PMID: 11923059Mar 30, 2002Paper

The effect of amiloride on the in vivo effective permeability of amoxicillin in human jejunum: experience from a regional perfusion technique

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
H LennernäsG L Amidon

Abstract

The purpose of this human intestinal perfusion study (in vivo) was twofold. Firstly, we aimed to determine the effective in vivo jejunal permeability (P(eff)) of amoxicillin and to classify it according to the Biopharmaceutics Classification System (BCS). Secondly, we investigated the acute effect of amiloride on the jejunal P(eff) of amoxicillin. Amoxicillin, a beta-lactam antibiotic, has been reported to be absorbed across the intestinal mucosa by both passive diffusion and active transport. A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 14 healthy volunteers. Each perfusion lasted for 200 min and was divided into two periods of 100 min each. The concentration of amoxicillin entering the jejunal segment was 300 mg/l in both periods, and amiloride, an inhibitor of the Na+/H+ exchanger, was added at 25 mg/l in period 2. The concentrations of amoxicillin and amiloride in the outlet jejunal perfusate were measured with two different HPLC-methods. Antipyrine and [14C]PEG 4000 were added as internal standards to the perfusion solution. Amiloride had no significant effect on the jejunal P(eff) of amoxicillin. The human in vivo jejunal P(eff) for amoxicillin was 0.34+/-0.11 x 10(-4) ...Continue Reading

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Citations

May 11, 2007·Archives of Pharmacal Research·Teerawat SahasathianNongnuj Muangsin
Mar 22, 2005·International Journal of Pharmaceutics·Kouki ObataYosinori Aso
Apr 25, 2003·International Journal of Pharmaceutics·Kiyohiko SuganoYoshinori Aso
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