HPLC-超滤法测定雷公藤红素与家兔、大鼠、人血浆的蛋白结合率  

Determination of Plasma Protein Binding Rate of Celastrol in Rats,Rabbits and Human by HPLC-Ultrafitration

作　　者：刘鹏[1] 陈莹[1] 

机构地区：[1]中国医科大学附属第一医院,沈阳110001

出　　处：《中国药房》2015年第1期62-65,共4页China Pharmacy

摘　　要：目的：测定雷公藤红素在家兔、大鼠和人血浆中的血浆蛋白结合率。方法：采用高效液相色谱（HPLC）-超滤法分离测定游离药物和血浆蛋白结合药物。以高效液相色谱法测定离体大鼠、家兔和人血浆中雷公藤红素含量,计算血浆蛋白结合率。色谱柱为Diamonsil C18,流动相为乙腈-0.2%甲酸（80∶20,V/V）,检测波长为425 nm,流速为1.0 ml/min,进样量为10μl,柱温为40℃。结果：0.52、2.08、8.32 mg/L雷公藤红素在大鼠、家兔和人血浆中的检测质量浓度线性范围均为0.10-16.64 mg/L（r分别为0.999 5、0.999 6、0.999 5）;血浆样品精密度试验的RSD均小于15%,在37、25、4℃下1 440 min内稳定性试验的RSD均小于5%。在0.52、2.08、8.32 mg/L质量浓度下雷公藤红素与人血浆的血浆蛋白结合率分别为84.62%、81.24%、83.14%,与大鼠的血浆蛋白结合率分别为79.44%、78.61%、78.15%,与家兔的血浆蛋白结合率分别为67.86%、68.71%、69.23%。结论：雷公藤红素的血浆蛋白结合率与其质量浓度无关;雷公藤红素与人的血浆蛋白结合率较高,其次为大鼠和家兔。OBJECTIVE： To determine the plasma protein binding rate of celastrol in rabbits, rats and human. METHODS ： U1traflitration method was used to isolate and detemine free drug and plasma protein binding substance. HPLC was employed to determine the plasma concentration of celastrol in rabbits, rats and human, and then on the basis of which plasma protein binding rates were calculated. The determination was performed on Diamonsil C18 coltLmn with acetonitrile-0.2% formic acid （80：20, V/V） at the flow rate of 1.0 ml/min. The detection wavelength was set at 425 nm and the column temperature was 40℃. The sample size was 10 μl. RESULTS： The linear range of celastrol （0.52, 2.08, 8.32 mg/L） were 0.10-16.64 mg/L in plasma of rats, rabbits and human （r=0.999 5, 0.999 6, 0.999 5）. RSD of the test was lower than 15%, and RSD of stability test was lower than 5% within 1 440 min at 37, 25 and 4 %. The plasma protein binding rates of celastrol （0.52, 2.08, 8.32 mg/L） in human were 84.62%, 81.24% and 83.14%, respectively; those were 79.44%, 78.61% and 78.15% in rats, while 67.86%, 68.71% and 69.23% in rab- bits, respectively. CONCLUSIONS： The plasma protein binding rates of celastrol are not associated with drug concentration; those of celastrol in human are the highest, followed by in rats and in rabbits.

关 键 词：雷公藤红素 超滤法 高效液相色谱法 血浆蛋白结合率 体外试验 

分 类 号：R969.1[医药卫生—药理学]