Feldstein M M, Raigorodskii I M, Iordanskii A L, Hadgraft J
Lekbiotech R&D Center, 'Biotechnologia' JSCo., Moscow, Russia.
J Control Release. 1998 Mar 2;52(1-2):25-40. doi: 10.1016/s0168-3659(97)00208-3.
A comparative study of the barrier function of human skin and polydimethylsiloxane-polycarbonate block copolymer Carbosil membrane was performed in vitro using 14 drugs spanning a wide range of structures and therapeutic classes. The drug permeability coefficients across the skin and the Carbosil membrane wee examined as an explicit dependence of permeant molecular weight, melting point, solubility in aqueous solution in aqueous solution and octanol-water partition coefficient. Owing to heterophase and heteropolar structure, Carbosil membranes and human skin epidermis share a common solubility-diffusion mechanism of drug transport. This synthetic membrane is shown to provide a mechanistically substantiated model for percutaneous drug absorption. Carbosil membrane can be used both foe quantitative prediction for transdermal drug delivery rate and as a skin-imitating standard membrane in the course of in vitro drug delivery kinetics evaluation.
使用14种结构和治疗类别广泛的药物，在体外对人体皮肤和聚二甲基硅氧烷 - 聚碳酸酯嵌段共聚物Carbosil膜的屏障功能进行了比较研究。研究了药物在皮肤和Carbosil膜上的渗透系数与渗透物分子量、熔点、在水溶液中的溶解度以及正辛醇 - 水分配系数的明确关系。由于具有异相和异极性结构，Carbosil膜和人体皮肤表皮具有共同的药物转运溶解扩散机制。这种合成膜被证明为经皮药物吸收提供了一个有机制依据的模型。Carbosil膜可用于经皮给药速率的定量预测，也可在体外药物传递动力学评估过程中作为仿皮肤标准膜。
