可注射丹参酮ⅡA自微乳制剂的处方筛选及化学稳定性考察  

Formulation optimization and chemical stability study of Self-microemulsified Tanshinone ⅡA emulsion for injection

作　　者：张晓君[1] 王东凯[1] 姚建美[1] 韩晓[1] 王玉[1] 

机构地区：[1]沈阳药科大学药学院

出　　处：《中国药剂学杂志（网络版）》2010年第5期117-125,共9页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的建立丹参酮IIA自微乳化制剂处方及含量测定方法,并考察其稳定性。方法通过溶解度实验,配伍实验和三元相图的绘制,以乳化效果为指标筛选油相,乳化剂和助乳化剂,采用星点设计-效应面法选择最优处方比例制备丹参酮IIA自乳化微乳。用HPLC法测定丹参酮IIA自微乳化制剂的药物含量及高温、光照加速实验前后药物的含量,考察其化学稳定性。结果以优化的条件,辛酸/葵酸三甘油脂为油相,聚氧乙烯蓖麻油和磷脂为混合乳化剂,乙醇为助乳化剂,质量比为27.81:37.64:9.48:25.07,所制备的自微乳给药系统中丹参酮IIA的溶解度质量分数为0.75%,乳化后可得到平均粒径61.5nm的微乳。处方经高温实验下,0、5、10d丹参酮IIA的平均含量质量分数的变化为99.9%、99.2%、99.1%。结论星点设计-效应面法适用于丹参酮IIA自微乳给药系统的处方优化,按照优化的处方可制备粒径较小的丹参酮IIA自微乳化给药系统,所制备的制剂对热稳定,光照降解,应避光保存。Objective To optimize the formulation of Tanshinone IIA loaded self-microemulsifying drug delivery systems (SMEDDS) and study its chemical stability.Method The oil phase,emulsifier and coemulsifier of tanshinone IIA self-microemulsifying emulsion was selected based on solubility experiments,compatibility tests and pseudo-ternary phase diagrams using emulsification efficiency as the criteria.The optimal formulation was predicted by response surface design method.The content and chemical stability of the SMEDDS formulation was evaluated by HPLC.Result The optimal composition was GTCC:ELP:SPC:Ethanol=27.81:37.64:9.48:25.07,the drug loading and particle size were 7.5mg/g and 61.5 nm,respectively.The average content of Tanshinone IIA in the SEMDDS was 99.9%,99.2%,99.1%,respectively,after being stored at 40℃ for 0,5 and 10 days,.Conclusion The central composite design-response surface method is useful for the formulation optimization of tanshinone IIA self-microemulsion drug delivery system.Self-microemulsifying drug delivery system of tanshinoneIIA could be prepared according to the optimal formulation.The preparation was stable to heat,but need to be protected from light.

关 键 词：药剂学 丹参酮IIA 自微乳化给药系统 星点设计 效应面法 化学稳定性 

分 类 号：R283[医药卫生—中药学]