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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.
OBJECTIVE: To establish a basis for the further study of the absorption, distribution, metabolism and formulation prescription of alkylated derivatives of berberine in vitro. The experimental study investigated the apparent oil-water partition of alkylated derivatives of berberine in n-octanol-water Coefficient.METHODS: The content of alkylated derivatives of berberine was determined by ultraviolet spectrophotometry and the apparent oil-water partition coefficient of alkylated derivatives of berberine in n-octanol-water was determined by classical shake flask method.RESULTS: At 37 ℃, with the extension and increase of alkyl carbon chain, the apparent oil-water partition coefficients of the derivatives are larger, and have a good linear relationship with the number of carbon atoms in the alkyl carbon chain. The apparent oil-water partition coefficients of 8-docosylberberry are the highest.The results suggest that the in vivo metabolism of berberine and its derivatives can be affected by the alkylation structure of berberine and increase the absorption and expansion in vivo Distribution, and is expected to berberine derivatives to obtain new drugs.