Elewski Boni E
Department of Dermatology, University of Alabama School of Medicine, Birmingham, AL 35294-0009, USA.
Adv Ther. 2007 Mar-Apr;24(2):239-46. doi: 10.1007/BF02849891.
Topical formulations containing identical active agents are available in various vehicles and concentrations, which may affect percutaneous absorption. This study was undertaken to evaluate the in vitro percutaneous absorption pharmacokinetics of metronidazole in different vehicles and concentrations as the active agent in 6 topical formulations. Formulations were applied to sections from 3 cadaver skin donors, and percutaneous absorption of metronidazole was measured over a 48-h test period through the finite dose technique and the use of Franz diffusion cells. Metronidazole penetrates into and through human cadaver skin. Data show the general ranking of delivery of similar concentrations of metronidazole according to vehicle as cream > lotion > gel. The 48-h penetration of metronidazole in the human cadaver skin model was greatest with cream formulations and lowest with gel formulations. These results reveal the importance of the vehicle selected for penetration of metronidazole into the skin. The relevant target zone in rosacea is the dermis because this is the area where inflammation takes place. Additional studies are warranted to examine absorption of metronidazole into the relevant target zone and the correlation of absorption with efficacy.
含有相同活性剂的局部用制剂有多种赋形剂和浓度可供选择，这可能会影响经皮吸收。本研究旨在评估甲硝唑作为6种局部用制剂中的活性剂，在不同赋形剂和浓度下的体外经皮吸收药代动力学。将制剂应用于3名尸体皮肤供体的皮肤切片上，并通过有限剂量技术和使用Franz扩散池，在48小时的测试期内测量甲硝唑的经皮吸收情况。甲硝唑可渗透进入并穿过人体尸体皮肤。数据显示，根据赋形剂不同，相似浓度甲硝唑的释放总体排序为乳膏>洗剂>凝胶。在人体尸体皮肤模型中，甲硝唑在乳膏制剂中的48小时渗透率最高，在凝胶制剂中最低。这些结果揭示了选择赋形剂对甲硝唑渗透进入皮肤的重要性。酒渣鼻的相关靶区是真皮，因为这是炎症发生的部位。有必要进行进一步研究，以考察甲硝唑在相关靶区的吸收情况以及吸收与疗效的相关性。
