摘要
目的:制备蝙蝠葛碱自微乳化释药系统(Dau-SMEDDS)并对其进行质量评价。方法:通过溶解度试验、伪三元相图绘制和正交试验设计筛选并优化处方;考察优化处方所制制剂的类型、粒径和Zeta电位、体外累积溶出率和3个月内的稳定性以评价其质量。结果:最优处方为载药量为50 mg/g,以油酸-油酸乙酯(1∶1)为油相,聚氧乙烯醚-40氢化蓖麻油为乳化剂,月桂酸聚乙二醇甘油酯为助乳化剂,后二者比为2∶1,油相与混合乳化剂的比例为2∶5。所制系统为O/W型微乳,平均粒径为(58.3±9.21)nm,40 min即几乎全部溶出,累积溶出率为原料药的4倍以上,常温下3个月内各检查指标保持稳定。结论:本试验制备Dau-SMEDDS的工艺简单,溶出速率快,性质稳定。本研究可为蝙蝠葛碱新剂型的开发提供参考。
OBJECTIVE： To prepare and evaluate the quality of self-microemulsifying drug delivery system of dauricine （Dau-SMEDDS）. METHODS： The formulation of Dau-SMEDDS was optimized by the solubility test, pseudo-ternary phase dia- grams and orthogonal design. The type, particle size and Zeta potential, cumulative in vitro dissolution rate, and stability within 3 months of the preparation produced on the basis of the above-mentioned formulation were observed to evaluate the quality of such preparation. RESULTS： The optimal formation was as follows as the drug-loading of 50 mg/g, oleic acid-EO （1 ： 1） as oil phase, Cremophor RH 40 as emulsifier, Gelucire 44/14 as co-emulsifier, Km of 2：1 and oil phase-mixed emulsifier ratio of 2：5. The pre- pared Dau-SMEDDS was an O/W microemulsion, with average particle size of （58.3 ± 9.21） nm, in which nearly all the drug was dissolved within 40 min, demonstrating a cumulative dissolution rate more than 4 times as much as that of crude materials; the test- ed indexes kept stable at room temperature within 3 months. CONCLUSIONS： The technology of preparing Dau-SMEDDS is sim- ple with high dissolution rate and stable nature of the drug. The study can provide a reference for the development of new formula- tions of dauricine.
出处
《中国药房》
CAS
北大核心
2015年第16期2269-2272,共4页
China Pharmacy
关键词
蝙蝠葛碱
自微乳化释药系统
伪三元相图
制备
处方筛选
正交试验
质量评价
Dauricine
Self-microemulsifying drug delivery system
Pseudo-ternary phase diagrams
Preparation
Formulation screening
Orthogonal test
Quality evaluation
