槲皮素自乳化释药系统的制备和质量评价

目的：制备槲皮素自乳化制剂,并对其质量进行评价。方法：通过测定药物在不同油相中的溶解度,研究油相与各种乳化剂、助乳化剂的配伍对自微乳效率的影响,并结合伪三元相图,筛选槲皮素自乳化制剂的处方。考察该制剂经水稀释后形成微乳的形态、粒径和电势,测定药物的溶解度,并通过加速实验评价制剂的稳定性。结果：自乳化介质处方为油酸乙酯-Cremophor EL-正丁醇(10∶54∶36)；槲皮素自乳化制剂稀释50倍后在透射电镜下呈圆球型,分布均匀,粒径为(16.3±4.6) nm,ξ电位为(2.1±0.8) mV；药物在自乳化制剂中的溶解度为(62.42±0.11) mg·mL^-1,比水中溶解度增大2 229倍；加速实验表明槲皮素自乳化制剂的各质量指标稳定。结论：槲皮素自乳化制剂制备简便,质量稳定,能够显著提高药物的溶解度。

Preparation and quality evaluation of quercetin self-emulsifyied drug delivery systems

OBJECTIVE: To prepare the quercetin self-emulsified formulation and evaluate its quality. METHOD: The quercetin self-emulsified formulation was optimized based on the quercetin solubility in different oils, and the self-microemulsified efficiency of various combinations of emulsifier and co-emulsifier evaluated using the pseudo-ternary phase diagram. The microemulsion of morphology, size and zeta potential were examined. The quercetin of solubility in self-emulsified system was tested and the formulation stability was investigated by accelerated experiment. RESULT: The blank self-emulsified system was composed of ethyl oleate/Cremophor EUL/butanol with weight ratio of 10: 54: 36. After being dilutied with water, the morphology of microemulsion was homogeneous small spherical drops observed under the electro-microscopy. The particle size and the zeta potential were 16.3 +/- 4.6 nm and 2.1 +/- 0.8 mV, respectively. The solubility of quercetin in self-emulsifing system was (62.42 +/- 0.11) mg x mL(-1), increased 2 229 folds compared with that of in water. The quality of quercetin self-emulsified formulation was stable during the 3 months storage at 40 degrees C. CONCLUSION: The solubility of quercetin is significantly increased in self-emulsified system and the formulation is stable and easy to prepare.