超滤法结合HPLC测定连翘苷的血浆蛋白结合率

Determination of Plasma Protein Binding Rate of Phillyrin by Ultrafiltration and HPLC

血浆蛋白结合率是药代动力学参数之一,对于连翘苷新药研发具有重要意义。本实验采用超滤法结合HPLC测定连翘苷在大鼠血浆中的游离型药物浓度,考察连翘苷的血浆蛋白结合率。结果发现当连翘苷在大鼠血浆中的血药浓度分别为10、20、40μg/mL时,与大鼠的血浆蛋白结合率分别为(62.78±2.69%),(62.61±2.73%),(60.07±2.81%)。建立的连翘苷血浆蛋白结合率测定方法符合生物药物分析要求,连翘苷与大鼠血浆蛋白结合属于中等强度结合,且无浓度依赖性。

Plasma protein binding rate is one of the pharmacokinetic parameters, which plays an important role in the development of phillyrin. The concentration of phillyrin in rat plasma was determined by ultrafiltration combined with HPLC, and the plasma protein binding rate of phillyrin was investigated. The results showed that the concentration of phillyrin in rat plasma was 10, 20 and 40 μg/mL, respectively, The protein binding rate with rat plasma was 62.78%±2.69%, 62.61%±2.73%, 60.07%±2.81%, respectively. The established method for determination of plasma protein binding rate of phillyrin met the requirements of biopharmaceutical analysis, and the binding of phillyrin with rat plasma protein was of medium intensity without concentration dependence.