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Comparison of in vitro – in vivo extrapolation of biliary clearance using an empirical scaling factor versus transport‐based scaling factors in sandwich‐cultured rat hepatocytes

dc.contributor.authorZou, Pengen_US
dc.contributor.authorLiu, Xingrongen_US
dc.contributor.authorWong, Susanen_US
dc.contributor.authorFeng, Meihua Roseen_US
dc.contributor.authorLiederer, Bianca M.en_US
dc.date.accessioned2013-08-02T20:51:37Z
dc.date.available2014-10-06T19:17:44Zen_US
dc.date.issued2013-08en_US
dc.identifier.citationZou, Peng; Liu, Xingrong; Wong, Susan; Feng, Meihua Rose; Liederer, Bianca M. (2013). "Comparison of in vitro – in vivo extrapolation of biliary clearance using an empirical scaling factor versus transport‐based scaling factors in sandwich‐cultured rat hepatocytes." Journal of Pharmaceutical Sciences 102(8): 2837-2850. <http://hdl.handle.net/2027.42/99050>en_US
dc.identifier.issn0022-3549en_US
dc.identifier.issn1520-6017en_US
dc.identifier.urihttps://hdl.handle.net/2027.42/99050
dc.description.abstractBiliary clearance (CL b ) is often underestimated by in vitro – in vivo extrapolation from sandwich‐cultured hepatocytes (SCHs). The objective of this study was to compare the performance of a universal correction factor with transporter‐based correction factors in correcting underestimation of CL b . The apparent in vitro CL b of a training set of 21 compounds was determined using the SCH model and extrapolated to apparent in vivo CL b (CL b, app ). A universal correction factor (10.2) was obtained by a linear regression of the predicted CL b, app and observed in vivo CL b of training set compounds and applied to an independent test set ( n = 20); the corrected CL b predictions of 13 compounds were within twofold error of observed values. Furthermore, two transporter‐based correction factors (Organic anion transporting polypeptides/multidrug‐resistance‐related protein 2 and diffusion/P‐glycoprotein) were estimated by linear regression analysis of training set compounds. The applications of the two correction factors to the test set resulted in improved prediction precision. In conclusion, both the universal correction factor and transporter‐based correction factors provided reasonable corrections of CL b values, which are often underestimated by the SCH model. The use of transporter‐based correction factors resulted in an even greater improvement of predictions for compounds with intermediate‐to‐high CL b values. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:2837–2850, 2013en_US
dc.publisherWiley Subscription Services, Inc., A Wiley Companyen_US
dc.subject.otherHepatocytesen_US
dc.subject.otherClearanceen_US
dc.subject.otherDrug Transporten_US
dc.subject.otherHepatobiliary Dispositionen_US
dc.subject.otherIn Vitro / in Vivo Correlations (IVIVC)en_US
dc.subject.otherOrganic Aniontransporting Polypeptide Transportersen_US
dc.subject.otherP‐Glycoproteinen_US
dc.subject.otherBiliary Excretionen_US
dc.titleComparison of in vitro – in vivo extrapolation of biliary clearance using an empirical scaling factor versus transport‐based scaling factors in sandwich‐cultured rat hepatocytesen_US
dc.typeArticleen_US
dc.rights.robotsIndexNoFollowen_US
dc.subject.hlbsecondlevelPharmacy and Pharmacologyen_US
dc.subject.hlbtoplevelHealth Sciencesen_US
dc.description.peerreviewedPeer Revieweden_US
dc.contributor.affiliationumDepartment of Pharmaceutical Sciences, University of Michigan, Ann Arbor, Michigan 48109en_US
dc.contributor.affiliationotherGenentech, Inc., Drug Metabolism and Pharmacokinetics, South San Francisco, California 94080en_US
dc.contributor.affiliationotherGenentech, Inc., Drug Metabolism and Pharmacokinetics, South San Francisco, California 94080. Telephone +650‐467‐7343; Fax: 650‐225‐6452en_US
dc.identifier.pmid23712819en_US
dc.description.bitstreamurlhttp://deepblue.lib.umich.edu/bitstream/2027.42/99050/1/23620_ftp.pdf
dc.identifier.doi10.1002/jps.23620en_US
dc.identifier.sourceJournal of Pharmaceutical Sciencesen_US
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dc.owningcollnameInterdisciplinary and Peer-Reviewed


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