6533b838fe1ef96bd12a474b

RESEARCH PRODUCT

Regional Intestinal Drug Permeability and Effects of Permeation Enhancers in Rat

David DahlgrenMikael HedelandMaria-jose Cano-cebriánHans LennernäsTobias OlanderMarkus Sjöblom

subject

DrugKetoprofenmedia_common.quotation_subjectlcsh:RS1-441Pharmaceutical ScienceGastroenterology and Hepatology02 engineering and technologyPharmacology030226 pharmacology & pharmacyArticleDosage formlcsh:Pharmacy and materia medicaJejunumPharmaceutical Sciences03 medical and health sciences0302 clinical medicineabsorption-modifying excipientsintestinal perfusionIn vivoGastroenterologimedicineLarge intestineregional intestinal permeabilitymedia_commonIntestinal permeabilityChemistrypermeation enhancersPermeationFarmaceutiska vetenskaper021001 nanoscience & nanotechnologymedicine.diseasepharmaceutical developmentmedicine.anatomical_structureoral peptide delivery0210 nano-technologymedicine.drug

description

Sufficient colonic absorption is necessary for all systemically acting drugs in dosage forms that release the drug in the large intestine. Preclinically, colonic absorption is often investigated using the rat single-pass intestinal perfusion model. This model can determine intestinal permeability based on luminal drug disappearance, as well as the effect of permeation enhancers on drug permeability. However, it is uncertain how accurate the rat single-pass intestinal perfusion model predicts regional intestinal permeability and absorption in human. There is also a shortage of systematic in vivo investigations of the direct effect of permeation enhancers in the small and large intestine. In this rat single-pass intestinal perfusion study, the jejunal and colonic permeability of two low permeability drugs (atenolol and enalaprilat) and two high-permeability ones (ketoprofen and metoprolol) was determined based on plasma appearance. These values were compared to already available corresponding human data from a study conducted in our lab. The colonic effect of four permeation enhancers&mdash

yearjournalcountryeditionlanguage
2020-03-01Pharmaceutics
https://doi.org/10.3390/pharmaceutics12030242