目的 比較草烏甲素在不同方式制備的家兔破損皮膚體外滲透速率的差異,了解皮膚破損方式對(duì)草烏甲素透過率的影響.方法 結(jié)合組織病理學(xué)檢查,對(duì)所獲破損皮膚的破損程度進(jìn)行判斷,同時(shí)采用改良Franz擴(kuò)散池裝置進(jìn)行透皮試驗(yàn),以草烏甲素含量為考察指標(biāo),HPLC-MS/MS法測(cè)定接受液中指標(biāo)性成分含量.結(jié)果 針頭劃傷、砂紙打磨、4% Na₂S脫毛劑處理這3種方式均能得到不同損傷程度的破損皮膚;組織病理學(xué)檢查顯示砂紙打磨至皮膚發(fā)紅時(shí),破損程度比較適宜,局部表皮缺失,真皮完好.三者滲透速率常數(shù)存在明顯差別,分別為96.82、210.2、2.821 ng/(cm∙h),以砂紙打磨所獲破損皮膚的滲透速率常數(shù)最大.結(jié)論 砂紙打磨可以獲得較好的破損皮膚模型,該模型對(duì)藥物透過率影響較小.

Objective To research the effects of permeation on the damaged ways of skin, and compare the permeation rates in vitro of damaged skin prepared by different ways on rabbits. Methods We judged the injured degree of damaged skin by combining with histopathological examination. We developped the transdermal tests by using modified Franz diffusion cells, and used content of bulleyaconitin A as a index to determine the content of bulleyaconitin A in accepting liquid by using HPLC-MS/MS. Results The damaged skins of different levels were dealled by three different ways: needle scratches, sandpaper polished, and 4% Na₂S depilatory. The histopathological results indicated that extent of damage by sandpaper polished was more appropriate, and in which created deleted partial epidermis and intact dermis. There were obvious differences among the three permeation rate constants, respectively, 96.82, 210.2, 2.821 ng/(cm∙h). The maximum one was obtained with sandpaper polished skin. Conclusion The better model of damaged skin was obtained with sandpaper polished because of the less influence factors of drug permeability.