Mills P C, Magnusson B M, Cross S E
School of Veterinary Science, University of Queensland, Brisbane, Qld 4072, Australia.
Res Vet Sci. 2004 Feb;76(1):37-41. doi: 10.1016/s0034-5288(03)00142-5.
The effect of region of application on the percutaneous penetration of solutes with differing lipophilicity was investigated in canine skin. Skin from the thorax, neck, back, groin, and axilla regions was harvested from Greyhound dogs and placed in Franz-type diffusion cells. Radiolabelled (14C) ethanol (Log P 0.19) or hexanol (Log P 1.94) was applied to each skin section for a total of 5h. The permeability coefficient (kP, cm h(-1)) and residue of alcohol remaining in the skin were significantly (P=0.001) higher for hexanol compared to ethanol. In contrast, ethanol had a far greater maximum flux (Jmax, mol (cm2)(-1) h(-1)) than hexanol (P=0.001). A comparison of regional differences shows the kP and Jmax for ethanol in the groin was significantly lower (P=0.035) than the back. The kP and Jmax for hexanol were significantly higher (P=0.001) in the axilla than the other four skin sites. An understanding of factors influencing percutaneous drug movement is important when formulating topical preparations for the dog.
在犬类皮肤中研究了给药部位对不同亲脂性溶质经皮渗透的影响。从灵缇犬身上采集胸部、颈部、背部、腹股沟和腋窝部位的皮肤,并置于弗兰兹型扩散池中。将放射性标记(14C)的乙醇(Log P 0.19)或己醇(Log P 1.94)施加到每个皮肤切片上,共5小时。与乙醇相比,己醇的渗透系数(kP,cm h(-1))和残留在皮肤中的酒精残留量显著更高(P = 0.001)。相反,乙醇的最大通量(Jmax,mol (cm2)(-1) h(-1))比己醇大得多(P = 0.001)。区域差异比较表明,腹股沟部位乙醇的kP和Jmax显著低于背部(P = 0.035)。腋窝部位己醇的kP和Jmax显著高于其他四个皮肤部位(P = 0.001)。在为犬类配制局部制剂时,了解影响药物经皮移动的因素很重要。