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期 刊 ：中国中药杂志 2007年 32卷 09期 页码：805.

关键词：槲皮素；自乳化；质量评价；伪三元相图；

Keywords:quercetin, self-emulsified, quality evaluation, pseudo-ternary phase diagram,

摘 要 ：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。

Abstract: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 EL/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·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 ℃. Conclusion: The solubility of quercetin is significantly increased in self-emulsified system and the formulation is stable and easy to prepare.

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