摘要
目的以喷雾干燥法制备卡莫司汀（carmustine，BCNU）-聚乳酸缓释微球，研究工艺条件对微球形态及药物释放的影响方法将BCNU、聚乳酸溶解于丙酮、氯仿或乙酸乙酯溶液中，控制不同溶液浓度、进口温度，以扫描电子显微镜观察微球形貌，以^1H—NMR分析了不同温度奈件对BCNU稳定性的影响，以分光光度法测定微球载药率，并研究BCNU的缓释特性。结果以丙酮为溶剂难以得到球形颗粒，不规则形态使其药物释速率较快，突释明显、以氯仿或乙酸乙酯为溶剂则可得到较好的球形颗粒，BCNU释放突释放较小，释放较平缓、在操作条件下BCNU均具有较好的稳定性，包载率可达14％～42％、结论喷雾干燥法可以得到高BCNU包载率的聚乳酸缓释微球，以乙酸乙酯为溶剂时效果最佳。
OBJECTIVE To prepare earmustine（ BCNU）-loaded polylactie acid mierospheres by spray dU method, and to study the effect of the process technologic on the morphology and drug release behavior. METHODS BCNU and polylaetie acid were codissolved in acetone, chloroform or ethyl acetate, and then submitted to spray dry. The morphologies of mierosphere obtained under different process condition, such as polymer coneentration and inlet temperature of spray drier, were observed by TEM. The stability of BCNU after the spray drying was studied using ^1H-NMR analysis, and the drug release behavior was investigated through speetrophotometer. RESULTS BCNU-loaded polylaetic acid mierospheres were prepared using chloroform or ethyl acetate as solvent, while the particles with irregular shape were obtained with acetone as solvent, resulting in the fast release rate of the BCNU from these microshperes. The drug-loading was ranged from 14% -42%. CONCLUSION BCNU-loaded polylaetie acid mireopsheres ean be prepared using spray dry technique with ethyl aeetate as solvent.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2008年第21期1638-1642,共5页
Chinese Pharmaceutical Journal
基金
天津市科技攻关项目(06YFGZSH00800)
