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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
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通过原子层涂层来提高生物利用性:Fenofibrate是一个案例研究.

Balaji Ganapathy1, Vijayendra Redasani2, Sujit Debnath1

  • 1Applied Materials India Pvt. Ltd., IIT-Bombay, Powai, Maharashtra, India.

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概括
此摘要是机器生成的。

原子层涂层 (ALC) 显著提高了可溶性较差的药物纤维酸盐的生物可用性. 在没有毒性的动物模型中,氧化物涂层的纤维酸盐显示生物可用性增加了两倍.

关键词:
原子层沉积的原子层沉积.分散性 分散性.溶解研究 溶解研究氧化涂层是用氧化进行的.湿透性 湿透性 湿透性氧化涂层是用氧化进行的.

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科学领域:

  • 制药科学 制药科学
  • 材料科学 材料科学 材料科学
  • 化学工程是化学工程的重要组成部分.

背景情况:

  • 生物制药分类系统 (BCS) 的II类药物具有较差的溶解性和高透性.
  • 纤维酸 (FF) 是一种BCSII类药物,用于控制高胆固醇和甘油三水平.
  • 原子层涂层 (ALC) 是一种表面工程技术,用于修改活性药物成分 (API) 颗粒.

研究的目的:

  • 调查ALC在提高纤维酸生物可用性的有效性.
  • 为了比较未涂层,氧化涂层和氧化涂层纤维的物理和性能特征.
  • 评估ALC修饰的纤维酸的体内安全性和有效性.

主要方法:

  • 用ALC用氧化和氧化涂覆了纤维酸颗粒.
  • 分析了物理性能 (流动,湿) 和化学/固态稳定性 (1H NMR,粉末X射线衍射).
  • 在动物和狗体内研究评估了生物可用性 (AUC,Cmax).
  • 口服亚急性毒性研究对氧化物涂层的纤维酸进行了研究.

主要成果:

  • ALC涂层 (氧化,氧化) 并没有损害 fenofibrate 的结构完整性.
  • 氧化涂层改善了湿透 (接触角度接近0°) 和水友性.
  • 氧化涂层改善了流动特性和颗粒脱聚.
  • 在不改变平衡溶解度的情况下,ALC提高了溶解速率.
  • 在体内研究显示,氧化涂层纤维酸的AUC增加了约2倍,Cmax增加了约3倍.
  • 没有观察到ALC涂装 fenofibrate 的毒性.

结论:

  • ALC是一种有前途的技术,可以提高水溶性较差的BCSII类药物的生物可用性,如纤维酸盐.
  • 氧化涂层通过改善湿化和水友性来增强纤维酸的生物可用性.
  • 氧化涂层在颗粒处理和分散方面具有好处.
  • 经ALC修饰的纤维酸表明了有利的安全性.