为建立中药复方六神丸血浆药物化学的研究方法,利用HPLC—uV技术分析比较了空白血浆、体内六神丸血浆和体外六神丸血浆样品成分的异同,鉴定了灌服六神丸后大鼠血浆中移行成分及其代谢产物的变化;检测了不同时间点体内六神丸血浆中成分的含量;测定了六神丸中对应成分的标准品入血后,转化为目标峰12号物质的转化率。结果表明:大鼠灌胃六神丸后,HPLC图显示15个入血成分,其中10个成分为新产生的代谢产物,5个成分可能为六神丸所合成分的原型;六神丸经大鼠体内代谢后,在血浆中被检测到的主要成分11号和12号移行成分,有良好的浓度一时间依赖性;六神丸中主要成分华蟾酥毒基、酯蟾毒配基、蟾毒灵、蟾毒它灵均转化成12号类移行成分,且12号成分的转化率为:7.48%、2.93%、0.55%、0.94%。说明了大鼠灌胃六神丸后的血中移行成分及其代谢产物,可能为六神丸在体内发挥作用的活性物质群;而六神丸入血后的代谢变化规律,将为进一步研究六神丸有效成分及作用机理奠定基础。
To develop a method to study the plasma pharmacochemistry of Liu--Shen--Wan. METHODS: Based on the HPLC--UV chromatogram, comparison was carried out among the components and contents of control plasma, plasma containing drug and Liu--Shen--Wan extraction to identify the transitional components and metabolite in the rat blood after administration of the Liu--Shen--Wan extraction. The comparison of the composition and contents of plasma at different time points after gastric perfusion was taken. Determin the conversion rates that corresponding components in Liu--Shen--Wan converted to the target peak 12 after adding standardinto the bloodstream, material. RESULTS:The source of 15 peaks have been found, 10 of them were metabolites And 5 components contain ingredi- ents of prototypes. The main metabolites were components of No. 11 and No. 12c after Liu--Shen--Wan was metabolized in mice and they have good concentration -- time dependence. The conversion rates to 12 substances of main components of Liu--Shen Wan incuding Resibufogenin,Cinobufagin,Bufalin,Cinobufotalin are 7.48%, 2.93%, 0. 55% and 0.94%, respectively. CONCLUSION : The compounds absorbed into blood and its possible metabolites are capable of being the effective constituents in Liu--Shen--Wan. The result is helpful to further study on active ingredients of Liu--Shen--Wan and action mechanism.