摘要
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 signifi cantly improve glycemic control in patients with type 2 diabetes. Long-acting microspheres of exenatide can improve patient compliance and reduce adverse reactions. However, the problems of poor stability, burst release and low entrapment effi ciency in the preparation process are commonly encountered. The solutions to above problems are reviewed in this paper. The stability of exenatide in microspheres can be improved by selecting appropriate polymeric carriers and organic solvents as well as adding stabilizers, such as polyhydroxy compounds, salts and metal cations. Structure modifi cations of exenatide itself and polymeric carriers, addition of osmoregulators or emulsifi ers and adoption of novel preparation method（w/o/o emulsion method, for example） are all contribute to improving burst effect and entrapment effi ciency of exenatide.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2016年第4期484-488,共5页
Chinese Journal of Pharmaceuticals
关键词
艾塞那肽
微球
制备
研究现状
exenatide
microsphere
preparation
research status
