盐酸帕洛诺司琼PLGA缓释微球的制备与研究  

Preparation and Evaluation of Palonosetron Hydrochloride Loaded PLGA Sustained-release Microspheres

作　　者：苏莉莉 林霞 王艺澄 杨子毅 金坚 SU Li-li;LIN Xia;WANG Yi-cheng;YANG Zi-yi;JIN Jian(School ofPharmaceutical Science,Jiangnan University,Jiangsu Wuxi 214122,China)

机构地区：[1]江南大学药学院

出　　处：《广州化工》2019年第12期47-50,共4页GuangZhou Chemical Industry

基　　金：国家自然科学基金(81603060);江苏高校品牌专业建设工程项(PPZY2015B146)

摘　　要：为了降低盐酸帕洛诺司琼给药频率,提高对延迟性化疗相关性恶心呕吐(CINV)的缓解作用,本研究以聚乳酸-羟基乙酸共聚物(PLGA)为载体,制备盐酸帕洛诺司琼PLGA缓释微球(Pal-MS),并对其体外释药特性进行评价。结果表明,外水相pH值和药物/PLGA质量比可显著影响Pal-MS包封率和药物释放。当外水相pH为7.0,药物/PLGA质量比为1:39时,Pal-MS包封率高达82.75%,体外7d内呈现零级释药特征(y=0.1163x-0.0006,R^2=0.9944),有望制备出可在体内缓释一周的制剂。To reduce the administration frequency of palonosetron hydrochloride (Pal ) and improve the efficacy in preventing delayed chemotherapy induced nausea and vomiting (CINV ),a palonosetron hydrochloride loaded PLGA sustained-release microspheres (Pal-MS ) was designed using poly (lactic-co-glycolic acid )(PLGA ). The in vitro drug release of Pal-MS was also evaluated. The study showed that the pH of the external aqueous phase and the ratio of Pal to PLGA could significantly affect the encapsulation efficiency and the drug release behavior of Pal-MS. By adjusting the pH of the external aqueous phase to 7.0 and reducing the weight ratio of drug to PLGA from 1 : 10 to 1 : 39,the encapsulation efficiency of Pal-MS was increased from 23.94% to 82.75%. The drug was released from Pal-MS nearly at a constant rate,which was well fitted to the zero-order model (y=0.1163x-0.0006,R ^2=0.9944 ),it was expected to prepare a formulation that could be sustained for one week.

关 键 词：盐酸帕洛诺司琼 化疗相关性恶性呕吐(CINV) PLGA缓释微球 

分 类 号：R943.42[医药卫生—药剂学] R979.1[医药卫生—药学]