单纯形网格法优化设计高良姜素自微乳处方

Optimization Design of Galangin Self⁃emulsion Prescription by Simplex Lattice Method

目的:采用单纯形网格法(SLD)优化设计高良姜素(Gal)自微乳(SMEDDS)处方,并对其进行质量评价。方法:通过溶解度试验、处方配伍试验及三元相图筛选辅料种类及用量;采用SLD优选Gal⁃SMEDDS处方;对制备的Gal⁃SMEDDS进行形态、体外释放度等质量评价。结果:Gal⁃SMEDDS最优处方W(油酸乙酯)∶W(氢化蓖麻油CO 40)∶W(PEG⁃400)=10%∶60%∶30%,载药量(21.15±0.32)mg/g。制剂透射电镜下形态均匀且圆整,各项指标结果:平均粒径(21.33±0.62)nm,PDI(0.096±0.003),包封率(96.74±0.25)%,去离子水、人工肠液及人工胃液中24 h内累积释放度分别为(87.31±2.52)%、(84.14±3.10)%、(79.37±2.49)%。结论:Gal⁃SMEDDS可明显改善Gal的溶解度、溶出度,且理化性质良好。

Objective:To optimize the formulation of Galangin(Gal)self⁃microemulsion(SMEDDS)by simplex lattice design meth⁃od(SLD)and evaluate its quality.Methods:The types and dosage of excipients were selected by solubility test,prescription compatibility test and ternary phase diagram.The formulation of Gal⁃SMEDDS was optimized by SLD.The morphology,in vitro release and other char⁃acteristics of the Gal⁃SMEDDS were evaluated.Results:The optimal formulation of Gal⁃SMEDDS was W(ethyl oleate)∶W(cremophor CO 40)∶W(PEG⁃400)=10%∶60%∶30%,the drug loading capacity was(21.15±0.32)mg/g.The morphology of Gal⁃SMEDDS was uni⁃form and round under the transmission electron microscope,the average particle size was(21.33±0.62)nm,the PDI was(0.096±0.003),the entrapment efficiency was(96.74±0.25)%.The cumulative releases of Gal⁃SMEDDS in distilled water,artificial intestinal fluid and artificial gastric fluid were(87.31±2.52)%,(84.14±3.10)%and(79.37±2.49)%within 24 hours,respectively.Conclusion:Gal⁃SMEDDS can significantly improve the solubility,dissolution of Gal,its physical and chemical properties are good.