摘要
目的:制备松萝酸自微乳,优化其处方,评价其质量。方法:采用乳化法,以中链甘油三酯-单亚油酸甘油酯(1∶1,m/m)为油相,聚氧乙烯氢化蓖麻油为乳化剂,二乙二醇单乙基醚为助乳化剂,制备松萝酸自微乳。在溶解度试验和伪三元相图的基础上,以自乳化时间(t)、透光率(T)、药物平衡溶解度(S)、5 min和60 min时药物的累积溶出度(Q_(5 min)、Q_(60 min))作为评价指标,采用星点设计-响应面法优化微乳处方中油相占比和乳化剂-助乳化剂质量比(K_m)。同时对最优处方进行验证试验,并对其形态、粒径、载药量、溶出度等进行考察。结果:最优处方中油相占比为25%、K_m为2.0,即处方中混合油相、乳化剂、助乳化剂的质量比分别为25%、50%、25%;最优处方所制松萝酸自微乳的t、T、S、Q_(5 min)、Q_(60 min)分别为1.96 min、87.67%、5.67 mg/g、66.58%、76.73%(RSD均小于3%,n=3),与预测值的相对误差均小于4%(n=3)。松萝酸自微乳经水稀释后为球形乳滴,乳化后平均粒径为39.4 nm,平均载药量为4.55 mg/g,在p H 6.8磷酸盐缓冲液中Q_(90 min)为99.58%(n=3)。结论:所制松萝酸自微乳的质量符合相关要求。关键词松萝酸;自微乳;伪三元相图;星点设计-响应面法;
OBJECTIVE：To prepare Usnic acid self-microemulsion,prescription optimization and evaluate its quality.METHODS：Usnic acid self-microemulsion was prepared by emulsification method using medium chain triglycerides-single linoleic acid glyceride（1∶1,m/m）as oil phase,polyoxyethylene hydrogenated castor oil as emulsifier,diethylene glycol monoethyl ether as co-emulsifier.Based on the solubility test and pseudotemary phase diagram,using self-emulsifying time（t）,light transmittance（T）,drug equilibrium solubility（S）,accumulative dissolution rate at 5 min and 60 min（Q5 min,Q60 min）as evaluation indexes,central composite design-response surface methodology was utilized to optimize oil phase ratio and ratio of emulsifier to co-emulsifier（Km）in microemulsion formulation.At the same time,the optimal formulation was verified,the morphology,particle size,drug-loading amount and dissolution of Usnic acid self-microemulsion were investigated.RESULTS：The optimal formulation was as follows as oil phase ratio of 25%,Kmof 2.0;ratio of mixed oil phase,emulsifier,co-emulsifier in the formulation was25%,50%,25%.t,T,S,Q5 min and Q60 min of Usnic acid self-microemulsion prepared by optimal formulation were 1.96 min,87.67%,5.67 mg/g,66.58%,76.73%（all RSD3%,n=3）,respectively.The relative errors of them to predicted values were all less than 4%（n=3）.Usnic acid self-microemulsion was spherical droplet in shape after diluted with water.The average particle size was 39.4 nm,average drug-loading amount was 4.55 mg/g.Q90 min of Usnic acid self-microemulsion reached 99.58%in p H 6.8phosphate buffer（n=3）.CONCLUSIONS：Prepared Usnic acid self-microemulsion is in line with quality requirements.
出处
《中国药房》
CAS
北大核心
2018年第3期312-317,共6页
China Pharmacy
基金
重庆市科学技术委员会基础与前沿研究计划项目(No.CSTC2014JCYJA10037)
关键词
松萝酸
自微乳
伪三元相图
星点设计-响应面法
质量评价
Usnic acid
Self-microemulsion
Pseudotemary phase diagram
Central composite design-response surface methodology
Quality evaluation
