Chemical and Pharmaceutical Bulletin · 1978 · 57 citations · 0 references
PharmacyPharmacokineticsPharmacologyBioavailabilityDrug DeliveryOral Drug DeliveryDrug DispositionFormulation Effects On BioavailabilityFormulation Effects On DissolutionOral BioavailabilityOral Bioavailability EnhancementRelative BioavailabilityCumulative Urinary ExcretionDissolution Rate AnalysisDrug Formulation ComparisonNonsteroidal Anti-inflammatory Drug PharmacologyPharmacokinetic Bioavailability AnalysisRabbit Drug FormulationsRabbit PharmacokineticsVeterinary Pharmacokinetics
Freeze-dried inclusion compounds of nonsteroidal antiinflammatory drugs with β-cyclodextrin were administered orally to rabbits and beagle dogs in comparison with simply freeze-dried drugs. The antiinflammatory drugs used were flufenamic acid, ibuprofen, ketoprofen and indomethacin. Freeze-dried inclusion compounds showed higher levels of blood concentration and cumulative urinary excretion compared with simply freeze-dried drugs, except for indomethacin. In general, freeze-dried inclusion compounds of drugs with β-cyclodextrin showed a high dissolution rate and high bioavailability. As an exceptional case, no enhancement of the bioavailability was observed in rabbits for the inclusion compound of indomethacin compared with the simply freezedried drug. A double maxima phenomenon in blood concentration was observed in the cases of flufenamic acid and indomethacin.