低分子肝素前体脂质体制剂的研究  

STUDY ON THE PROLIPOSOMAL PREPARATION OF LOW MOLECULAR WEIGHT HEPARIN

作　　者：翟光喜[1] 赵焰[1] 

机构地区：[1]山东大学药学院药剂学教研室

出　　处：《山东医科大学学报》2001年第3期218-220,共3页Acta Academiae Medicinae Shandong

摘　　要：目的 :探讨用前体脂质体法制备LMWH脂质体制剂的影响因素及质量评定。方法 :以包封率为指标 ,用正交设计试验法研究由前体脂质体制成含药脂质体过程中的影响因素 ,并以包封率、形态、粒度分布评估了制剂的质量 ,以动物试验考察了制剂的缓释性。结果 :影响因素作用的大小顺序为 :甘露醇用量>类脂配比 >药物浓度 >十八胺用量 ,最佳工艺制剂包封率为 37 3% ,在电镜下为圆形或椭圆形 ,90 %颗粒粒径小于 1 2 μm ,动物试验表明 ,该制剂体内可维持 8h的药物作用。 结论 :前体脂质体法制备的脂质体制剂有较高的包封率。Objective:To study liposomal preparation of LMWH prepared by the way of proliposome.Methods:Using encapsulated ratio as the estimated parameter,the affecting factors in the course of drug liposomes preparation by proliposomes were investigated based on orthogonal design and the characteristics of the preparation such as encapsulated ratio,vesicle conformation and diameter distribution were evaluated.The drug controlled release was investigated in rabbits.Results:The effects of the amout of mannitol and the proportion of lipids on the preparation were superior to those of drug concentration and the amount of stearic amine.The encapsulated ratio was 37.3%,liposome vesicles were globular or elliptic under the electronic microscopy,and the diameters of 90% vesicles were between 0.4 and 1.2μm.The results of animal experiment showed that the liposomal LMWH could have a drug activity for 8h in rabbits.Conclusion:Liposomal preparations prepared by the way of proliposome have a high encapsulated ratio,a narrow diameter distribution and a well sustained release property.

关 键 词：前体脂质体 脂质体 低分子肝素 药物载体 

分 类 号：R944[医药卫生—药剂学]