比索洛尔的结构表征及其透皮性能研究  

Structure characterization and percutaneous permeability of bisoprolol

作　　者：张钧[1] 杜洪光[1] 张恩宏[2] 柯光明[1] 王丽[2] 王树明[2] 

机构地区：[1]北京化工大学理学院,北京100029 [2]北京康倍得医药技术开发有限公司,北京100089

出　　处：《北京化工大学学报（自然科学版）》2006年第4期65-69,共5页Journal of Beijing University of Chemical Technology(Natural Science Edition)

基　　金：国家'863'计划(2004AA2Z3073)

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。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.

关 键 词：比索洛尔 结构表征 促渗剂 经皮渗透 

分 类 号：TQ460.7[化学工程—制药化工]