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引用本文:凌伟,唐静怡,石磊,戴智勇,徐智.pH值对吲哚美辛芳基吗啉酯衍生物表观油水分配系数的影响[J].中国现代应用药学,2011,28(10):903-906.
LING Wei, TANG Jingyi, SHI Lei, DAI Zhiyong, XU Zhi.Effect of pH on Apparent Oil/Water Partition Coefficient of Prodrugs of Indomethacin[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(10):903-906.
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pH值对吲哚美辛芳基吗啉酯衍生物表观油水分配系数的影响
凌伟,唐静怡,石磊,戴智勇,徐智1,2,3
1.中南大学湘雅医院,长沙 410008;2.中南大学药学院,长沙 410013;3.湖南大学化学化工学院,长沙 410082
摘要:
目的 测定盐酸吲哚美辛芳基吗啉酯衍生物的表观油水分配系数并探讨pH值和结构改造对其的影响。方法 用摇瓶法测定盐酸吲哚美辛芳基吗啉酯衍生物在正辛醇缓冲液体系中的表观油水分配系数,建立紫外分光光度法测定其含量。结果 25 ℃时盐酸吲哚美辛芳基吗啉酯衍生物在pH为4时其表观油水分配系数最大。结论 盐酸吲哚美辛芳基吗啉酯衍生物的表观油水分配系数与介质的pH和结构改造中引入基团的极性等因素有关。
关键词:  盐酸吲哚美辛芳基吗啉酯衍生物  表观油水分配系数  酸碱度  引入基团
DOI:
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基金项目:2009年度湖南省长沙市重点项目K0901077-31
Effect of pH on Apparent Oil/Water Partition Coefficient of Prodrugs of Indomethacin
LING Wei, TANG Jingyi, SHI Lei, DAI Zhiyong, XU Zhi1,2,3
1.Department of Pharmacy of Xiangya Hospital, Central South University, Changsha 410008, China;2.College of Pharmacy, Central South University, Changsha 410013, China;3.College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China
Abstract:
OBJECTIVE To study the effect of pH on apparent oil/water partition coefficient of prodrugs of indomethacin. METHODS The apparent oil/water partition coefficient of prodrugs of indomethacin was measured by shaking flask method. The concentration of prodrugs of indomethacin was determined by UV. RESULTS When the temperature was 25 ℃, the prodrugs of indomethacin have the highest partition coefficients in n-octanol/pH 4 buffer solution system. CONCLUSION The apparent oil/water partition coefficients of prodrugs of indomethacin are correlated to pH of the medium and the polarity of group which is added.
Key words:  prodrug of indomethacin  apparent oil/water partition coefficient  pH  added group
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