Percutaneous Penetration of Drugs: A Quantitative Structure–Permeability Relationship Study
| Autor: | Albert J. Leo, Bernard Testa, Pierre-Alain Carrupt, Corwin Hansch, Ruey-Shiuan Tsai, Nabil El Tayar |
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| Rok vydání: | 1991 |
| Předmět: |
Octanols
Chemical Phenomena Hydrocortisone Surface Properties Stereochemistry Administration Topical Skin Absorption Anti-Inflammatory Agents Pharmaceutical Science Percutaneous penetration Structure-Activity Relationship Phenols Humans Transcellular ddc:615 Chromatography Phenols/chemistry Chemistry Physical Chemistry Quantitative structure Physicochemical Phenomena Hydrogen Bonding Permeation Molecular Weight Partition coefficient Permeability (earth sciences) Solubility Alcohols Lipophilicity Anti-Inflammatory Agents/chemistry Solvents Steroids/chemistry/pharmacokinetics Alcohols/chemistry/pharmacokinetics Steroids |
| Zdroj: | Journal of Pharmaceutical Sciences, Vol. 80, No 8 (1991) pp. 744-749 |
| ISSN: | 0022-3549 |
| DOI: | 10.1002/jps.2600800807 |
| Popis: | Human skin permeation data taken from the literature were analyzed for quantitative relationships with physicochemical properties and structural descriptors. No correlations exist with molecular weights and solvent-accessible surface areas. In most cases, skin permeation was inversely correlated with the parameter delta log Poct-hep (i.e., log Poctanol minus log Pheptane), which is mainly a measure of the H-bond donor acidity of the solutes. Lipophilicity itself, as expressed by log Poctanol, also contributes positively to skin permeation in some cases. The results of this quantitative structure-permeability relationship study are interpreted in terms of a unified mechanistic model whereby drugs can permeate via an intercellular route (correlation with both delta log Poct-hep and log Poct) and/or a transcellular route (correlation with log Poct only). |
| Databáze: | OpenAIRE |
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