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

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dc.contributor.author Lennernäs, Hans en_US
dc.contributor.author Shah, Vinod P. en_US
dc.contributor.author Crison, John R. en_US
dc.contributor.author Amidon, Gordon L. en_US
dc.date.accessioned 2006-09-08T19:15:48Z
dc.date.available 2006-09-08T19:15:48Z
dc.date.issued 1995-03 en_US
dc.identifier.citation Amidon, 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.issn 1573-904X en_US
dc.identifier.issn 0724-8741 en_US
dc.identifier.uri http://hdl.handle.net/2027.42/41443
dc.identifier.uri http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=7617530&dopt=citation en_US
dc.description.abstract A 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.extent 1405834 bytes
dc.format.extent 3115 bytes
dc.format.mimetype application/pdf
dc.format.mimetype text/plain
dc.language.iso en_US
dc.publisher Kluwer Academic Publishers-Plenum Publishers; Plenum Publishing Corporation ; Springer Science+Business Media en_US
dc.subject.other Mathematical Modeling en_US
dc.subject.other Pharmacy en_US
dc.subject.other In Vitro–In Vivo Correlation en_US
dc.subject.other Biomedicine en_US
dc.subject.other Intestinal Permeability en_US
dc.subject.other Biochemistry, General en_US
dc.subject.other Pharmacology/Toxicology en_US
dc.subject.other Bioavailability en_US
dc.subject.other Biomedical Engineering en_US
dc.subject.other Medical Law en_US
dc.subject.other Drug Absorption en_US
dc.title A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability en_US
dc.type Article en_US
dc.subject.hlbsecondlevel Pharmacy and Pharmacology en_US
dc.subject.hlbtoplevel Health Sciences en_US
dc.description.peerreviewed Peer Reviewed en_US
dc.contributor.affiliationum College of Pharmacy, The University of Michigan, Ann Arbor, Michigan, 48109-1065 en_US
dc.contributor.affiliationother School of Pharmacy, Uppsala University, Box 580, S-751 23, Uppsala, Sweden en_US
dc.contributor.affiliationother TSRL, Inc., 540 Avis Drive, Suite A, Ann Arbor, Michigan, 48108 en_US
dc.contributor.affiliationother PDA, HFD-602, Rockville, Maryland, 20857 en_US
dc.contributor.affiliationumcampus Ann Arbor en_US
dc.identifier.pmid 7617530 en_US
dc.description.bitstreamurl http://deepblue.lib.umich.edu/bitstream/2027.42/41443/1/11095_2004_Article_306840.pdf en_US
dc.identifier.doi http://dx.doi.org/10.1023/A:1016212804288 en_US
dc.identifier.source Pharmaceutical Research en_US
dc.owningcollname Interdisciplinary and Peer-Reviewed
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