Show simple item record

A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability

dc.contributor.authorLennernäs, Hansen_US
dc.contributor.authorShah, Vinod P.en_US
dc.contributor.authorCrison, John R.en_US
dc.contributor.authorAmidon, Gordon L.en_US
dc.date.accessioned2006-09-08T19:15:48Z
dc.date.available2006-09-08T19:15:48Z
dc.date.issued1995-03en_US
dc.identifier.citationAmidon, Gordon L.; Lennernäs, Hans; Shah, Vinod P.; Crison, John R.; (1995). "A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability." Pharmaceutical Research 12(3): 413-420. <http://hdl.handle.net/2027.42/41443>en_US
dc.identifier.issn1573-904Xen_US
dc.identifier.issn0724-8741en_US
dc.identifier.urihttps://hdl.handle.net/2027.42/41443
dc.identifier.urihttp://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=7617530&dopt=citationen_US
dc.description.abstractA biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transport model and human permeability results for estimating in vivo drug absorption to illustrate the primary importance of solubility and permeability on drug absorption. The fundamental parameters which define oral drug absorption in humans resulting from this analysis are discussed and used as a basis for this classification scheme. These Biopharmaceutic Drug Classes are defined as: Case 1. High solubility-high permeability drugs, Case 2. Low solubility-high permeability drugs, Case 3. High solubility-low permeability drugs, and Case 4. Low solubility-low permeability drugs. Based on this classification scheme, suggestions are made for setting standards for in vitro drug dissolution testing methodology which will correlate with the in vivo process. This methodology must be based on the physiological and physical chemical properties controlling drug absorption. This analysis points out conditions under which no in vitro-in vivo correlation may be expected e.g. rapidly dissolving low permeability drugs. Furthermore, it is suggested for example that for very rapidly dissolving high solubility drugs, e.g. 85% dissolution in less than 15 minutes, a simple one point dissolution test, is all that may be needed to insure bioavailability. For slowly dissolving drugs a dissolution profile is required with multiple time points in systems which would include low pH, physiological pH, and surfactants and the in vitro conditions should mimic the in vivo processes. This classification scheme provides a basis for establishing in vitro-in vivo correlations and for estimating the absorption of drugs based on the fundamental dissolution and permeability properties of physiologic importance.en_US
dc.format.extent1405834 bytes
dc.format.extent3115 bytes
dc.format.mimetypeapplication/pdf
dc.format.mimetypetext/plain
dc.language.isoen_US
dc.publisherKluwer Academic Publishers-Plenum Publishers; Plenum Publishing Corporation ; Springer Science+Business Mediaen_US
dc.subject.otherMathematical Modelingen_US
dc.subject.otherPharmacyen_US
dc.subject.otherIn Vitro–In Vivo Correlationen_US
dc.subject.otherBiomedicineen_US
dc.subject.otherIntestinal Permeabilityen_US
dc.subject.otherBiochemistry, Generalen_US
dc.subject.otherPharmacology/Toxicologyen_US
dc.subject.otherBioavailabilityen_US
dc.subject.otherBiomedical Engineeringen_US
dc.subject.otherMedical Lawen_US
dc.subject.otherDrug Absorptionen_US
dc.titleA Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailabilityen_US
dc.typeArticleen_US
dc.subject.hlbsecondlevelPharmacy and Pharmacologyen_US
dc.subject.hlbtoplevelHealth Sciencesen_US
dc.description.peerreviewedPeer Revieweden_US
dc.contributor.affiliationumCollege of Pharmacy, The University of Michigan, Ann Arbor, Michigan, 48109-1065en_US
dc.contributor.affiliationotherSchool of Pharmacy, Uppsala University, Box 580, S-751 23, Uppsala, Swedenen_US
dc.contributor.affiliationotherTSRL, Inc., 540 Avis Drive, Suite A, Ann Arbor, Michigan, 48108en_US
dc.contributor.affiliationotherPDA, HFD-602, Rockville, Maryland, 20857en_US
dc.contributor.affiliationumcampusAnn Arboren_US
dc.identifier.pmid7617530en_US
dc.description.bitstreamurlhttp://deepblue.lib.umich.edu/bitstream/2027.42/41443/1/11095_2004_Article_306840.pdfen_US
dc.identifier.doihttp://dx.doi.org/10.1023/A:1016212804288en_US
dc.identifier.sourcePharmaceutical Researchen_US
dc.owningcollnameInterdisciplinary and Peer-Reviewed


Files in this item

Show simple item record

Accessibility: If you are unable to use this file in its current format, please select the Contact Us link and we can modify it to make it more accessible to you.