【摘要】 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。更多还原

【Abstract】 AIM The purpose is to establish a reversed phase HPLC method for determination of ampicillin and to study it′s pharmacokinetics in healthy subjects. METHOD S The plasma concentration of ampicillin, a main active metabolite of bac ampicillin, was determined by a HPLC method. The drug was extracted from plasma with perchloric acid. Hypersil C 18, 5 μm,150 mm×4.6 mm I.D. column was used. Mobile phase consisted of 78% 11 mmol/L KH 2PO 4 (pH 4.0)and 22% met hanol. The eluted peaks were detected by UV detector at 231 nm. The pharmacokin etics of bacampicillin in 20 healthy subjects was studied after oral administra tion of 800 mg. RESULTS The recoveries of ampicillin from plasma were larger than 90% and RSD(%) of intra-day and inter-day was smaller th an 15% . Calibration curves were linear over 0.316～20.220 μg/ml (r=0.9998,P<0.01 )and the minimum detection concentration was 0.316 μg/ml. After oral administra tion of 800 mg bacampicillin tablet in 20 men, the main pharmacokinetic paramete r s were estimated as follows:T 1/2K 1.13±0.31 h, T max 0.81 ±0.30 h,c max 10.75±2.53 μg/ml, MRT 2.01±0.40 h, and AUC\+6\-0 21.25±4.20 μg·h/ml. CONCLUSION The assay method was convenie nt for clinical study of bacampicillin.更多还原