盐酸纳曲酮多囊脂质体(DepoNTX)的制备及体内外评价  

Multivesicular Liposomes for Sustained Release of NaltrexoneHydrochloride(DepoNTX):Design,Characterization and in vitro/in vivo Evaluation

作　　者：孙丽君[1] 王涛[2] 全东琴[2] 冯端浩[1] 

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

出　　处：《中国医药导刊》2011年第8期1455-1457,共3页Chinese Journal of Medicinal Guide

摘　　要：目的:制备盐酸纳曲酮多囊脂质体(DepoNTX),并考察其理化性质和体内外释放行为。方法:采用复乳法制备盐酸纳曲酮多囊脂质体;RP-HPLC法测定含量、包封率和体内外释放特性;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: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40mM;初乳的体积和第二水相的体积比为1:2.5。粒径范围为(5～50)μm,平均粒径为12.4μm。盐酸纳曲酮在生理盐水中120h的累积释放度可达到(80～85)%,在血浆中较生理盐水释放快;大鼠皮下注射DepoNTX,与盐酸纳曲酮溶液相比,消除时间明显延长。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;体内外释放结果表明,DepoNTX具有明显的缓释效果。Objective：To prepare Naltrexone Hydmchloride Multivcsicular liposomes（DepoNTX）, and to study the physicochemicat properties and drug rcicasc behavior in vitro.Methods：DepoNTX wcre prepared using multiple cmulsion method. RP-HPLC was used to determine the concentration of Naltrexone, encapsulation efficiency and in vitro/in vivo release assay. The formulation and pharmaceutical process were optimized by orthogonal experimental design,with the encapsulation efficiency as the criteria. The multivesieutar liposomes particles were characterized by their morphologh which was observed using light microscope, the partical size and distribution was determined with coulter counter.Results：The optimal Rnmula was that： the concentration ralio was 1：1 of V.PC and CH,the vortex time was 10s, thc conccntration of L-lysine was 40raM, the volume rate of thc first emulsification and thc second aqueous solution is 1：2.5. The parlical size of DepoNTX were （5-50） μm,the mean partical size uas 12.4μm. Naltrcxone Hydrochloride was continuously released from MVL in 0.9%NaCL in vitro, and reachcd a maximum of 80% - 85% witnin 120h. I：oltowing intramuscular injection in rats, the elimination time was more prolonged after DepoNTX injection to solusion.Conclusion：DepoNTX was successfully encapsulated in this depot with good yield. Morphological examination using light microscope showed the smooth, multivcsieular particles. The capsnlation sfficieney is higher. The release profile shows that the drt;g is sustained-released.

关 键 词：纳曲酮 多囊脂质体 包封率 缓释 

分 类 号：R944[医药卫生—药剂学] TQ46[医药卫生—药学]