Aim To study the excretion of(-)-clausenamide in rats.Methods The urine,feces and bile were collected at predetermined time points after(-)-clausenamide was orally administrated to 6 rats(30 mg·kg^-1).The concentrations of(-)-clausenamide and its metabolite 6-OH-(-)-clausnamide were determined by HPLC-MS/MS method using glipzide as the internal reference,and the accumulative excretion amount of(-)-clausenamide and 6-OH-(-)-clausenamide was calculated in the urine,feces and bile,separately.Results(-)-Clausenamide was recovered mostly(44%) from feces in 112 hours,7.1% was found from urine in 120 hours and 0.013% was detected from bile in 24 hours.The accumulative excretions of 6-OH-(-)-clausenamide were 0.92%,0.46% and 0.0003% of the administered dose from feces,urine and bile,respectively.Conclusion The major amount of(-)-clausenamide was recovered from feces after(-)-clausenamide was orally administrated to rats(30 mg·kg^-1).
目的研究利可君的4个非对映异构体及其有关物质的结构。方法利用液相色谱-二极管阵列检测、液相色谱-串联质谱和液相色谱-核磁共振等联用技术研究利可君及有关物质的结构。采用Phenomnex Luna C18色谱柱(250 mm×4.60 mm ID,5μm),水-乙腈-冰醋酸(58∶42∶0.3)为流动相。结果确定了在溶液状态下利可君及其有关物质的结构,发现其均有4个非对映异构体;还对利可君的4个非对映异构体在溶液中互变与稳定性进行比较与量子化学计算,证明其稳定构型为3R4S5R。结论利可君在溶液中非对映异构体相互转化,有一种优势构型。
