大鼠口服泻心汤及其配伍组方中原小檗碱类成分尿排泄动力学

目的研究大鼠灌服泻心汤及其配伍组方中3种原小檗碱类生物碱(小檗碱、巴马汀、黄连碱)尿排泄动力学的变化。方法取SD大鼠20只随机分成黄连、大黄黄连、黄芩黄连、泻心汤4组,采集灌胃给药前及给药后不同时间段尿液,用HPLC法测定尿药浓度,由尿排泄-时间数据计算尿排泄动力学参数,采用方差分析比较各组中3种原小檗碱类生物碱尿排泄动力学参数的差异。结果3种原小檗碱类生物碱排泄速率常数相近,排泄半衰期为9~16h。与黄连组比较,泻心汤组、大黄黄连组、黄芩黄连组中黄连碱尿排泄量占给药量比值减少,其中泻心汤组与之比较差异具有统计学意义(P<0.05)。结论3种原小檗碱类生物碱具有类似的尿排泄特征,大黄、黄芩和黄连配伍能减少黄连碱的尿排泄量。

The urinary excretion kinetics of protoberberine alkaloids after oral administration of Xiexin decoction and different combinations of its constituent herbs in rats

Aim To investigate the urinary excretion kinetics of the three protoberberine alkaloids(berberine、palmatine、coptisine) after oral administration of Xiexin decoction(XXD) and the different combinations of its constituent herbs in rats.Methods Twenty SD rats were randomly divided into four groups: Coptis chinensis,Rhizome rhei+Coptis chinensis,Radix scutellaria+Coptis chinensis and Rhizome rhei+Radix scutellaria+Coptis chinensis(XXD).Urine was collected before and after dosing.Alkaloid concentrations in urine were determined by an HPLC-UV system.Excretion parameters were determined from urinary excretion-time data.The differences of excretion parameters of three protoberberine alkaloids among four groups were tested by one-way analysis of variance.Results Excretion constants of three protoberberine alkaloids in rat urine were similar in all groups with an excretion T12 being 9~16 h.Compared with the group of Coptis chinensis alone,the rest three groups,Rhizome rhei+Coptis chinensis,Radix scutellaria+Coptis chinensis and XXD,showed decreases in the urinary cumulative excretion amount/dosage ratio of coptisine,although only XXD group reached the significance level(P<0.05).Conclusions The results indicated that excretion characteristics of three protoberberine alkaloids in rat urine were similar and the combination of rhizome rhei and Radix scutellaria with Coptis chinensis might decrease excretion of coptisine in rat urine.