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。
Objective To design and optimize the formulation of lacidipine self-mincroemulsion in order to improve its absorption,biological availability and clinical efficiency.Methods By determining the solubility of lacidipine in various materials,we made a choose and combined it with various materials.With fully fonsidering the self emulsification region of the different prescription in ternary phase diagrams drawing,central composite design and response surface method,speed of emulsify,particle size distribution,zeta potential,the optimal formulation was confirmed.Then its surface and emulsion droplet form was obsevred,its dissolution and distribution was determined.Results The optimal formulation was Labrafil M 1944 cs,EL and PEG-400 with the weight percentage of 29.15%,51.16%and 19.69%,which can be quickly emulsified.The resultant microemulsion was clarified and transparent,and the particle size was distributed in the range of 15-30 nm.83.6%of lacidipine in formulation could be quickly released in 2 min under the experimental conditions,and products were stable for 3 months.Conclusions The optimal lacidipine selfmicroemulsion formulation can obviously improve lacidipine emulsifying efficiency and the rate of dissolution in vitro in order to improve its bioavailability.
作者
张云雷
刘晓娟
ZHANG Yun-lei LIU Xiao-juan(School of Pharmacy, Jinzhou Medical University, Jinzhou 121001, China)
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2017年第3期207-212,265,共7页
Journal of Shenyang Pharmaceutical University
关键词
拉西地平
自微乳
处方优化
体外评价
星点设计-效应面法
lacidipine
self-microemulsifying
formulation optimization
in vitro evaluation
composite design and response surface method
