Barry B W, Harrison S M, Dugard P H
J Pharm Pharmacol. 1985 Feb;37(2):84-90. doi: 10.1111/j.2042-7158.1985.tb05012.x.
This work tested the potential for predicting percutaneous absorption rates of a volatile penetrant from any vehicle by using thermodynamic activity measurements. Benzyl alcohol was chosen as a non-ideal, hydrogen bonding, volatile model penetrant. A manual headspace gas chromatography method measured benzyl alcohol vapour concentrations and thermodynamic activities above binary mixtures with vehicles: butanol, butyl acetate, isopropyl myristate, isophorone, toluene and propylene carbonate. Benzyl alcohol vapour diffusion through human, abdominal skin was also measured in-vitro for these mixtures. The benzyl alcohol vapour flux was linearly related to the activity, suggesting that percutaneous absorption is controlled by thermodynamic activity when the vehicle has no effect on the stratum corneum barrier.
本研究通过测量热力学活性,测试了利用其预测挥发性渗透剂在任何载体中的经皮吸收率的可能性。选择苯甲醇作为一种非理想的、具有氢键作用的挥发性模型渗透剂。采用手动顶空气相色谱法测定了苯甲醇在与载体(丁醇、乙酸丁酯、肉豆蔻酸异丙酯、异佛尔酮、甲苯和碳酸丙烯酯)形成的二元混合物上方的蒸汽浓度和热力学活性。还体外测量了这些混合物中苯甲醇蒸汽透过人体腹部皮肤的情况。苯甲醇蒸汽通量与活性呈线性关系,这表明当载体对角质层屏障无影响时,经皮吸收受热力学活性控制。