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雌二醇生物可降解缓释微球的制备四氢呋喃的加入对微球性质的影响

周新腾*, 朱峰, 潘卫三, 张汝华   

  1. 1.沈阳药科大学药剂教研室, 沈阳 110016;
    2.北京博泰康宁医药有限公司, 北京 100054
  • 收稿日期:2002-10-11 修回日期:2003-02-10 出版日期:2003-03-15 发布日期:2003-03-15
  • 通讯作者: 周新腾*

Preparation of PLA or PLGA Microspheres with Estradiol the Effects of THF-adding on the Properties of MS

ZHOU Xin-teng*, ZHU Feng, PAN Wei-san, ZHANG Ru-hua   

  1. 1.Shenyang Pharmaceutical University, Shenyang 110016, China;
    2.Beijing Botaikangni Medical Co.,Ltd., Beijing 100054, China
  • Received:2002-10-11 Revised:2003-02-10 Online:2003-03-15 Published:2003-03-15
  • Contact: ZHOU Xin-teng*

摘要: 目的 在本实验中, 以生物可降解和生物相容性良好的聚乳酸(PLA)或乳酸-乙醇酸共聚物(PLGA)为载体材料制备含有雌二醇药物的缓释微球, 考察在制备过程中水溶性更强的四氢呋喃的加入对微球性质的影响。方法 以乙酸乙酯和四氢呋喃为有机溶剂、采用乳化-溶剂萃取法制备含药微球, 分别从成球性、粒径、包封率和体外释药等方面, 进行制备工艺研究以及微球相关性质的研究。结果 在乙酸乙酯中加入四氢呋喃, 使包封率降低, 但在乙酸乙酯体积比大于50%, 增加四氢呋喃的用量对包封率无明显影响。相同条件下, 在考察范围内, 粒径随四氢呋喃用量比例的增大而增大, 而载体的性质和微球含药量是影响微球释药的主要因素。结论 尽管在制备过程中的油相中加入了水溶性更强的四氢呋喃, 但是通过控制制备工艺和条件, 仍然可以得到球形态好、有适当粒径分布范围、载药量高并且突释程度小的雌二醇生物可降解缓释微球。

关键词: 聚乳酸, 乳酸-乙醇酸共聚物, 雌二醇, 微球, 四氢呋喃, 乳化-溶剂萃取法

Abstract: Aim Polylactic acid (PLA) or polylactide co glycolide (PLGA) was used as biodegradable and biocompatible carriers to achieve sustained release of estradial PLGA/PLA Microspheres (E2 PLGA/PLA MS). THF was added in the organic phase to study its effects on the properties of MS. Methods MS were formed by an emulsification solvent extraction method with mixture of ethyl acetate (EtoAc) and tetrahydrofuran (THF) as the organic solvents, and then the properties and in vitro drug release behavior were examined. Results The results indicated that the drug loading efficiency decreased when THF added, but when the ratio of EtoAc was more than 50%, there was no obvious effect of THF ratio, but the particle size increased accordingly. The carriers' properties and the drug contents were the main factors influencing the in vitro drug release. Conclusions By controlling the technology and formulation, we can get sustained release E2 biodegradable microsperes with proper particle size, drug content and low burst release, although THF with readily solubility in water was used in the organic phase.

Key words: PLA/PLGA, PLA/PLGA, estradiol, estradiol, microspheres, microspheres, THF, THF, emulsification solvent extraction method, emulsification solvent extraction method

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