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目的:建立丹参酚酸B的反相高效液相色谱分析方法,并对其在大鼠体内的药代动力学行为特性进行全面的分析研究。方法:生物样品采用液-液萃取方法,以Hypersil C18ODS色谱柱(200 mm×4 .6 mm,5μm) ,柱温40 ℃,流动相:乙腈水=20 80(含0 .25 mol/L乙酸胺) ,用磷酸调pH至4 .0 ,流速:1 .0 mL/min;紫外检测波长:328 nm。结果:鼠尾静脉给予丹参酚酸B1 .6、3 .2、6 .4 mg/kg后,结果显示鼠α相半衰期为(3 .1±0 .1) min,β相半衰期为(31 .5±3 .2) min。大鼠尾静脉给予丹酚酸B后,组织中浓度依次为(高→低) :心、肝、肺、小肠、肾脏、脾、胃、卵巢和脑组织。丹参酚酸B在粪便和尿中24 h及胆汁中2 h的累积排泄百分数分别约为1.43 %、0.77 %及8 .03%。丹参酚酸B人血浆蛋白结合率和大鼠血浆蛋白结合率分别为89 .2 %±1 .8 %和92 .5 %±1 .5 %。结论:本法准确、稳定、灵敏度高,适合生物样品中丹参酚酸B的分析。丹参酚酸B在大鼠体内消除速度快,血浆蛋白结合率较高,胆汁为其主要排泄途径。
Objective: To establish a reversed-phase high performance liquid chromatographic method for the analysis of salvianolic acid B, and to conduct a comprehensive analysis of its pharmacokinetic behavior in rats. METHODS: The biological samples were extracted by liquid-liquid extraction with Hypersil C18 ODS column (200 mm×4.6 mm, 5μm), column temperature 40 °C, mobile phase: acetonitrile water = 20 80 (containing 0.25 mol/L acetic acid Amines), pH adjusted to 4.0 with phosphoric acid, flow rate: 1.0 mL/min, UV detection wavelength: 328 nm. RESULTS: After administration of salvianolic acid B1 .6, 3.2, and 6.4 mg/kg in tail vein of rats, the results showed that the alpha phase half life of mice was (3.1 ± 0.1) min, and the half life of β phase was (31. 5±3 .2) min. After salvianolic acid B was administered to the tail vein of rats, the concentrations in the tissues were (high → low): heart, liver, lung, small intestine, kidney, spleen, stomach, ovary and brain. The cumulative excretion rates of salvianolic acid B in feces and urine 24 h and bile 2 h were approximately 1.43%, 0.77%, and 8.3%, respectively. The plasma protein binding rate of rat salvianolic acid B and rat plasma protein binding were 89.2%±1.8% and 92.5%±1.5%, respectively. Conclusion: This method is accurate, stable, and high sensitivity, suitable for analysis of salvianolic acid B in biological samples. Salvianolic acid B is rapidly eliminated in rats and has a high plasma protein binding rate. Bile is the main excretion route.