复乳法制备左布比卡因多囊泡脂质体及其体外特性表征  

Preparation and characterization in vitro of levobupivacaine multivesicular liposome using multiple emulsion method

作　　者：仝新勇 雷国峰 毛姝君 谭燕[2] 

机构地区：[1]上海恒瑞医药有限公司,上海200245 [2]上海市食品药品监督管理局科技情报研究所,上海200233

出　　处：《中国新药与临床杂志》2009年第9期683-687,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的复乳法制备左布比卡因多囊泡脂质体,并对其体外特性进行表征。方法采用复乳法制备左布比卡因多囊泡脂质体,以包封率和粒径为评价指标,对处方及工艺进行单因素考察,并对其在pH7.4的磷酸盐缓冲液(PBS)和人血浆中的体外释放进行表征。结果确定处方工艺为氢化磷脂20g·L-1,胆固醇30g·L-1,二棕榈酰磷脂酰甘油10g·L-1,三油酸甘油酯8g·L-1,外水相葡萄糖浓度为5%,有机溶剂为氯仿-乙醚(1∶1,V/V),乳化时间为6min,氮气流速6L.min-1制备脂质体,左布比卡因多囊泡脂质体呈典型的非同心囊泡结构,平均粒径22.38μm,在PBS中释放较慢,人血浆中释放较快,72h的累积释放量均可达到80%以上。结论左布比卡因多囊泡脂质体具有较为明显的体外缓释效果。AIM A multiple emulsion method was undertaken to prepare levobupivacaine muhivesicular liposome （Levo-B-MVL） and characterization in vitro was proceeded. METHODS Muhivesicular liposome containing levobupivacaine was prepared with multiple emulsion method. The formulation and preparation processes were sieved and optimized by single factors using encapsulation efficiency and particle size as the index. The releases of Levo-B-MVL in PBS with pH7.4 and human plasma in vitro were characterized. RESULTS The formulation and preparation processes were as follows： the Levo-B-MVL contained formulation of hydrogenated phosphatidyl choline （SPC） 20 g·L^-1, cholesterol （CH） 30 g·L^-1, 1, 2-dipalmitoyl-sn-glycero- 3-phospho-rac-glycerol （DPPG） 10 g·L^-1, triolein （TO） 8 g·L^-1 and 5% glucose in the external water phase and utilized organic solvent chloroform-ether （1 ： 1, V/V） with emulsification time 6 min and nitrogen flow rate 6 L·min^-1 The outcoming of Levo-B-MVL had typical non-concentric vesicle-like structure with average particle diameter of 22.38 μm and had a faster release in human plasma than in PBS, but with equal cumulative release volume up to 80% or higher at the time of 72 h. CONCLUSION Muhivesicular liposome containing levobupivacaine bears the characteristics of significant sustained release properties in vitro.

关 键 词：左布比卡因 脂质体 药物释放系统 复乳法 缓释 

分 类 号：R943[医药卫生—药剂学]