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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 value and structure modification on apparent oil-water partition coefficient (P) of berberine hydrochloride and its alkylated derivatives. Methods: A UV spectrophotometric method for the determination of berberine hydrochloride and its alkylated derivatives was established. The contents of berberine hydrochloride and its alkylated derivatives in n-octanol-buffer system were determined by shake flask method Apparent oil-water partition coefficient. Results: The lgP values of berberine were all less than 0 at pH 2.0-8.0, and the lgP value of water was the lowest. Berberine derivatives lgP values are greater than 0, but little change; with the extension of the modified carbon chain, the oil-water partition coefficient gradually increased, 8-cetyl-berberine lgP values at different pH values Greater than 1, presumably its absorption in the gastrointestinal tract is superior to berberine. Conclusion: At 37 ℃, pH value has little effect on the apparent oil-water partition coefficients of barberry and its derivatives, but positively correlates with the polarity of the introduced groups.