正交设计优化川芎嗪乳酸-羟基乙酸共聚物微球处方与制备工艺

山东大学学报(医学版) ›› 2010, Vol. 48 ›› Issue (1): 154-158.

正交设计优化川芎嗪乳酸-羟基乙酸共聚物微球处方与制备工艺

石洋，李慧，徐淼，李岩，张娜，黄桂华

山东大学药学院，济南 250012

收稿日期:2009-06-30 出版日期:2010-01-16 发布日期:2010-01-16
通讯作者: 黄桂华，女，副教授，主要研究方向为药物新剂型的研究及新药开发
作者简介:石洋（1986- ），男，硕士研究生，主要从事药物新剂型研究。 E-mail：zidane-sy@yahoo.com.cn
基金资助:
山东省科技攻关资助课题（2007GG2NS02061）

Orthogonal experiments for optimizing the formulation and preparation conditions of tetramethylpyrazine loaded PLGA microspheres

SHI Yang, LI Hui, XU Miao, LI Yan, ZHANG Na, HUANG Guihua

School of Pharmaceutics, Shandong University, Jinan 250012, China

Received:2009-06-30 Online:2010-01-16 Published:2010-01-16

摘要/Abstract

摘要：

目的制备川芎嗪PLGA微球并考察其物理化学性质及体外释药性。方法采用O/W型乳化-溶剂挥发法制备川芎嗪PLGA微球，正交试验设计优化处方组成和制备工艺，对微球的外观形态、粒径及粒度分布、包封率和载药量等理化性质进行了检测。结果以优化处方制备的川芎嗪PLGA微球为圆球形，粒度分布较均匀，平均粒径为(10±2.2)μm，包封率为(81.36±1.15)%，载药量为(8.2±0.43)%，药物体外释放可延长至768?h，释药特性符合Weibull方程，经差示扫描量热法（DSC）分析证明，形成了新的物相，表明载药微球确已形成。结论采用O/W型乳化-溶剂挥发法制备的川芎嗪PLGA微球包封率和载药量高，粒径均匀，具有明显的缓释作用。

关键词: 川芎嗪；微球；乳酸-羟基乙酸共聚物；乳化-溶剂挥发法；正交设计

Abstract:

Objective To prepare tetramethylpyrazine (TMP) loaded PLGA microspheres. Methods TMP loaded PLGA microspheres were prepared by an O/W emulsion-solvent evaporation method. The formulation and the preparation conditions were optimized by orthogonal experiments using entrapment efficiency and drug loading as the composite evaluation index. The morphology was evaluated by an optical microscope. The particle size distribution was evaluated by Mastersizer 3000 (Malvern).The entrapment efficiency and the drug loading were assessed. Results The results showed that TMP loaded PLGA microspheres were concinnous and spherical in shape. The mean diameter was (10±2.2)μm. The average entrapment efficiency was (81.36±1.15)% and drug loading was (8.2±0.43)%. In vitro release of the TMP loaded PLGA microspheres sustained for 768 h and the release profile was depicted by Weibull kinetics. The formation of a new material phase was testified by analysis of differential scanning calorimetry (DSC). Conclusion TMP loaded PLGA microspheres with a highly encapsulation efficiency, drug loading, uniform size distribution and sustained release profile were prepared by an O/W emulsion-solvent evaporation method.

Key words: Tetramethylpyrazine； Microspheres； PLGA； Emulsion solvent evaporation method； Orthogonal experiments

中图分类号:

R944.9

石洋，李慧，徐淼，李岩，张娜，黄桂华. 正交设计优化川芎嗪乳酸-羟基乙酸共聚物微球处方与制备工艺[J]. 山东大学学报(医学版), 2010, 48(1): 154-158.

SHI Yang, LI Hui, XU Miao, LI Yan, ZHANG Na, HUANG Guihua. Orthogonal experiments for optimizing the formulation and preparation conditions of tetramethylpyrazine loaded PLGA microspheres[J]. JOURNAL OF SHANDONG UNIVERSITY (HEALTH SCIENCES), 2010, 48(1): 154-158.

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