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引用次数: 1

摘要

尽管富含脂肪的食物/药物相互作用具有重要意义,但人们对摄入的脂类对口服疏水药物生物利用度的影响的了解并不完全。为了确定脂质和脂质消化对药物溶解和吸收的影响,基于胃肠道内容物的知识,设计了一个更新的体外脂质消化模型。消化动力学对关键参数,包括pH,钙浓度和脂质底物的敏感性进行了研究。体外脂解实验结合了多种技术,如动态光散射(DLS)和电子顺磁共振(EPR),分别表征了胶体颗粒的大小和形态,以及相间药物的动态分配。
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Effects of lipids on dissolution of poorly water-soluble drugs
Despite the significance of fat-rich food/drug interactions, there is an incomplete understanding of the influence of ingested lipids on orally delivered hydrophobic drug bioavailability. In order to determine the impact of lipid and lipid digestion on drug dissolution and absorption, an updated in vitro lipid digestion model has been designed based on knowledge of gastrointestinal contents. The digestion kinetics sensitivity to key parameters, including pH, calcium concentration, and lipid substrate, has been studied. In vitro lipolysis experiments have been coupled with several techniques, such as dynamic light scattering (DLS), and electron paramagnetic resonance (EPR), to characterize respectively: size and morphology of colloidal particles, and dynamic drug partitioning between phases.
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