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The permeation of amphoteric drugs through artificial membranes - An in combo absorption model based on paracellular and transmembrane permeability
Tam K.Y.2; Avdeef A.1; Tsinman O.1; Sun N.1
2010-01-28
Source PublicationJournal of Medicinal Chemistry
ISSN00222623
Volume53Issue:1Pages:392-401
Abstract

The permeability characteristics of 33 amphoteric drugs (about 64% zwitterions at physiological pH) were studied using the parallel artificial membrane permeability assay (PAMPA) at pH 6.5. The PAMPA data were modified to include the paracellular permeability component found in cellular monolayers based on a newly generalized version of a popular model devised for Caco-2 cells. These "in combo" PAMPA data were used to predict the human absolute bioavailability of the ampholytes. The analysis produced a good fit, with only five outliers whose transport properties, could be rationalized by (a) nonpassive permeability processes, (b) metabolic instability, and (c) the possible sensitivity to microclimate pH effects in the case of acidic ampholytes. With the exception of two compounds, all of the ampholytes with bioavailability <50% were predominantly transported by the paracellular route, surprisingly with several of the compounds having molecular weights exceeding 350 Da. ©2009 American Chemical Society.

DOI10.1021/jm901421c
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000273268300033
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Citation statistics
Cited Times [WOS]:33   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.PION INC
2.AstraZeneca
Recommended Citation
GB/T 7714
Tam K.Y.,Avdeef A.,Tsinman O.,et al. The permeation of amphoteric drugs through artificial membranes - An in combo absorption model based on paracellular and transmembrane permeability[J]. Journal of Medicinal Chemistry,2010,53(1):392-401.
APA Tam K.Y.,Avdeef A.,Tsinman O.,&Sun N..(2010).The permeation of amphoteric drugs through artificial membranes - An in combo absorption model based on paracellular and transmembrane permeability.Journal of Medicinal Chemistry,53(1),392-401.
MLA Tam K.Y.,et al."The permeation of amphoteric drugs through artificial membranes - An in combo absorption model based on paracellular and transmembrane permeability".Journal of Medicinal Chemistry 53.1(2010):392-401.
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