华西口腔医学杂志

• 专栏论著 • 上一篇    下一篇

平阳霉素白蛋白微球的制备及其体外释药的实验研究

高庆红1,郑根建2,王昶光3,周 岚2,温玉明1,王昌美1,侯世祥3   

  1. 1.口腔生物医学工程教育部重点实验室,四川大学,四川 成都610041; 2.浙江省台州市中心医院 口腔科,浙江 台州318000;3.四川大学华西药学院 药剂研究室,四川 成都610041
  • 收稿日期:2005-02-25 修回日期:2005-02-25 出版日期:2005-02-20 发布日期:2005-02-20
  • 通讯作者: 温玉明,Tel: 028-85501440
  • 作者简介:高庆红(1967-),男,四川人,副主任医师,博士
  • 基金资助:
    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)

An Experimental Study on the Preparation and Drug Sustained Release Characteristics of Pingyangmycin Albumin Micro- spheres

GAO Qing-hong1,ZHENG Gen-jian2,WANG Chang-guang3,ZHOU Lan2,WEN Yu-ming1,WANG Chang-mei1, HOUShi-xiang3   

  1. 1.Key.Laboratory.ofOral Biomedical Engineering ofMinistry ofEducation,Sichuan University,Chengdu 610041,China; 2.Dept.ofStomatology,Taizhou Central Hospital,Taizhou318000,China; 3.Dept.ofPharmacy,West China College ofPharmacology,Sichuan University,Chengdu610041,China
  • Received:2005-02-25 Revised:2005-02-25 Online:2005-02-20 Published:2005-02-20

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。

关键词: 平阳霉素, 白蛋白微球, 缓释

Abstract:

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.

Key words: pingyangmycin, albumin microspheres, sustained-releasing