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微球制剂的药物突释现象一直是难以解决的问题。突释效应造成在短时间内释放出大量的药物,使体内的血药水平陡然升高,产生不良反应。对于靶向缓释微球而言,将导致靶部位有效药物量的减少,最终削弱微球制剂的靶向作用。因此,如何有效地减少药物突释,实现药物的控制释放一直是药学工作者努力研究的课题。作者结合国内外研究报道综合介绍影响微球制剂释放性能的因素,为其进一步的应用提供相关的理论基础。
Drug release microspheres burst phenomenon has been difficult to solve. Burst effect caused by the release of a large number of drugs in a short period of time, so that the blood level of the body suddenly increased, resulting in adverse reactions. For targeted release microspheres, this will result in a reduction in the amount of drug available at the target site, ultimately impairing the targeting of the microsphere formulation. Therefore, how to effectively reduce drug burst and achieve the controlled release of pharmaceuticals has always been a subject that pharmaceutical workers are trying hard to study. Combined with domestic and foreign research reports, the author comprehensively introduces the factors that affect the release properties of microsphere formulations and provides relevant theoretical basis for its further application.