苯环喹溴铵血浆蛋白结合率测定

为了测定苯环喹溴铵大鼠和人的血浆蛋白结合率,将大鼠和人的血浆样品加入内标后用甲醇直接沉淀法进行LC/ESI/MS分析,然后采用平衡透析法测定大鼠和人血浆中苯环喹溴铵的血浆蛋白结合率。结果表明,苯环喹溴铵大鼠血浆中药物浓度为105.2~1842ng/ml,血浆蛋白结合是线性的,苯环喹溴铵与大鼠血浆蛋白结合率约为42.0%;苯环喹溴铵人血浆中药物浓度为305.3~3813ng/ml,血浆蛋白结合是线性的,与人血浆蛋白结合率约为71.4%。苯环喹溴铵在不同种属中的血浆蛋白结合率是不同的,与人的血浆蛋白结合率较大鼠的血浆蛋白结合率高,且与人的血浆蛋白具有中等强度的结合。

Determination of Plasma Protein Binding Rate of Bencycloquidium Bromide

The plasma protein binding rate of bencycloquidium bromide of rats and human were determined.After addition of internal standard, the plasma samples were deproteinized with methanol, and the supernatant was assayed by LC/ESI/MS.Equilibrium dialysis was employed to determine the plasma protein binding rate of bencycloquidium bromide in rats and human.The plasma protein binding rate of bencycloquidium bromide with rats and human plasma were 42.0% and 71.4%,respectively.The ranges of plasma concentration of bencycloquidium bromide were 105.2 to 1842 ng/ml for rats and 305.3 to 3813 ng/ml for human,respectively,in which the plasma protein binding was linear.The plasma protein binding rate of bencycloquidium bromide in various species was different.The plasma protein binding rate of bencycloquidium bromide in human was greater than in rats and the binding rate of bencycloquidium bromide with human plasma protein was middling strength.