Influence of bile on the gastrointestinal absorption of phenytoin in rats.

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

doi:10.1248/cpb.33.5023

Cited by 12 publications

(5 citation statements)

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“…Roxithromycin dissolution in the presence of 30 mM sodium taurocholate was 3.09-fold greater than that when no bile salt was added. Enhanced solubility and dissolution rates by bile salts have been demonstrated in vitro for compounds such as griseofulvin [14], phenytoin [15] and danazol [16].…”

Section: Resultsmentioning

confidence: 99%

“…When calculating the amount of sodium taurocholate administered, the gut volume was considered as 11.3 ml/0.25 kg rat [10]. Blood samples (approximately 220 ml, each) were collected from the carotid artery at 0 (as a control), 5,15,30,60,90,120,180,240,360,480, 600, 720 and 1440 min following oral administration of roxithromycin. A volume of 0.3 ml of heparinized 0.9% NaClinjectable solution (25 U/ml) was used to flush each cannula immediately after obtaining each blood sample, in order to prevent blood clotting and to compensate for fluid loss.…”

Section: Pharmacokinetics In Ratsmentioning

confidence: 99%

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Decrease in gastrointestinal absorption of roxithromycin in bile duct cannulated rats due to depletion of bile salts

Lee

Park

et al. 2013

Biopharm & Drug Disp

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The purpose of this study was to investigate the effect of bile salts on gastrointestinal absorption and the plasma second peak phenomenon of roxithromycin in rats. The pharmacokinetic parameters of roxithromycin were calculated after single oral administration at a dose of 20 mg/kg in sham-operated (control), bile duct cannulated (BDC) and bile salt co-administered bile duct cannulated (BSBDC) rats. In BDC rats, the total area under the plasma concentration-time curve from time zero to time infinity (AUC0-∞) and the peak plasma concentration (Cmax) were significantly smaller (0.572-fold) and lower (0.412-fold), respectively, than those in the control rats. These values were recovered by co-administration of bile salt (0.831- and 0.828-fold for AUC0-∞ and Cmax compared with the control, respectively). Thus, the decreased absorption of roxithromycin in BDC rats could be due to a depletion of bile. The solubility of roxithromycin was 3.09-fold increased at 30 mm of sodium taurocholate. The oral dosage regimen of roxithromycin could be changed in patients with bile deficiency or when the drug is administered to individuals on a high-fat diet, if the present rat data can be extrapolated to humans.

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Section: Resultsmentioning

confidence: 99%

Section: Pharmacokinetics In Ratsmentioning

confidence: 99%

Decrease in gastrointestinal absorption of roxithromycin in bile duct cannulated rats due to depletion of bile salts

Lee

Park

et al. 2013

Biopharm & Drug Disp

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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%

“…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%

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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“…Although in these experiments, the plasma concentrations of YJA-20379-8 were higher (Figure 2), AUC 0 ± 12 h was (P`0Á154) greater (54%), and the percentages of injected dose recovered at 24 h as unchanged drug was less (P`0Á452, 32%) than in rats without bile juice injection after bile duct cannulation, the lack of signi®cance between these values in the limited number of rats studied precluded any interpretation. However, enhanced absorption of poorly water-soluble drugs, phenytoin (Shinkuma et al 1985) and vitamin E (Traber et al 1986) by bile juice has been reported.…”

Section: Closed-loop Studymentioning

confidence: 99%

Gastrointestinal Absorption of a New Reversible Proton Pump Inhibitor, YJA-20379-8, and its Pharmacokinetics after Oral Administration in Acetic Acid-induced Gastric Ulcer in Rats

Chung

Han

Kim

et al. 1999

Journal of Pharmacy and Pharmacology

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The absorption of YJA-20379-8 (3-butyryl-4-[5-(R)-(+)-methylbenzylamino]-8-ethoxy-1,7-naphthyrid ine) from various rat gastrointestinal segments was evaluated using in-situ closed-loops. The pharmacokinetics of the drug were also evaluated after oral administration to rats with acetic acid-induced gastric ulcer (AIURs). The concentrations of YJA-20379-8 in the biological samples were analyzed by HPLC. The absorption of YJA-20379-8 from stomach and jejunum was fast, but approximately 50% of the drug was recovered from each segment at 24 h. The total areas under the plasma concentration-time curves from time zero to 24h (AUC(0-24h)) were 161, 392, 233, 365, and 226 microg min mL(-1) for stomach, duodenum, jejunum, ileum, and colon, respectively. After oral administration of the drug, the plasma concentrations and the resultant AUC (0- 12h) were not significantly different between control and AIURs. The detection limits of YJA-20379-8 in human plasma and urine were 50 and 100 ng mL(-1), respectively. The results suggest that modification of the oral dose of YJA-20379-8 may not be required in gastric ulcer patients if the present rat pharmacokinetic data could be extrapolated to man.

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Influence of bile on the gastrointestinal absorption of phenytoin in rats.

Cited by 12 publications

References 0 publications

Decrease in gastrointestinal absorption of roxithromycin in bile duct cannulated rats due to depletion of bile salts

Decrease in gastrointestinal absorption of roxithromycin in bile duct cannulated rats due to depletion of bile salts

Study on enteral nutrient components causing decreased gastric phenytoin absorption

Gastrointestinal Absorption of a New Reversible Proton Pump Inhibitor, YJA-20379-8, and its Pharmacokinetics after Oral Administration in Acetic Acid-induced Gastric Ulcer in Rats

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