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目的 建立正常人血浆中巴氨西林浓度的 HPLC测定方法 ,研究巴氨西林在正常人体内的药代动力学行为。方法 采用反相高效液相色谱 -紫外检测的方法 ,测定巴氨西林在人体中的主要代谢产物氨苄西林的血药浓度。流动相 :1 1 mmol/L KH2 PO4(含 0 .1 ml/L冰醋酸 ) -甲醇 (78∶ 2 2 ,v/v)。色谱柱为 Hypersil ODS2 ,5μm,1 5 0 mm× 4 .6mm ID,紫外检测波长 2 3 1 nm。测定 2 0名男性健康志愿受试者单剂量口服 80 0 mg巴氨西林片后血药浓度 -时间过程。结果 方法的专属性较好 ,血浆中杂质不干扰样品的测定。方法的回收率大于 90 % ,日间日内变异系数低浓度小于 2 0 % ,高浓度小于 1 0 % ,线性范围 0 .3 1 6～ 2 0 .2 2 0 μg/ml(r=0 .9998,n=5 ) ,最低检测浓度 0 .3 1 6μg/ml,符合生物样品分析要求。受试者口服巴氨西林片 80 0 mg后 ,以巴氨西林体内的主要活性代谢产物氨苄西林估算的末端相半衰期 (T1 / 2 ) 1 .1 3± 0 .3 1 h,峰时间 (Tmax) 0 .81± 0 .3 0 h,峰浓度 (Cmax) 1 0 .75± 2 .5 3 μg/ml,MRT2 .0 1± 0 .4 0 h,2 1 .2 5± 4 .2 0 μg· h/ml。结论 建立的 HPLC紫外检测方法适合于巴氨西林片的临床研究。
Objective To establish a method for the determination of the concentration of bacampicillin in normal human plasma by HPLC and to study the pharmacokinetics of bacampicillin in normal human. Methods The plasma concentration of ampicillin, the major metabolite of bacampicillin in the human body, was determined by reversed-phase high performance liquid chromatography-ultraviolet detection. Mobile phase: 1 1 mmol / L KH2 PO4 (containing 0.1 ml / L glacial acetic acid) -methanol (78: 2 2, v / v). The chromatographic column was Hypersil ODS2, 5 μm, 150 mm × 4.6 mm ID, and the UV detection wavelength was 231 nm. The plasma concentration-time course was determined after a single oral dose of 80 mg bolicillin in 20 healthy male volunteers. The specificity of the results was good, and impurities in the plasma did not interfere with the determination of the sample. The recovery rate of the method was more than 90%. The daily intra-day coefficient of variation was less than 20% and the high concentration was less than 10%. The linear range was 0.31 ~ 20.22 0 μg / ml (r = 0.9998 , n = 5), the lowest detection concentration of 0.31 6μg / ml, in line with biological sample analysis requirements. After oral administration of benazolin 80 mg, the terminal half-life (T1 / 2) of the ampicillin, the major active metabolite in the bacampicillin, was 1.13 ± 0.31 h and the peak time (Tmax ) 0 .81 ± 0. 3 0 h, peak concentration (Cmax) 1 0 .75 ± 2 .5 3 μg / ml, MRT2 .0 1 ± 0. 4 0 h, 2 1 .2 5 ± 4. 2 0 μg · h / ml. Conclusion The established HPLC UV detection method is suitable for the clinical study of bafilizin tablets.