
doi: 10.1007/bf00371943
pmid: 2128017
Percutaneous absorption of five compounds was studied in the hairless rat in vivo: benzoic acid, caffeine, hydrocortisone, inulin and thiourea. The results clearly demonstrate that, as with in vitro experiments, a steady-state flux can be achieved in vivo. This steady-state flux is strongly molecule dependent. Thus, the values for inulin and benzoic acid differ by a factor of about 40. In contrast, although the physicochemical properties of the studied compounds vary widely, their lag times were not significantly different. The mean lag time was 11 +/- 2 min. Different compounds could be considered to have approximately the same apparent diffusion coefficient with regard to their percutaneous absorption in vivo. Thus, for a given thickness of stratum corneum and a given anatomical site, the penetration flux value of a substance depends only on its stratum corneum/vehicle partition coefficient. Using a classical model, we have demonstrated that the amount of substance present in the stratum corneum (Qsc) at equilibrium (30 min) is related to this partition coefficient. There is also a linear relationship between steady-state flux and Qsc. In practice, the in vivo steady-state flux of penetration of a compound can be predicted from the simple measurement of the amount present in the stratum corneum after a contact time of 30 min.
Hydrocortisone, Skin Absorption, Inulin, Thiourea, Rats, Inbred Strains, Benzoic Acid, Benzoates, Models, Biological, Rats, Solubility, Caffeine, Animals, Female, Epidermis, Pharmaceutical Vehicles
Hydrocortisone, Skin Absorption, Inulin, Thiourea, Rats, Inbred Strains, Benzoic Acid, Benzoates, Models, Biological, Rats, Solubility, Caffeine, Animals, Female, Epidermis, Pharmaceutical Vehicles
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