶出度。结果最优处方为:Labrafil M 1944cs、EL和PEG400各自所占的质量分数分别为:29.15%、51.16%和19.69%,此处方乳化速度快,液体澄清透明,略显淡蓝色,粒径分布15~30 nm,在实验条件下,2 min溶出度可达82.6%,并且放置3个月性质稳定。结论筛选出拉西地平自乳化的最优处方,拉西地平自微乳乳化效率和体外溶出速度显著提高,从而有效提高其生物利用度。
[Abstract]:Objective to design and optimize the formulation of lacidipine self-microemulsion, improve drug absorption, improve the bioavailability and clinical efficacy of lacidipine. Methods the solubility of lacidipine in various excipients was determined. The self-emulsifying regions of different prescriptions were drawn by ternary phase diagram, the appearance, emulsifying speed, particle size distribution and Zeta potential were combined with star design-effect surface method. The optimum formulation of self-microemulsion was determined and evaluated in vitro to observe the appearance and droplet morphology of the emulsion. The particle size distribution and dissolution were determined. Results the optimal formulation was: 1: Labrafil M 1944cslEL and PEG400 occupied 51.16% and 19.69%, respectively. The emulsifying speed of the solution was fast, the liquid was clear and transparent, and the liquid was slightly blue. Under the experimental conditions, the dissolution rate of 2 min could reach 82.6 and the property was stable for 3 months. Conclusion the optimum formulation for self-emulsification of lacidipine was obtained, and the emulsifying efficiency and dissolution rate of microemulsion were improved significantly. Thus, the bioavailability can be improved effectively.
【作者单位】：锦州医科大学药学院;
【分类号】：R943

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