盐酸纳曲酮多囊脂质体的处方及制备工艺研究  

Formulation and preparation technology of naltrexone hydrochloride multivesicular liposomes

作　　者：孙丽君[1] 王涛[1] 全东琴[1] 冯端浩[2] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]解放军309医院药剂科,北京100091

出　　处：《中国药物应用与监测》2010年第6期338-341,共4页Chinese Journal of Drug Application and Monitoring

摘　　要：目的:制备盐酸纳曲酮多囊脂质体(DepoNTX),并考察其理化性质。方法:采用复乳法制备DepoNTX;RP-HPLC法测定含量、包封率;以包封率为指标,单因素及正交试验筛选、优化工艺和处方;光学显微镜下观察多囊脂质体形态、用库尔特计数仪测定其粒径和粒度分布。结果:制备的最佳条件是卵磷脂/胆固醇为1:1(摩尔比),形成复乳的振荡时间为10s,L-赖氨酸的浓度为40mmol·L-1,初乳和第二水相的体积比为1:2.5。粒径范围为5～50μm,平均粒径为12.4μm,包封率为44.5%。结论:制备的DepoNTX包封率较高,粒子表面呈光滑球形,内部具有非同心的多囊泡结构。Objective：To prepare the naltrexone hydrochloride multivesicular liposomes（DepoNTX）,and study its physicochemical properties.Methods：DepoNTX were prepared using multiple emulsion method.RP-HPLC was used to determine the concentration of naltrexone and encapsulation efficiency.The formulation and pharmaceutical process were optimized by single factor design and orthogonal experimental design with the encapsulation efficiency as the criteria.The multivesicular liposomes particles were characterized by their morphology which was observed using light microscope,the particle size and distribution were determined by coulter counter.Results：The optimal formula was as follows：the mole ratio of phosphatidylcholine to cholesterol was 1：1,the vortex time for emulsion polymerization was 10 s,the concentration of L-lysine was 40 mmol·L-1,the volume ratio of the first emulsification to the second aqueous phase solution was 1：2.5.The particle sizes of DepoNTX were 5-50 μm with the mean particle size of 12.4 μm,the encapsulation efficiency of DepoNTX was 44.5%.Conclusion：DepoNTX was successfully encapsulated in this depot with high yield,and showed spherical shape with the non-concentric multivesicular aqueous compartment.

关 键 词：纳曲酮 多囊脂质体 包封率 制备工艺 

分 类 号：R944[医药卫生—药剂学]