目的确定甘草次酸修饰马钱子碱脂质体(CPGL)的最佳处方。方法在单因素考察的基础上确定影响脂质体处方的因素,采用中心复合设计试验对处方进行优化,考察磷脂胆固醇比、磷脂药物比及磷脂修饰材料比对评价的影响。结果优选的最佳处方为胆固醇用量为20mg、投药量用量为1.6mg/mL、修饰材料用量为3.4mg,包封率为86.82%,粒径为147.2nm,累积释放度为51.43%。结论中心复合设计优化处方预测性良好,可以快速准确的优化CPGL处方。
OBJECTIVE To determine the optimal formulation of brucine liposome modified by glycyrrhetinic acid(CPGL).METHODS Based on single factor review,the critical factors which influence the preparation of the modified liposomes were evaluated.Central composite design was applied to screen its formulations.Independent variables were ratios of phospholipids and cholesterol,drugs,and glycyrrhetinic acid.RESULTS The optimal formulation was as follow: 20mg cholesterol,1.6 mg/mL drug,3.4 mg glycyrrhetinic acid.The encapsulation rate and particle size were 86.82% and 147.2 nm respectively with the accumulated released rate of 51.43%.CONCLUSION Central compound design,which is of great prediction can successfully optimize the formulation of CPGL.