Solubility measurement of poorly soluble drugs in fasted state simulated intestinal fluid

Zoe McKinnon, Hannah Batchelor, I. Khadra, Gavin W. Halbert
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Abstract

Adequatedrug solubility in the gastrointestinal tract is essential for systemic therapyof orally administered medications. To carry out research on the solubility ofpoorly soluble drugs in vitro, simulated intestinal fluid (SIF) is usedin place of human intestinal fluid (HIF). However, typical SIF reflects averagecompositions of HIF rather than the full range of compositions previouslyreported. This study examines a new suite of SIF media (based on variabilityobserved in HIF) to explore the range of solubility of four poorly soluble drugs(Naproxen, Indomethacin, Phenytoin and Tadalafil) in the fasted state.
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难溶性药物在空腹模拟肠液中的溶解度测定
药物在胃肠道的充分溶解度对于口服药物的全身治疗至关重要。为了研究难溶性药物的体外溶解度,采用模拟肠液(SIF)代替人肠液(HIF)。然而,典型的SIF反映了HIF的平均成分,而不是先前报道的全部成分。本研究考察了一套新的SIF培养基(基于HIF观察到的变异性),以探索四种难溶性药物(萘普生、吲哚美辛、苯妥英和他达拉非)在禁食状态下的溶解度范围。
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