姜黄素自微乳化制剂制备及其稳定性研究

Study on Preparation and Stability of Curcumin-loaded Self-microemulsifying Drug Delivery System

目的:研究姜黄素自微乳化制剂(SMEDDS)的处方最佳组成和比例;考察SMEDDS对姜黄素稳定性的影响。方法:用溶解性试验、初步筛选试验和伪三相图法进行姜黄素SMEDDS制备研究,通过评价自微乳化效果和乳滴粒径大小,绘制出姜黄素SMEDDS的成乳区域,优选处方的最佳组成和比例;采用HPLC-UV检测比较姜黄素提取物及其SMEDDS中姜黄素的含量变化。结果:姜黄素SMEDDS处方组成为中碳链甘三酯、聚氧乙烯蓖麻油、丙三醇时,能获得较好的自微乳化效果;光照、50℃和100℃加热各6 h,以及酸性条件下姜黄素及其SMEDDS稳定性良好。但pH>7时,姜黄素迅速分解,其SMEDDS稳定。结论:姜黄素SMEDDS的处方比例为碳链甘三酯4.2 g、聚氧乙烯蓖麻油1.8 g、丙三醇4.0 g时,姜黄素载量为200 mg,制得的姜黄素SMEDDS乳化效果良好,且在弱碱性条件下其稳定性大大提高。

Objective： To investigate the optimum formula of curcumin-loaded self-microemulsifying drug delivery system （SMEDDS） and evaluate the stability of curcumin. Method： Solubility test, screening test and a pseudo-ternary phase diagram were used to study the preparation of curcumin-loaded SMEDDS. The region and optimum formula of the SMEDDS were determined by the self-emulsifying degree and the particle size. The stability of curcumin in SMEDDS was evaluated based on the HPLC analysis. Result： The formula of the eurcumin SMEDDS was composed of Crodamol GTCC as the oil phase, Cremophor EL as the nonionie surfaetant and glycerol as the co-surfaetant, which could obtain the best emulsifying effect. Curcumin was stable under the conditions of strong light, 50℃ and 100℃ as well as pH value ≤7. In alkaline solution, curcumin was decomposed quickly, however eurcumin in the SMEDDS was still stable. Conclusion ： The proportion of Crodamol GTCC of 4.2 g, Cremophor EL of 1.8 g and glycerol of 4.0 g exists in the region of SMEDDS which could form a good self-emulsifying preparation. Moreover, SMEDDS could improve the stability of curcumin in alkaline solution with the drug loading of 200 mg.