槲皮素自微乳制剂的制备

Preparation of self-microemulsifying drug delivery system for quercetin

目的利用星点设计-效应面法优化处方,制备槲皮素自微乳制剂。方法通过溶解度考察、相稳定性评价、伪三元相图绘制筛选槲皮素自微乳制剂的处方组成。以乳化剂与助乳化剂的比值和油相百分含量为考察因素,以溶解度、微乳粒径为评价指标进行处方优化。评价最优处方制剂稀释后的粒径、Zeta电位。结果制剂处方为油酸聚乙二醇甘油酯-聚氧乙烯35蓖麻油-二乙二醇单乙基醚,三者比例为27.0∶55.6∶17.4(w∶w∶w)时乳化迅速,溶解度为67.87 mg/g,用水稀释50倍后平均粒径为25.26 nm,Zeta电位为-6.73 m V。结论星点设计-效应面法达到了优化处方的目的,制备的槲皮素自微乳制剂质量稳定。

Objective To optimize the prescription of self-microemulsifying drug delivery system for quercetin（ QTSMEDDS） by central composite design-response surface method and prepare QT-SMEDDS. Methods Components of prescription was screened by measuring the solubility of quercetin in different secondary solvents,investigating the phase instability and plotting pseudo-ternary phase diagram. According to the balanced solubility and particle size of quercetin in different self-microemulsifying drug prescriptions,the optimal prescription was determined using central composite design-response surface methodology. The particle size and Zeta-potential were investigated in detail. Results The optimal prescription of quercetin in SMEEDS was composed of Labrafil M1944CS（ oil）,Cremophor EL（ surfactant）,and Transcutol HP（ co-surfactant）,with a weight ratio of 27. 0% ∶ 55. 6% ∶ 17. 4%. The balanced solubility was67. 87 mg / g,the average particle size diluted 50 times with water was 25. 26 nm,and Zeta-potential was- 6. 73 m V.Conclusion The optimized prescription of QT-SMEDDS is obtained and its quality is stable.