胰岛素聚β-羟基丁酸酯微球体外性质的研究

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目的:以液中干燥法优化制得到的胰岛素聚β-羟基丁酸酯微球作为研究对象,考察微球的体外相关性质。方法:通过光学显微镜观察微球表面形态;用固定漏斗法测定微球的流动性;通过重量法考察微球的吸湿性;在冷藏和室温条件下,考察微球的初步稳定性;通过体外释放试验,考察微球中药物体外释放特点。结果:微球表面光滑,外观呈球形,流动性良好,临界相对湿度为95.09%,在考察条件下,微球的外观及微球的载药量没有显著变化;与原药胰岛素相比,微球中药物体外释放t_(1/2)延长6倍多,表现出一级动力学规律,释药后微球形态改变。结论:微球的缓释作用明显,微球释放药物后,发生了明显的降解。 OBJECTIVE: To investigate the in vitro related properties of microspheres in vitro with poly-β-hydroxybutyrate-insulin microspheres prepared by liquid-drying method. Methods: Morphology of microspheres was observed by light microscopy. The fluidity of microspheres was measured by fixed funnel method. The hygroscopicity of microspheres was examined by gravimetric method. The initial stability of microspheres was investigated under refrigeration and at room temperature. Test, investigate the microspheres drug release characteristics in vitro. Results: The microspheres had a smooth surface, a spherical appearance and good fluidity with a critical relative humidity of 95.09%. Under the conditions of investigation, the appearance of the microspheres and the drug loading of the microspheres did not change significantly. Compared with the original drug insulin, The in vitro release of t_ (1/2) drug in the ball prolonged more than 6 times, showing a first-order kinetic law, and the shape of the microspheres changed after drug release. Conclusion: The sustained-release effect of the microspheres is obvious. After the microspheres release the drug, obvious degradation occurs.
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