比索洛尔的结构表征及其透皮性能研究

利用元素分析、IR、1H-NMR和13C-NMR等方法对比索洛尔的结构进行了表征，并研究了促渗剂对比索洛尔贴剂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比索洛尔贴剂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）的复合促渗剂的比索洛尔贴剂具有良好的透皮性能。将加入复合促渗剂的贴剂中比索洛尔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。

Structure characterization and percutaneous permeability of bisoprolol

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.