用于口服的含有胰岛素的-酸微粒的配方和评估
Ildikó Bácskay1,2, Boglárka Papp1, Péter Pártos1
1Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, 4032 Debrecen, Hungary.
Pharmaceutics
|January 23, 2024
概括
研究人员开发了用于口服胰岛素的-酸微粒. 这些配方增强了胰岛素的吸收,并在胃肠道中保护了胰岛素,这表明改善了口服生物可用性.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统是药物输送系统.
- 生物材料是一种生物材料.
背景情况:
- 口服胰岛素的输送面临挑战,因为的不稳定性和吸收不良.
- 酸是一种适合保护胃肠道中药物的pH响应性聚合物.
- 非离子表面活性剂和透增强剂可以改善的吸收.
研究的目的:
- 制备用于口服胰岛素的-酸微粒.
- 评估胰岛素载微粒的封装效率,稳定性和透性.
- 调查Labrasol ALF和Labrafil M 2125 CS作为透增强剂的作用.
主要方法:
- 酸微粒与胰岛素一起配制.
- 确定了封装效率.
- 进行了体外溶解和酶稳定性测试.
- 使用Caco-2细胞进行了透性研究.
主要成果:
- 微粒子配方实现了超过80%的封装效率.
- 酸微粒表明pH响应性胀和药物释放,保护胰岛素.
- 在模拟肠液 (SIF) 中120分钟后,胰岛素含量保持在66%.
- 透增强剂显著改善了通过Caco-2细胞的胰岛素运输.
结论:
- 酸微粒有效地封装胰岛素.
- 这些配方保护胰岛素免受胃肠道的降解.
- 透增强剂和酸盐微粒可以增强胰岛素的吸收.
- 这些微粒系统显示出改善口服胰岛素生物可用性的潜力.
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