摘要
目的 研究格列美脲与人血清白蛋白(humanserumalbumin,HSA)结合作用。方法 采用高效液相色谱 迎头分析法(highperformanceliquidchromatography frontalanalysis, HPLC FA)。色谱柱为内表面反相(internal surfacereversed phase,ISRP)硅胶柱PinkertonGFFII S5 80(1.50mm×4 .6mmID, 5μm);流动相为 67mmol·L-1磷酸盐等渗缓冲液 (pH 7. 4, I=0 17mol·L-1 );流速 0 2mL·min-1;检测波长 230nm;进样量 900μL;柱温37℃。结果应用非线性回归参数估算求得HSA分子上两类结合位点结合的格列美脲分子数及相应的结合平衡常数:n1 =1和K1 =5. 1 (μmol·L-1 )-1;n2 =7和K2 =0. 017 (μmol·L-1 )-1。结论 HPLC FA法操作简便,适用于研究格列美脲与HSA的结合作用。
Aim To study the protein binding of glimepiride. Methods An HPLC-FA method is performed by using Pinkerton GFF II-S5-80 internal-surface reversed-phase silica support (150 mm×4.6 mm ID, 5 μm) at pH 7.4 in a 67 mmol·L-1 isotonic sodium phosphate buffer at 37 ℃. Other conditions included flow rate of 0.2 mL·min-1, UV detection at wavelength 230 nm and injection volume 900 μL. Results Nonlinear regression parameter estimation was used for the association constant measurement of glimepiride to both primary and secondary sites, which were 5.1 (μmol·L-1)-1 and 1 for K_1 and n_1, and 0.017 (μmol·L-1)-1 and 7 for K_2 and n_2, respectively. Conclusion The method is shown to be suitable for investigation of protein binding of glimepiride.
出处
《药学学报》
CAS
CSCD
北大核心
2005年第1期39-42,共4页
Acta Pharmaceutica Sinica
关键词
格列美脲
高效液相色谱-迎头分析法
人血清白蛋白
蛋白结合作用
glimepiride
high performance liquid chromatography-frontal analysis
human serum albumin
protein binding interaction
