0000000000600018

AUTHOR

N Ruiz-balaguer

showing 2 related works from this author

Nonlinear intestinal absorption kinetics of cefuroxime axetil in rats.

1997

Cefuroxime is commercially available for parenteral administration as a sodium salt and for oral administration as cefuroxime axetil, the 1-(acetoxy)ethyl ester of the drug. Cefuroxime axetil is a prodrug of cefuroxime and has little, if any, antibacterial activity until hydrolyzed in vivo to cefuroxime. In this study, the absorption of cefuroxime axetil in the small intestines of anesthetized rats was investigated in situ, by perfusion at four concentrations (11.8, 5, 118 and 200 microM). Oral absorption of cefuroxime axetil can apparently be described as a specialized transport mechanism which obeys Michaelis-Menten kinetics. Parameters characterizing absorption of prodrug in free solutio…

PharmacologyMaleCefuroximeChromatographyChemistryAbsorption (skin)ProdrugPharmacologyIntestinal absorptionBioavailabilityCephalosporinsRatsInfectious DiseasesPharmacokineticsIntestinal AbsorptionOral administrationIntestine SmallmedicineAnimalsPharmacology (medical)Rats WistarCefuroximemedicine.drugAntibacterial agentResearch Article
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Intestinal transport of cefuroxime axetil in rats: absorption and hydrolysis processes.

2002

Studies were performed using three cefuroxime axetil solutions (11.8, 118 and 200 microM) in three selected intestinal segments and one cefuroxime axetil solution (118 microM) in colon of anaesthetized rats. First-order absorption rate pseudoconstants, k(ap) and effective permeability coefficients, P(eff), were calculated in each set. Absorption of cefuroxime axetil can apparently be described as a carrier-mediated transport, which obeys Michaelis-Menten and first order kinetics in the proximal segment of the small intestine and a passive diffusion mechanism in the mean and distal segments. The absorption kinetic parameters for cefuroxime axetil were obtained: Vm=0.613 (0.440) microM min-1;…

MaleStereochemistryPharmaceutical ScienceModels BiologicalIntestinal absorptionPharmacokineticsmedicineAnimalsProdrugsIntestinal MucosaRats WistarBiotransformationAntibacterial agentCefuroximeIntestinal permeabilityChromatographyChemistryHydrolysisBiological TransportProdrugmedicine.diseaseSmall intestineCephalosporinsRatsPerfusionmedicine.anatomical_structureIntestinal AbsorptionCefadroxilCefuroximeAlgorithmsmedicine.drugInternational journal of pharmaceutics
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