pH值对盐酸小檗碱烷基化衍生物表观油水分配系数的影响  

Effect of pH value on oil-water partition coefficient of alkylated derivatives of berberine

作　　者：陈超[1] 郑珊[1] 胡宇莉[1,2] 李学刚[1] 曾忠良[1] 

机构地区：[1]西南大学药学院中医药学院,重庆400715 [2]重庆市动物疫病预防控制中心,重庆401120

出　　处：《中兽医医药杂志》2014年第4期11-13,共3页Journal of Traditional Chinese Veterinary Medicine

基　　金：国家科技部"十二五"科技支撑项目(2011BAI13B02-4)

摘　　要：目的:探讨pH值和结构修饰对盐酸小檗碱及其烷基化衍生物表观油水分配系数(P)的影响。方法:建立紫外分光光度法测定盐酸小檗碱及其烷基化衍生物含量的检测方法,并采用摇瓶法测定盐酸小檗碱及其烷基化衍生物在正辛醇-缓冲液体系中的表观油水分配系数。结果:pH值在2.0-8.0时,小檗碱lgP值均小于0,且其在水中的lgP值最小。小檗碱衍生物lgP值均大于0,但变化不大;随着修饰碳链的延伸,其油水分配系数逐渐增大,8-十六烷基小檗碱lgP值在不同pH值条件下均大于1,推测其在胃肠道的吸收优于小檗碱。结论:37℃下,pH值对盐酸小檗及其碱衍生物的表观油水分配系数影响不大,但与其结构改造中引入基团的极性呈正相关。Objective： To investigate the effect of pH vMue and structural transformation on the apparent oil-water partaion coefficient of alkylated derivatives of berberine in n-octanol-buffer systems. Methods： The concentration of alkylated derivatives of berberenine hydrochloride was determined by UV, and its apparent oil-water partition coefficient in n-octanol- buffer systems was measured by shaking flask method. Results： When the pH value of the buffer solution was in the range of 2.0 to 8.0, the lgP of berberine was less than 0, moreover, it was the lowest in the water. While the lgP of alkylated derivatives of berberine was greater than zero, moreover, it was increased with the extension of alkyl chain. The lgP of 8-cetyl berberine was always more than one under different pH Condition, from which we can surmise that 8-cetyl berberine would be easier absorbed in gastrointestinal tract than berberine. Conclusion： The apparent oil-water partition coefficient of alkylated derivatives of berberine was hardly affected by pH value, but positively correlated with the introduction of the structural transformation of polar groups.

关 键 词：盐酸小檗碱烷基化衍生物 PH值 表观油水分配系数 

分 类 号：S853.7[农业科学—临床兽医学]