姜黄素自微乳化释药系统处方优化及体外评价

Formulation Optimization of Curcumin Self-Microemulsifying Drug Delivery System and Its in Vitro Evaluation

目的制备姜黄素自微乳化释药系统(Cur-SMEDDS),并考察其体外释药性能。方法测定姜黄素在各辅料中的溶解度,绘制伪三元相图筛选自微乳化基质,以粒径和溶解度为指标确定最佳处方,并对Cur-SMEDDS的体外释药性质进行研究。结果 Cur-SMEDDS最佳处方组成为:EO-Cremophor RH40-Transcutol P比例为30∶52.5∶17.5,乳化后微乳的平均粒径为36.14nm。结论成功制备了Cur-SMEDDS,可显著改善姜黄素的溶解度,有望提高姜黄素的口服生物利用度。

OBJECTIVE To prepare the curcumin self-microemulsifying drug delivery system （Cur-SMEDDS） and study its re- lease characteristics in vitro. METHODS The optimalum formulations of Cur-SMEDDS were screened by solubility experiment, and pseudo-ternary phase diagrams, with average particle size and solubility as parameters. The release curves of Cur-SMEDDS in different release mediuma were measured. RESULTS The optimumal formulation of Cur-SMEDDS was composed of Ethyl oleate/Cremophor RH40/Transcutol P with weight ratio of 30： 52. 5： 17.5. The average particle size of the microemulsion was 36. 14 nm. CONCLU- SION Cur-SMEDDS were prepared successfully and couldwith significantly increased curcumin the solubility of curcumin significant- ly, which is advantageous to improve oral bioavailability of curcumin.