阿托伐他汀钙微球对高血脂症模型大鼠降脂作用研究

The Research of Lipid-lowering Effect of Atorvastatin Calcium Microspheres on Hyperlipidemia Model of Rats

制备载阿托伐他汀钙聚合物微球,研究高血脂症模型大鼠降脂作用。采用复乳-溶剂挥发法制备载阿托伐他汀钙微球,利用扫描电镜观察微球表面形态,红外光谱分析载药微球的组成,考察微球的粒径、晶体结构及体外释放性能,通过体内药效学实验研究微球的降血脂作用。结果:阿托伐他汀钙微球的制备工艺稳定,微球形态圆整,平均粒径为2.048±0.15μm,药物被包埋在微球中。通过最佳工艺处方制备的阿托伐他汀钙微球的载药量为10.14±0.34%,包封率为80.12±1.28%,微球体外释放实验证实具有缓释性能。结论:高血脂模型大鼠体内的降血脂实验证实微球具有降血脂和保护肝脏作用。

Objective Atorvastatin calcium polymeric microspheres were prepared and lipid-lowering effect of hyperlipidemia model of rats were studied.Methods The atorvastatin calcium microspheres were prepared by double emulsion-solvent evaporation method.The surface morphology of the microspheres was observed by scanning electron microscopy.The microspheres were verified by infrared spectroscopy.The formation,the properties of these microspheres,such as particle size,crystal structure and in vitro release characteristics were studied.The lipid-lowering effects were studied by pharmacodynamic experiment in animals.Results The preparation process of atorvastatin calcium microspheres is stable,the shape of the microspheres is round,the average particle size distribution is 2.048±0.15μm,and the drug has been encapsulated in the microspheres.The drug loading of fenofibrate microspheres prepared by the best process prescription was 10.14±0.34%,and the encapsulation efficiency was 80.12±1.28%.In vitro release experiment of microspheres has a slow release performance.Conclusions The Lipid-lowering experiment of hyperlipidemia model rats confirmed that the fall hematic fat action and protect the liver function of microspheres.