Estimation of Blood Concentration of Drugs after Topical Application from in Vitro Skin Permeation Data. I. : Prediction by Convolution and Confirmation by Deconvolution

概要

論文の詳細を見る
A new theoretical expression is derived to estimate the rate and amount of the in vivo percutaneous absorption of drugs from in vitro skin permeation data. Based on two assumptions, that the skin permeation rate of the drug in the in vivo experiment is equal to that in vitro and that the drug elimination follows linear kinetics, the time course of the blood (total blood, plasma or serum) concentration of the drug after topical application could be expressed as a convolution equation. Based on the same concept, the permeation rates in in vitro and in vivo experiments are also compared by means of a deconvolution equation.In the present study, nicorandil was selected as a model drug. The simulated plasma nicorandil level vs. time curve from the in vitro permeation study was approximately fitted to the in vivo experimental data in hairless rats, particularly up to 10h. This method was valuable to estimate the time course of plasma concentration after topical application within the range of acceptable variation from the results of in vitro permeation experiments. Some difference between the observed and calculated plasma levels might be due to differences of the skin condition and so on in the in vitro and in vivo experiments.
1988-06-25