Todo Hiroaki
Faculty of Pharmacy and Pharmaceutical Sciences, Josai University.
Nihon Yakurigaku Zasshi. 2022;157(5):335-339. doi: 10.1254/fpj.22034.
The skin is not only the site of drug application, but also the site of exposure to various chemical substances. Prediction of skin permeability, body absorption, and local skin concentration of chemicals are very important to assure efficacy and safety. Most in silico models for skin permeation of chemical are based on the prediction of its permeability coefficient (P, unit cm/s), and a certain level of prediction accuracy has been obtained. On the other hand, the amount absorbed in the body of a chemical is calculated from the sum of the amount of skin permeation and the amount under the stratum corneum (viable epidermis and dermis). The amount of skin permeation can be calculated from the P value as mentioned above, however, the amount under the stratum corneum, which is related to the local skin safety of the chemical, cannot be predicted. This article describes the principles of permeation of chemicals across the skin, the relationship between skin permeability and concentration in the skin, and the method for calculating the chemical concentration under the stratum corneum using skin permeation parameters.
皮肤不仅是药物施用的部位,也是接触各种化学物质的部位。预测化学物质的皮肤渗透性、机体吸收以及局部皮肤浓度对于确保疗效和安全性非常重要。大多数用于预测化学物质皮肤渗透的计算机模拟模型是基于其渗透系数(P,单位为cm/s)的预测,并且已经获得了一定水平的预测准确性。另一方面,化学物质在机体内的吸收量是根据皮肤渗透量和角质层以下(活性表皮和真皮)的量之和来计算的。皮肤渗透量可根据上述P值进行计算,然而,与化学物质局部皮肤安全性相关的角质层以下的量却无法预测。本文描述了化学物质透过皮肤的渗透原理、皮肤渗透性与皮肤中浓度的关系,以及使用皮肤渗透参数计算角质层以下化学物质浓度的方法。