平阳霉素白蛋白微球的制备及其体外释药的实验研究
An Experimental Study on the Preparation and Drug Sustained Release Characteristics of Pingyangmycin Albumin Micro- spheres
作者：高庆红,郑根建,王昶光,周岚,温玉明,王昌美,侯世祥
Author：GAO Qing-hong1,ZHENG Gen-jian2,WANG Chang-guang3,ZHOU Lan2,WEN Yu-ming1,WANG Chang-mei1, HOUShi-xiang3
收稿日期：2005-02-25 年卷（期）页码：2005,23(01):69-
期刊名称：华西口腔医学杂志
Journal Name：West China Journal of Stomatology
关键字：平阳霉素,白蛋白微球,缓释,
Key words：pingyangmycin,albumin microspheres,sustained-releasing,
基金项目：四川省科技攻关资助项目(03SG022-101);浙江省台州市科委立项基金资助项目(022219)
中文摘要
目的 制备平阳霉素白蛋白微球(PYM-AMS),用于治疗动静脉血管畸形。方法 采用乳化热固化法,在 140℃制备出PYM-AMS,并考察其理化性质:通过超声测定强度,激光散射粒径分析仪测定粒径大小,紫外分光光度法测定载药率、包封率和体外模拟累积释放度。把制备好的PYM-AMS分装后,经60Co辐照灭菌。并通过放置于冰箱(3~5℃)、室温(15~25℃)和37℃,RH75%条件下放置3月,考察其稳定性。结果 制备的PYM-AMS平均粒径为139·422μm,56~251μm的微球约占总数的80%,载药率为26·47%,包封率为84·3%;5 h内药物快速释放,之后进入缓慢过程,24 h累积释放率为88·65%,t50为1·5 h;分装后,经60Co辐照灭菌;性质稳定,经5号、6号药典筛筛分后,可获得125~180μm的微球。结论 制备的PYM-AMS载药量高,具有缓释效果,能够达到治疗动静脉畸形的要求。
英文摘要
Objective The aim of this study was to prepare Pingyangmycin Albumin Microspheres (PYM-AMS) for arterio- venous malformations treatment.Methods PYM-AMS was prepared at 140℃by the method of emulsification-heat solidification and its characteristicswere evaluated, such as morphosis, particle size, drug loading (DL%), encapsulation efficiency (EE%), stability and drug sustained-releasingin vitro. After being packaged, PYM-AMS were sterilized with 13.7 kGy of60Co. Small samples of PYM-AMS were packaged in small bottles and stored at 3~5℃、15~25℃、37℃for 3 months, then checked the change of morphology、DL、EE and the release rate.Results The surface of particleswas smooth and integrated. The average di- ameter of PYM-AMS particles was 139.422μm and 80% was in the range of 56~251μm. The mean DL% and EE% were 26·47% and 84.3%, respectively. PYM released fast in 5 h, but then released slowly. 88.65% drugs were released in 24 h, and t50was 1.5 h. There was no obvious change of the morphology、DL、EE and the release rate of PYM-AMS stored at 3~5℃、 15~25℃、37℃for 3 months.Conclusion PYM-AMS prepared in this study had sustained-release effect, high drug loading and high stability. Albumin is a good carrier of PYM embolization agent.
上一条：HSV-tk与p53基因对涎腺多形性腺瘤细胞的杀伤作用
【关闭】
