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Predicting the exposure and antibacterial activity of fluoroquinolones based on physicochemical properties
Volgyi G.3; Vizseralek G.3; Takacs-Novak K.3; Avdeef A.1; Tam K.Y.2
2012-08-30
Source PublicationEuropean Journal of Pharmaceutical Sciences
ISSN09280987 18790720
Volume47Issue:1Pages:21-27
Abstract

The purposes of this study are to evaluate if the PAMPA (Parallel Artificial Membrane Permeability Assay) permeability and the true partition coefficient could be useful for predicting AUC and MIC data of a group of antibacterial fluoroquinolones (FQs). The protonation macro- and microconstants, the n-octanol/water partition coefficients at isoelectric pHs, and the PAMPA permeability of 11 selected FQs were determined, and used to calculate the true partition coefficient, the interactivity parameter between the acidic and basic group, and the apparent intrinsic permeability. It has been shown that the apparent intrinsic permeability correlates well with the AUC in human, whereas the true partition coefficient and the interactivity parameter correlate with 1/MIC values on two Gram-positive bacteria, namely Streptococcus pneumonia and Staphylococcus aureus (methicillin-susceptible). The AUC/MIC ratios predicted from these correlations have shown to be in good agreement with the literature values. It is envisaged that the models described in this study could be useful in the development of new FQs by enabling an early prediction of AUC/MIC ratios based on physicochemical properties. © 2012 Elsevier B.V. All rights reserved.

KeywordAntimicrobial Activity Fluoroquinolones Mic Pampa Protonation Microconstants True Partition Coefficients
DOI10.1016/j.ejps.2012.04.022
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000307696800004
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Cited Times [WOS]:22   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.In-ADME Research
2.AstraZeneca
3.Semmelweis Egyetem
Recommended Citation
GB/T 7714
Volgyi G.,Vizseralek G.,Takacs-Novak K.,et al. Predicting the exposure and antibacterial activity of fluoroquinolones based on physicochemical properties[J]. European Journal of Pharmaceutical Sciences,2012,47(1):21-27.
APA Volgyi G.,Vizseralek G.,Takacs-Novak K.,Avdeef A.,&Tam K.Y..(2012).Predicting the exposure and antibacterial activity of fluoroquinolones based on physicochemical properties.European Journal of Pharmaceutical Sciences,47(1),21-27.
MLA Volgyi G.,et al."Predicting the exposure and antibacterial activity of fluoroquinolones based on physicochemical properties".European Journal of Pharmaceutical Sciences 47.1(2012):21-27.
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