Estimation of Local Bioavailability for Transdermally Applied Drugs by the Monitoring of Unboud-form Drug Concentrations in the Skin

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Estimation of local bioavailability for transdermally applied drugs by the monitoring of unboud-form drug concentrations in the skin was studied.1.Estimation of pharmacokinetic local bioavailability(1)Application of Muliti-batch Zero-Net Flux microdialysisMuliti-batch Zero-Net Flux microdialysis method enables to shorten the sampling interval. The usefulness of this method in monitoring unboud-formdrug concentrations in the skin in vivo was clarified.(2)Application of Lipo-microdialysis (Lipo-MD)Photodegradation products of ketoprofen after the dermal application were detected by the use of Lipo-MD method in vivo.2.Estimation of pharmacodynamic local bioavailabilityIn the triphasic vascular response induced by bradykinin in rat perfused mesenteric vascular beds, serial responses interfere each other. Information derived from the kinetical analysis is valuable to discuss the mechanism of action obtained by pharmacodynamic analysis.3.Antibody-incorporated microdialysisAntibody-incorporated microdialysis enables to increase the relative recovery for teicoplanin 2 to 5 times compared with that in the conventional microdialysis.4.In vivo monitoring for implanted controlled-release DDS in the skinLocal pharamacokinetic profiles were determined in two positions by microdialysis. The profile determined at 10 mm away from the DDS was completely different from that determined just beside the DDS. The importance of the precise estimation of local pharmacokinetics of unboud-form drugs was clarified.