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机构地区:[1]南京师范大学化学与材料科学学院,南京210023 [2]河北医科大学药学院,石家庄050017
出 处:《中国药房》2013年第41期3868-3870,共3页China Pharmacy
基 金:河北省教育厅2009年科学研究计划项目(No.2009148)
摘 要:目的:测定双苯氟嗪的解离常数(pKb)和油水分配系数(lgP)。方法:采用非对数滴定法,以不同比例的乙醇-水(70∶30、60∶40、50∶50、40∶60,V/V)为溶剂配制不同浓度(0.01、0.02、0.03 mmol/L)的双苯氟嗪溶液,用盐酸溶液滴定,经数学计算推算出双苯氟嗪的pKb;以正辛醇-水为模拟系统,采用摇瓶法-紫外分光光度法测定油水分配平衡(正辛醇与水相体积比为1∶1、1∶3)后双苯氟嗪的浓度,计算双苯氟嗪的lgP。结果:双苯氟嗪的pKb为8.11;正辛醇与水相体积比为1∶1、1∶3时双苯氟嗪的lgP分别为0.59±0.038、0.85±0.046。结论:双苯氟嗪属于脂溶性强的药物。OBJECTIVE: To determine the dissociation constant (pK) and oil/water partition coefficient (lgP) of dipfluzine. METHODS: The pKb of dipfluzine was determined by non-logarithmic potentiotitration method. Different proprotions of ethanol-wa- ter mixtures (70 : 30, 60 : 40, 50 : 50, 40 : 60, V/V) were used to prepare different concentrations of dipfluzine solutions (0.01, 0.02 and 0.03 mmol/L) which were titrated by hydrochloric acid solution. Using n-octyl alcohol-water simulation system, the concentra- tion of dipfluzine was determined and lgP of dipfluzine was calculated by shake flask-ultraviolet spectrophotometry after balancing oil/water partition (volume ratio of n-octyl alcohol to water as 1 : 1 and 1:3). RESULTS: The pKb of dipfluzine was 8.11; lgP of dipfluzine were 0.59 ± 0.038 and 0.85 ± 0.046 when the volume ratio of n-octyl alcohol to water was 1 : 1 and 1 : 3, respectively. CONCLUSIONS: Dipfluzine is fat soluble drug.
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