中国组织工程研究

中国组织工程研究 ›› 2011, Vol. 15 ›› Issue (51): 9608-9612.doi: 10.3969/j.issn.1673-8225.2011.51.025

• 药物控释材料 drug delivery materials • 上一篇    下一篇

利福平/聚乳酸-聚羟基乙酸缓释微球的制备及特性

叶向阳1，孙  湘2，贾会文3，汤立新1，赵玉果1，甄  平4   

  1. 1南阳市中心医院骨一科，河南省南阳市  473000
    2河南省淅川县人民医院输血科，河南省淅川县  474450
    3南阳市中心医院急救中心，河南省南阳市  473000
    4解放军兰州军区兰州总医院全军骨科中心，甘肃省兰州市  730050
  • 收稿日期:2011-03-11 修回日期:2011-04-27 出版日期:2011-12-17 发布日期:2011-12-17
  • 通讯作者: 甄平，主任医师，教授，博士，硕士生导师，解放军兰州军区兰州总医院全军骨科中心，甘肃省兰州市 730050 zhenpingok@163.com
  • 作者简介:叶向阳★，男，1978年生，河南省南阳市人，汉族，硕士，主治医师，主要从事骨结核治疗与骨组织工程修复材料的研究。 yexyang2008@163.com

Preparation and characterization of rifampicin-loaded poly(lactic-co-glycolic acid)  microspheres

Ye Xiang-yang1, Sun Xiang2, Jia Hui-wen3, Tang Li-xin1, Zhao Yu-guo1, Zhen Ping4   

  1. 1First Department of Orthopedics, Nanyang Central Hospital, Nanyang  473000, Henan Province, China
    2Department of Blood Transfusion, Xichuan Country People’s Hospital, Xichuan  474450, Henan Province, China
    3Emergency Department, Nanyang Central Hospital, Nanyang  473000, Henan Province, China
    4Department of Orthopedics, Lanzhou General Hospital of Lanzhou Military Area Command of Chinese PLA, Lanzhou  730050, Gansu Province, China
  • Received:2011-03-11 Revised:2011-04-27 Online:2011-12-17 Published:2011-12-17
  • Contact: Zhen Ping, Doctor, Chief physician, Professor, Master’s supervisor, Department of Orthopedics, Lanzhou General Hospital of Lanzhou Military Area Command of Chinese PLA, Lanzhou 730050, Gansu Province, China zhenpingok@163.com
  • About author:Ye Xiang-yang★, Master, Attending physician, First Department of Orthopaedics, Nanyang Central Hospital, Nanyang 473000, Henan Province，China yexyang2008@163.com

PDF

554

被引次数

29

摘要：

背景：虽然国内外有很多制备利福平/聚乳酸-聚羟基乙酸共聚物(poly lactic acid-glycolic acid copolymer，PLGA)微球的报道，但这些微球粒径多在10 μm左右，不适合与磷酸钙骨水泥复合制备成具有良好降解性的抗结核修复材料。
目的：制备大粒径利福平/PLGA缓释微球，观察其理化特性和体外缓释特性。
方法：以PLGA为载体，将利福平分散于PLGA的有机溶剂中，采用复乳溶剂挥发法制备利福平/ PLGA缓释微球。光镜和扫描电镜下观察微球的形态特征，测定微球平均直径和跨距，高效液相色谱法测定载药量和包封率，以溶出法和高效液相色谱法观察其体外释药特性，并拟合药物体外释放曲线建立曲线方程。
结果与结论：利福平/PLGA微球电镜观察呈圆球形，分散性好，粘连少，粒径分布集中，平均粒径(80.0±9.4) μm。载药量、包封率分别为(33.18±1.36)%，(54.79±1.13)%。体外缓释试验显示突释期内微球释放度为(14.66±0.18)%，前3 d累计释放度(18.09±0.45)%，到42 d体外累积释放度达到(92.17±1.23)%。提示利福平/PLGA微球具有良好的缓释效果，是一种较为理想的抗结核药物的载体材料和释放系统；PLGA是良好的药物缓释载体，可以用来制备载药缓释微球。

关键词: 聚乳酸-聚羟基乙酸, 利福平, 药物载体, 微球, 缓释, 骨缺损

Abstract:

BACKGROUND: Some scholars prepared rifampicin-loaded poly (lactic-co-glycolic acid) (PLGA) microspheres with diameter of 10μm which was not suitable to be combined with calcium phosphate cement to prepare repair materials with good degradation.
OBJECTIVE: To conduct the preparation of rifampicin-loaded PLGA microspheres with large size and to study the physicochemical characteristics of the microspheres and the characteristics of drug release in vitro.
METHODS: Rifampicin-loaded microspheres of biodegradable PLGA were prepared using a double-emulsion solvent-extraction [(water-in-oil)-in-water] technique. The morphology of the microspheres was observed by scanning electron microscope and light microscope. Their average diameter and the span were measured. Their envelopment rate and drug-carried rate were determined by high performance liquid chromatography. Their release characteristics were studied in vitro by dissolution method. The curve of drug release in vitro was fitted and the equation of the curve was established.
RESULTS AND CONCLUSION: Rifampicin-loaded PLGA microspheres presented complete globe, good dispersibility and no obviously aggregation. Their average diameter was (80.0±9.4) μm, drug-carried rate was (33.18±1.36)% and envelopment rate was (54.79±1.13)%. In vitro release property of the microspheres was good. In the burst release phase, the rate of drug release in vitro was (14.66±0.18)%, and rose to (18.09±0.45)% and (92.17±1.23)% 3 and 42 days later. Rifampicin-loaded PLGA microspheres have the characteristics of slowing antituberculosis drugs releasing.

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