| Drug permeation through human skin II: Permeability of ionizable compounds. | |
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MedLine Citation:
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PMID: 6502479 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The aim of this study was to establish whether ionized as well as un-ionized forms of certain 4-oxo-4H-1-benzopyran-2-carboxylic acids (chromone-2-carboxylic acids) with pKa values less than 2 permeated through excised human skin and, if so, to determine the permeability coefficients of the permeating species. The permeation properties of four carboxylic acids were studied as a function of concentration over the pH range 5-7 at 37 degrees C with plexiglass diffusion cells. Plots of J/CA- (the total flux due to un-ionized and ionized species obtained under steady-state conditions per unit concentration of ionized drug in the donor compartment) against CH3O+ resulted in straight-line relationships. The intercepts of these plots were shown to equal PA-, whereas the slopes multiplied by the Ka values of the compounds equalled PHA, the permeability coefficients of the ionized and un-ionized species, respectively. With all four compounds, both species were found to permeate skin, although the permeability coefficients of the un-ionized species were approximately 10(4) greater than those for the ionized species. It was demonstrated that the relative contributions of the ionized and un-ionized species to the total flux, as well as the total flux, vary significantly, depending on the pH of the drug solution in the donor cell. This may provide a means of controlling the flux of these and similar compounds through human skin. |
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Authors:
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J Swarbrick; G Lee; J Brom; N P Gensmantel |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 73 ISSN: 0022-3549 ISO Abbreviation: J Pharm Sci Publication Date: 1984 Oct |
Date Detail:
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Created Date: 1985-01-09 Completed Date: 1985-01-09 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1352-5 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Chromatography, High Pressure Liquid Chromones / metabolism Humans Hydrogen-Ion Concentration Kinetics Permeability Pharmaceutical Preparations / metabolism* Skin Absorption* Solubility |
| Chemical | |
Reg. No./Substance:
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0/Chromones; 0/Pharmaceutical Preparations; 4940-39-0/chromone-2-carboxylic acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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