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The Relationship of pK a and Acute Skin Irritation in Man
Authors:Berner  Bret  Wilson  Donald R  Guy  Richard H  Mazzenga  Gerard C  Clarke  Frank H  Maibach  Howard I
Institution:(1) CIBA-GEIGY, 444 Saw Mill River Road, Ardsley, New York, 10502;(2) Department of Dermatology, University of California Medical School, San Francisco, California, 94143;(3) Department of Pharmacy and Pharmaceutical Chemistry, University of California, San Francisco, California, 94143
Abstract:The relationship between pK a and skin irritation in man is studied for a homologous series of benzoic acid derivatives, which permeate through human skin at comparable rates (15–88 µg/cm2/hr). Skin irritation and pK a are correlated for pK a le 4. Laser Doppler velocimetric assessment of skin blood flow, color meter readings, erythema, edema, and the primary irritation index are all linearly correlated and related to pK a, erythema at 24 hr appears to be the most sensitive parameter to variation in pK a when pK a le 4.
Keywords:skin irritation  pK a  pH  skin permeation  chemical structure/irritation
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