[The effect of molecular volume and partition coefficient on percutaneous absorption].
A series of 8 p-aminobenzoate esters were selected as model drugs to study the effect of molecular volume and partition coefficient on percutaneous absorption. The octanol/water partition coefficient and solubility of these compounds were determined and their penetration rate through rat skin in vitro was measured using a Keshany-Chien diffusion cell. The results showed that when the molecular volume was increased the permeation coefficient was decreased. However, when the partition coefficient was increased, the permeation coefficient was increased at first and then reached a plateau. The mathematical formula has been derived from a bi-layer diffusion model to show how the molecular volume and the partition coefficient influence the permeation coefficient. The formula could be used to estimate the permeation coefficient of drug through skin.
Liang
W Q
WQ
Department of Pharmaceutics, Zhejiang Medical University, Hangzhou.
Lin
W
W
D010129:4-Aminobenzoic Acid / Q000493:pharmacokinetics*; D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D008433:Mathematics; D008958:Models, Molecular; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D012995:Solubility; D062366:para-Aminobenzoates
D062366:para-Aminobenzoates; D010129:4-Aminobenzoic Acid