星点设计-效应面法优化异长春花碱脂质体的处方Optimized formulation of vinorelbine liposomes by a central composite design-response surface methodology
李学涛,程岚,贾天柱,唐凌
LI Xue-tao1,CHENG Lan1,JIA Tian-zhu1,TANG Ling2 (1.School of Pharmacy
摘要(Abstract):
目的采用星点设计-效应面法优化异长春花碱脂质体的处方。方法以磷脂/药(质量比)、胆固醇/磷脂(摩尔比)、水化温度为考察因素,以脂质体的包封率和脂质体的平均粒径为指标,采用二次多项式方程描述考察指标和影响因素之间的数学关系,根据此数学模型描绘效应面,选择最佳处方,并进行预测分析。结果所建立的考察指标和影响因素之间的数学模型具有较高的可信度。以优化后的处方制备样品,各指标实测值与预测值偏差较小。结论所建立的模型预测性良好,制备的脂质体符合设计要求。
Objective To optimize the formulations of vinorelbine liposome by a central composite design/response surface methodology.Methods The effects of three independent variables,cholesterol/VRB,phospholipids/cholesterol,and the temperature of the hydration were investigated with the parameter of the entrapment efficiency and mean particle size.Nonlinear mathematic models were used to estimate the relationship between independent and the dependent variables.Response surfaces were delineated according to the mathematic models,and optimum formulation was selected.Results The vinorelbine liposome was prepared according to the optimal experimental condition and evaluated for entrapment efficiency and mean particle size.The observed values agreed well with model predicted values.Conclusions It shows that the optimum mathematic model is highly predictive.
关键词(KeyWords):
异长春花碱;星点设计;效应面;脂质体
vinorelbine;central composite design;response surface methodology;liposome
基金项目(Foundation):
作者(Author):
李学涛,程岚,贾天柱,唐凌
LI Xue-tao1,CHENG Lan1,JIA Tian-zhu1,TANG Ling2 (1.School of Pharmacy
DOI: 10.14066/j.cnki.cn21-1349/r.2010.08.017
参考文献(References):
- [1]MILLER VA,KRUG LM.Phase I trial of docetaxel andvinorelbine in patients with advanced non small cell lungcarcinoma[J].Cancer,2000,88(5):1045.
- [2]祖元刚,罗猛.长春花生物碱成分及其药理作用研究进展[J].天然产物研究与开发,2006,18:325-329.
- [3]吴伟,崔光华.星点设计-效应面优化法及其在药学中的应用[J].国外医学药学分册,2000,27(5):292-298.
- [4]宋力,范文源.优福定脂质体的处方与工艺优化[J].中国药房,2007,18(19):1479-1481.
- [5]何军,奉建芳,庞家忠,等.星点设计-效应面法优化水飞蓟素固体脂质纳米粒的制备[J].中国医药工业杂志,2005,36(1):18-21.