Comparison of the effects of sesame oil and oleic acid as suspension vehicles on gastrointestinal absorption of phenytoin in rats.

Shinkuma, Denji; Hamaguchi, Tsuneo; Yamanaka, You; Mizuno, Nobuyasu; Yata, Noboru

doi:10.1248/cpb.33.4989

Cited by 7 publications

(2 citation statements)

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“…The limitation of this study is that we could not determine the effect of lipids on PHT permeability because lipids cannot dissolve in the transport solution of the Caco‐2 permeability assay. Lipids are the major nutrient components of ENs, and the gastrointestinal absorption of PHT, a poorly soluble drug, has been reportedly altered by lipids 35,36 . Future studies are needed to elucidate the effects of lipids in ENs on gastrointestinal PHT absorption using experimental systems other than the Caco‐2 cell permeability assay.…”

Section: Discussionmentioning

confidence: 99%

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Study on enteral nutrient components causing decreased gastric phenytoin absorption

Urashima

Ueno

Takeda

et al. 2023

J Parenter Enteral Nutr

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BackgroundPreviously, we revealed that coadministration of particular enteral nutrients (ENs) decreases plasma concentrations and gastric absorption of phenytoin (PHT), an antiepileptic drug, in rats; however, the mechanism has not been clarified.MethodsWe measured the permeability rate of PHT using a Caco‐2 cell monolayer as a human intestinal absorption model with casein, soy protein, simulated gastrointestinal digested casein protein (G‐casein or P‐casein) or simulated gastrointestinal digested soy protein (G‐soy or P‐soy), dextrin, sucrose, degraded guar gum, indigestible dextrin, calcium, and magnesium, which are abundant in the ENs, and measured the solution's properties.ResultsWe demonstrated that casein (40 mg/ml), G‐soy or P‐soy (10 mg/ml), and dextrin (100 mg/ml) significantly decreased the permeability rate of PHT compared with the control. By contrast, G‐casein or P‐casein significantly increased the permeability rate of PHT. We also found that the PHT binding rate to casein 40 mg/ml was 90%. Furthermore, casein 40 mg/ml and dextrin 100 mg/ml have high viscosity. Moreover, G‐casein and P‐casein significantly decreased the transepithelial electrical resistance of Caco‐2 cell monolayers compared with casein and the control.ConclusionCasein, digested soy protein, and dextrin decreased the gastric absorption of PHT. However, digested casein decreased PHT absorption by reducing the strength of tight junctions. The composition of ENs may affect the absorption of PHT differently, and these findings would aid in the selection of ENs for orally administered PHT.

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Section: Discussionmentioning

confidence: 99%

“…Lipids are the major nutrient components of ENs, and the gastrointestinal absorption of PHT, a poorly soluble drug, has been reportedly altered by lipids. 35,36 Future studies are needed to elucidate the effects of lipids in ENs on gastrointestinal PHT absorption using experimental systems other than the Caco-2 cell permeability assay.…”

Section: Discussionmentioning

confidence: 99%