胸腺五肽缓释微球的制备及其质量评价

Preparation and Quality Evaluation of the Thymopentin Sustained Release Microspheres

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67.8μm,27d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。

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 μm. 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.