口服固体制剂的体外释放和生物可访问性在动态胃肠道系统中模拟禁食和食状态:对甲福明化片的案例研究
Shilei Yang1, Zejun Hu1, Peng Wu2
1Life Quality Engineering Interest Group, School of Chemical and Environmental Engineering, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, Jiangsu Province 215123, China; Xiao Dong Pro-health (Suzhou) Instrumentation Co Ltd, Suzhou, Jiangsu Province 215152, China.
食物显著影响口服药片中甲福明的释放,持续释放 (SR) 配方的食物效应比立即释放 (IR) 配方更小. 动态人类胃肠 (DHSI-IV) 系统准确地预测了这些体内行为.
科学领域:
- 药理动力学 药理动力学
- 药物输送系统 药物输送系统
- 胃肠道生理学 胃肠道生理学
背景情况:
- 食物摄入显著影响胃肠道 (GI) 释放和吸收口服固体剂型.
- 了解这些食物的影响对于优化药物配方和预测体内性能至关重要.
研究的目的:
- 为了研究食状态与禁食状态对甲福明化即时释放 (IR) 和持续释放 (SR) 片的胃肠道释放和生物可访问性的影响.
- 评估动态人体胃肠系统在体外 (DHSI-IV) 对体内药物动力学结果的预测能力.
主要方法:
- 利用动态人体胃肠体外 (DHSI-IV) 系统来模拟禁食和食状态.
- 评估了梅特福林IR和SR片的动态连续释放和生物可访问性.
- 采用基于卷积的方法,将体外生物可访问性与体外血度数据相关联.
主要成果:
- 两种甲素IR和SR片在养状态下显示延迟释放,与禁食状态相比.
- 在食条件下,梅特福林IR片显示生物可访问分数 (76.2%的禁食状态) 在食条件下显著减少.
- 梅特福林SR片表现出较少的食物损害,食/禁食生物可访问性比为95.5%.
结论:
- DHSI-IV系统有效地模拟了饮食对药物释放和吸收的影响.
- 与立即释放 (IR) 配方相比,持续释放 (SR) 甲胺配方在食条件下表现更好.
- DHSI-IV系统显示了预测体内药理动力学参数和评估食物对口服药物产品影响的潜力.
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