Percutaneous penetration of drugs: a quantitative structure-permeability relationship study
|Published in||Journal of pharmaceutical sciences. 1991, vol. 80, no. 8, p. 744-749|
|Abstract||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).|
|Keywords||Administration, Topical — Alcohols/chemistry/pharmacokinetics — Anti-Inflammatory Agents/chemistry — Chemistry, Physical — Humans — Hydrocortisone — Hydrogen Bonding — Molecular Weight — Octanols — Phenols/chemistry — Physicochemical Phenomena — Skin Absorption — Solubility — Solvents — Steroids/chemistry/pharmacokinetics — Structure-Activity Relationship — Surface Properties|
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|EL TAYAR, Nabil et al. Percutaneous penetration of drugs: a quantitative structure-permeability relationship study. In: Journal of pharmaceutical sciences, 1991, vol. 80, n° 8, p. 744-749. doi: 10.1002/jps.2600800807 https://archive-ouverte.unige.ch/unige:9926|