The use of BDDCS in classifying the permeability of marketed drugs
2008 (English)In: Pharmaceutical research, ISSN 0724-8741, E-ISSN 1573-904X, Vol. 25, no 3, 483-488 p.Article in journal (Refereed) Published
We recommend that regulatory agencies add the extent of drug metabolism (i.e., >or=90% metabolized) as an alternate method in defining Class 1 marketed drugs suitable for a waiver of in vivo studies of bioequivalence. That is, >or=90% metabolized is an additional methodology that may be substituted for >or=90% absorbed. We propose that the following criteria be used to define>or=90% metabolized for marketed drugs: Following a single oral dose to humans, administered at the highest dose strength, mass balance of the Phase 1 oxidative and Phase 2 conjugative drug metabolites in the urine and feces, measured either as unlabeled, radioactive labeled or nonradioactive labeled substances, account for >or=90% of the drug dosed. This is the strictest definition for a waiver based on metabolism. For an orally administered drug to be >or=90% metabolized by Phase 1 oxidative and Phase 2 conjugative processes, it is obvious that the drug must be absorbed. This proposal, which strictly conforms to the present>or=90% criteria, is a suggested modification to facilitate a number of marketed drugs being appropriately assigned to Class 1.
Place, publisher, year, edition, pages
Springer , 2008. Vol. 25, no 3, 483-488 p.
BCS, BDDCS, bioequivalence, elimination pathways
IdentifiersURN: urn:nbn:se:uu:diva-86832DOI: 10.1007/s11095-007-9523-xPubMedID: 18236138OAI: oai:DiVA.org:uu-86832DiVA: diva2:127494