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目的:制备葛根素混合胶束,以增加葛根素在水中的溶解度。方法:以去氧胆酸钠和卵磷脂为辅料,采用正交试验制备混合胶束。以混合胶束的溶解度、形态、粒径等为指标,筛选葛根素混合胶束的最佳制备工艺。结果:优选出的最佳制备工艺为摩尔比3∶2∶4的葛根素、卵磷脂及去氧胆酸钠,溶于甲醇-氯仿(1∶1)中,30℃旋转蒸发至干。最佳工艺所得混合胶束粒径为(64.8±13)nm(体积径);溶解度为0.811 1 g.L-1,是葛根素原料溶解度(0.0364 g.L-1)的22.3倍。结论:胆盐/磷脂混合胶束制备技术能显著提高葛根素的溶解度。
Objective: To prepare puerarin mixed micelles to increase the solubility of puerarin in water. Methods: Using sodium deoxycholate and lecithin as excipients, the mixed micelles were prepared by orthogonal test. According to the solubility, morphology and particle size of the mixed micelles, the optimal preparation process of puerarin mixed micelles was screened. Results: The optimal preparation process was puerarin, lecithin and sodium deoxycholate with molar ratio 3: 2: 4, dissolved in methanol-chloroform (1: 1) and rotary evaporated to dryness at 30 ℃. The average particle size of the mixed micelles obtained by the best technique was (64.8 ± 13) nm (volume diameter) and the solubility was 0.811 1 g.L-1, which was 22.3 times of the solubility of puerarin raw material (0.0364 g.L-1). Conclusion: The bile salt / phospholipid mixed micelles preparation technology can significantly improve the solubility of puerarin.