关节腔注射用雷公藤甲素微球的制备与毒性评价(1)

http://www.100md.com 2016年10月25日 《中国当代医药》2016年第30期

     [摘要]目的 评价关节腔注射用雷公藤甲素微球的质量和毒性。方法 采用乳化溶剂挥发法制备雷公藤甲素微球，透射电镜观察微球表面形态和大小，红外光谱仪考察微球形成情况，马尔文粒度仪测定微球粒度分布，HPLC测定包封率、载药量，数学模型拟合微球体外释放规律，血液学参数和生化指标评价微球毒性。结果 微球形态圆整，大小均一，平均粒径、包封率和载药量分别为4.75 μm、(74.37±2.30)%、(1.53±0.27)%，微球释放更符合Ritger-Peppas方程，与空白对照组相比，各项血液学参数和生化指标未发生明显改变。结论 雷公藤甲素微球可以作为关节腔注射用缓释制剂的新型制剂。

    [关键词]雷公藤甲素；微球；毒性；关节腔注射

    [中图分类号] R943 [文献标识码] A [文章编号] 1674-4721(2016)10(c)-0004-05

    [Abstract]Objective To evaluate the quality and toxicity of triptolide microspheres for intra-articular injection.Methods Triptolide microspheres was prepared by emulsion solvent evaporation method.Surface morphology and size of microspheres were observed by transmission electron microscope.The formation of microspheres was investigated with infrared spectrometer.Entrapment efficiency and drug loading was determined by HPLC.The release of microspheres in vitro was fitted by mathematical model.The toxicity of microspheres was evaluated using hematological parameters and biochemical indexes.Results The microspheres were spherical in shape with uniform size.The mean diameter ......