盐酸伊立替康纳米粒的制备及体外评价  

Preparation and in vitro evaluation of nanoparticles of irinotecan hydrochloride

作　　者：杨付英[1] 陈和莉[1] 张文萍[1,2] 王欣瑜[1,2] 党宏万[1,2] 

机构地区：[1]宁夏医科大学,宁夏银川750004 [2]宁夏医科大学总医院临床药理研究室,宁夏银川750004

出　　处：《中国医院药学杂志》2012年第21期1723-1726,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备盐酸伊立替康纳米粒,并对其纳米粒形态、粒径、包封率和释放进行评价。方法:采用沉淀法制备盐酸伊立替康纳米粒,以包封率作为考察指标,筛选最优处方。用透射电镜观察纳米粒形态,激光粒径测定仪测定粒径,凝胶过滤法测定药物的包封率,透析法考察体外释药特质。结果:盐酸伊立替康纳米粒形态规整,几呈球形,强度径为(193.5±2.5)nm,载药量为26.35%,包封率为(98.00±0.01)%,体外24h的累积释放率为62.09%,比水溶液释放慢。结论:通过优化处方和工艺,制备出的盐酸伊立替康纳米粒粒径均匀,包封率较高,体外释药具有缓释特点。OBJECTIVE To prepare nanoparticles of irinotecan hydrochloride（CPT-11 NPS）and to evaluate their particle size,morphology,encapsulation efficiency and release characteristics.METHODS CPT-11 NPS were prepared by precipitation.The encapsulated ratio was used as an estimated parameter in order to select one of the most appropriate formulations The morphology of CPT-11 NPS was characterized by transmission electron microscopy.The particle size was measured by laser granularity analyzer.The encapsulation efficiency was determined by Sephadex G-50 gel chromatography.Dialysis was applied to investigate the release of CPT-11 NPS.RESULTS The prepared CPT-11 NPS were spherical with intensity diameter of（193.5±2.5） nm.The drug loading capacity and encapsulation efficiency were 26.35% and（98±0.01）%,respectively.The cumulative release amount reached 62.09% of CPT-11 NPS during 24 h,and CPT-11 NPS released CPT-11much more slowly compared with aqueous irinotecan hydrochloride solution.CONCLUSION The particle size of the CPT-11 NPS prepared by the use of this optimized formulation is uniform,the encapsulation efficiency is high and CPT-11 NPS have extended-release features.

关 键 词：盐酸伊立替康 纳米粒 沉淀法 包封率 体外释药 

分 类 号：R943[医药卫生—药剂学]