胸腺五肽缓释微球的制备及其质量评价.PDFVIP

胸腺五肽缓释微球的制备及其质量评价 李洪(广州健心药业有限公司，广州 510663) 摘要：目的 确立胸腺五肽(TP-5)微球的制备及质量评价方法。方法 以聚乳酸-羟基乙酸(PLGA)为载体材料，采用复乳法 (w/o/w)制备 TP-5 长效缓释注射微球，考察其粒径大小、外观、包封率等理化性质；采用 HPLC 测定微球中 TP-5 的含量。 结果 TP-5 微球球形圆整，包封率在 80%以上，平均粒径为 67.8 m ，27 d 体外累积释放百分率在 80%以上。结论 TP-5 微球的制备工艺合理，评价方法简便、快速、准确。 关键词：胸腺五肽；缓释微球；质量评价 中图分类号：R943.3; R943.41 文献标志码：A 文章编号：1007-7693(2009)07-0582-03 Preparation and Quality Evaluation of the Thymopentin Sustained Release Microspheres LI Hong (Guangzhou Jianxin Pharmaceutical Group Co.,Ltd, Guangzhou 510663, China) ABSTRACT: OBJECTIVE To establish the process of preparation and the quality evaluation method of thethymopentin microspheres (TP-5). METHODS TP-5 loaded microspheres were prepared with poly (lactic-co-glyeolic acid) (PLGA) as carrier material by double emulsion(w/o/w) ，to investigate the size, outside appearance and drug entrapment efficiency of the microspheres. HPLC method was used to determine the content of the TP-5 microspheres. RESULTS Microspheres with good shape were prepared by this method ．The drug entrapment efficiency was more than 80%. Mean particle size was 67.8 m. Under the release condition in vitro, cumulative drug release of microspheres was above 80% within 27 d. CONCLUSION The process of preparation of TP-5 microspheres is reasonable ．The evaluation method is simple，rapid ，accurate and suitable for the quality control of TP-5 microspheres. KEY WORDS: thymopentin; sustained release microspheres; quality evaluation 作者简介：李洪，女，工程师 Tel: (020E-mail: LiHong262@ ·582 · Chin JMAP,2009 July,Vol.26 No.7 中国现代应用药学杂志 2009 年 7 月第 26 卷第 7 期 胸腺五肽(thymopentin, TP-5)[1]是一种人工合成 元泵、在线脱气机、柱温箱、自动进样器、二极管 的促胸腺生成素，在 1979 年首次合成，TP-5 是具 阵列检测器、工作站) 。 有生物学活性最小的分子片段。TP-5 作用很多，如 2 方法和结果 影响神经肌肉的传递、区别于 T 细胞的诱导作用和