【摘要】 利用元素分析、IR1、H-NMR和13C-NMR等方法对比索洛尔(BSP)的结构进行了表征,并研究了促渗剂对比索洛尔贴剂(BSP-TTS)体外透皮性能的影响。以离体豚鼠皮肤为透皮屏障,采用改进的Franz扩散池,通过体外渗透性实验对含不同促渗剂的几组BSP-TTS进行了透皮性能的研究。结果表明:体外渗透曲线符合零级方程(Q=k.t),含3%月桂氮酮(Azone)和10%肉豆蔻酸异丙酯(IPM)的复合促渗剂的BSP-TTS具有良好的透皮性能。将加入复合促渗剂的贴剂中BSP的透皮速率与不加促渗剂贴剂的透皮速率比较,贴剂中药物的透皮性能有明显提高。更多还原

【Abstract】 The structure of bisoprolol was confirmed by elemental analysis,IR,（）¹H-NMR and（）¹³C-NMR.The effect of penetration enhancers on the percutaneous permeability of a bisoprolol transdermal therapeutic system patch（BSP-TTS） was assessed.The transdermal delivery characteristics of BSP-TTS patches containing different kinds of penetration enhancers were studied by a drug penetration test using excised guineapig skins in modified Franz diffusion cells.The analysis was carried out using HPLC.Various penetration enhancers showed different effects in BSP-TTS patches.In vitro permeation curves were found to conform to zero-order behavior（（Q=）k·t）.The permeation rate of a BSP-TTS patch containing 10% isopropyl myristate（IPM） and 3% 1-dodecylazacycloheptan-2-one（Azone） showed a significant enhancement compared with that without any enhancers.更多还原