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目的:测定大蒜辣素与大鼠及人血浆的蛋白结合率,为大蒜辣素的成药性研究提供参考。方法:以羟苯乙酯为替代对照品,采用C_(18)色谱柱,流动相甲醇-1%甲酸梯度洗脱,流速1.0 m L·min~(-1),检测波长254 nm,结合超滤法对大蒜辣素与大鼠及健康人血浆的蛋白结合率进行测定。结果:测得75,150,300 mg·L~(-1)大蒜辣素溶液与大鼠和人血浆蛋白结合率分别为23.2%,19.8%,28.1%及15.5%,25.8%,40.0%。结论:大蒜辣素与大鼠及人的血浆蛋白结合率均较低,替代对照品HPLC可用于测定大蒜辣素的血浆蛋白结合率。
OBJECTIVE: To determine the protein binding rate of allicin to rat and human plasma, and provide a reference for the study of allicin of allicin. METHODS: Hydroxyphenylacetate was used as a reference substance. The mobile phase was eluted with a mobile phase of methanol - 1% formic acid at a flow rate of 1.0 mL · L -1 on a C 18 column with a detection wavelength of 254 nm. Filter method of allicin and rat and healthy plasma protein binding rate was determined. Results: The binding rates of 75, 150 and 300 mg · L -1 allicin to rat and human plasma were 23.2%, 19.8%, 28.1% and 15.5%, 25.8% and 40.0%, respectively. Conclusion: Allicin has a low binding rate to plasma of rats and human. HPLC, an alternative reference substance, can be used to determine the plasma protein binding rate of allicin.