合成和释放的研究,以粉素为基础的胺酸NSAIDs的 Ester前药物
Shraddha Chugh1, Mousmee Sharma2, Garima Chandrasen1
1Department of Chemistry, University of Petroleum & Energy Studies, Dehradun, 248007, India.
Therapeutic delivery
|September 17, 2024
概括
与氨酸相关的美芬胺酸前药物显示了酶响应激活和释放. 胰腺素对于前药物激活至关重要,使得有针对性的结肠提供美胺酸.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 产品化学 药物化学
背景情况:
- 针对结肠的药物输送旨在提高治疗疗效和减少全身副作用.
- 梅芬胺酸是一种非类固醇抗炎药物 (NSAID),具有结肠特异性输送的潜力.
- 可以使用前药物策略来实现有针对性的药物释放.
研究的目的:
- 开发和表征以结的美芬胺酸的氨酸原药.
- 调查由这些前药物产生的梅芬胺酸的酶响应激活和结肠向释放.
- 为了评估释放的美芬胺酸对COX-1和COX-2的抑制.
主要方法:
- 使用1HNMR和IR光谱进行前药物表征.
- 在模拟肠道介质 (SIM) 中进行体外药物释放研究,酶度 (胰腺素) 不同.
- 高性能液体染色学 (HPLC) 用于药物定量,紫外线光谱用于释放动力学,ELISA用于酶抑制试验,扫描电子显微镜 (SEM) 用于形态学研究.
主要成果:
- 胰腺素被确定为前药物激活的必需物,使结易受水解.
- 与结合的氨酸-美芬胺酸合物在生理环境中表现出稳定性,直到被氨酸降解酶激活.
- 通过多种分析技术证实了胺酸的酶反应释放和激活的成功.
结论:
- 与埃斯特结合的氨酸-美芬胺酸合物为结肠向药物输送提供了一种有前途的方法.
- 酶响应激活是实现在结肠中向释放的关键机制.
- 这种前药物策略显示了局部NSAID治疗在胃肠道中的潜力.
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