盐酸小檗碱烷基化衍生物表观油水分配系数的测定  

Determination of Oil-Water Partition Coefficient of Alkylated Derivatives of Berberine

作　　者：郑珊[1] 陈超[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：《西南大学学报（自然科学版）》2015年第12期173-177,共5页Journal of Southwest University(Natural Science Edition)

基　　金：国家科技部十二五科技支撑项目(2011BAI13B02-4)

摘　　要：目的:为了小檗碱烷基化衍生物在体内的吸收、分布、代谢和制剂处方的进一步研究奠定基础,试验考察了小檗碱烷基化衍生物在正辛醇-水中的表观油水分配系数.方法:以紫外分光光度法测定小檗碱烷基化衍生物的含量,采用经典摇瓶法测定小檗碱烷基化衍生物在正辛醇-水中的表观油水分配系数.结果:在37℃下,随着烷基碳链的延伸和增加,衍生物的表观油水分配系数越大,并与烷基碳链中碳原子的个数呈现较好的线性关系.其中以目前合成的8-二十二烷基小檗碱的表观油水分配系数最大.结果提示可以通过小檗碱的烷基化结构改造影响小檗碱及其衍生物的体内代谢过程,增加体内吸收和扩大分布,并有望在小檗碱衍生物中获得新药.In order to understand the absorption,distribution and metabolism of the alkylated derivatives of berberine in vivo and lay a foundation for the further study of its preparation,their apparent oil-water partition coefficient in the n-octanol-water systems was investigated.The concentration of alkylated derivatives of berberenine hydrochloride was determined by UV,and their apparent oil-water partition coefficient was measured by the shaking flask method.The results indicated that the apparent oil-water partition coefficient of alkylated derivatives increased with the extension of the alkyl chain and showed a good linear relationship with the number of carbon atoms in it.The 8-docosyl berberine hydrochloricde synthesized at the present time had the highest partition coefficient in water at 37℃.This result suggested that the in vivo distribution process of berberine and its derivatives could be affected by improving its alkylation structure,which also could enhance its in vivo absorption and enlarge its distribution.So it is possible to develop a new drug from berberine derivatives.

关 键 词：小檗碱烷基化衍生物 表观油水分配系数 

分 类 号：R917[医药卫生—药物分析学]