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目的:优化吴茱萸碱脂质体的处方。方法:采用薄膜分散法制备脂质体,并采用星点设计-效应面法以包封率为考察指标,对大豆卵磷脂与药物质量比、大豆卵磷脂与胆固醇质量比、大豆卵磷脂浓度进行二项式拟合,通过三维效应面图和等高线选择最佳处方,对预测结果进行验证,并观察其外观、粒径及p H。结果:最佳处方为大豆卵磷脂与药物质量比30.58∶1,大豆卵磷脂与胆固醇的质量比15.22∶1,大豆卵磷脂浓度为42.26 mg·ml~(-1),制得吴茱萸碱脂质体的平均包封率为92.89%。吴茱萸碱脂质体外观为乳白色半透明,呈圆球形或椭圆形的球粒,粒径为126 nm,p H为6.94±0.17。结论:采用该处方工艺制备吴茱萸碱脂质体稳定、可行。
Objective: To optimize the formulation of evodiamine liposomes. Methods: The liposomes were prepared by the method of film dispersion. The encapsulation efficiency of the liposomes was determined by the method of star spot design-response surface method. The mass ratio of soybean lecithin to drug, the ratio of soybean lecithin to cholesterol and the concentration of soybean lecithin Binomial fitting, through the three-dimensional effect of surface maps and contour to select the best prescription, the prediction results to verify and observe the appearance, particle size and pH. Results: The best prescription was the mass ratio of soybean lecithin to drug 30.58:1, the mass ratio of soybean lecithin to cholesterol 15.22:1, the concentration of soybean lecithin 42.26 mg · ml -1, the evodiamine lipid The average entrapment efficiency of the body was 92.89%. The evodiamine liposomes were opalescent and translucent with spherical or oval spherical particles with particle size of 126 nm and p H of 6.94 ± 0.17. Conclusion: The preparation of evodiamine liposomes by this prescription is stable and feasible.