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艾塞那肽能显著改善2型糖尿病患者的血糖控制,其长效缓释微球可提高患者的顺应性,减轻药物的不良反应。然而,在微球制备过程中通常会遇到多肽稳定性下降、突释和包封率低等问题。本文综述了上述问题的解决方法或思路。通过选择合适的聚合物载体和有机溶剂、添加多肽稳定剂(如多羟基类、盐类和金属阳离子等),可提高微球中艾塞那肽的稳定性。对艾塞那肽本身及聚合物载体的结构修饰、添加渗透压调节剂或乳化剂,以及选择新型制备方法 (如w/o/o法等)有利于改善微球中药物突释、提高包封率。
Exenatide can significantly improve glycemic control in patients with type 2 diabetes, and its long-acting sustained-release microspheres can improve patient compliance and reduce drug adverse reactions. However, the stability of the polypeptide usually encountered in the preparation of microspheres decreased, burst release and entrapment efficiency and other issues. This article summarizes the solutions to these problems or ideas. The stability of exenatide in microspheres can be enhanced by selecting suitable polymeric carriers and organic solvents, adding peptide stabilizers (such as polyhydroxyls, salts and metal cations, etc.). Structure modification of exenatide itself and polymer carrier, addition of osmotic pressure regulator or emulsifier, and selection of new preparation methods (such as w / o / o method) are beneficial to improve drug burst release in microspheres and improve the package Lock rate.