【摘要】 为了研究阿莫西林-克拉维酸钾可溶性粉在猪体内的药代动力学特征,笔者以12.5 mg/kg·bw剂量单次给猪灌服阿莫西林-克拉维酸钾可溶性粉,于给药前和给药后特定时间点采集血浆样品,采用UPLC-MS/MS法测定血浆药物浓度,并使用WinNonlin R 8.1软件进行非房室模型分析。内服给药后,阿莫西林和克拉维酸的T1/2无显著差异(分别为1.14±0.24 h和1.32±0.29 h),二者的Cmax分别为2.58±0.67μg/mL和1.91±0.28μg/mL,Tmax分别为1.67±0.34 h和1.46±0.10 h,AUClast分别为7.33±1.80 mg·h/L和4.98±0.67 mg·h/L。阿莫西林和克拉维酸的平均内服生物利用度分别为23.0%和26.4%。试验结果说明,本研究建立的检测方法灵敏度高、干扰少,适用于猪血浆中阿莫西林-克拉维酸钾的检测;药代动力学研究表明2种药代谢快,在猪体内的停留时间较短。更多还原

【Abstract】 Pharmacokinetic characteristics of amoxicillin and clavulanate potassium in pigs was studied, amoxicillin and clavulanate potassium were given intravenously and orally at 12.5 mg/kg BW, respectively. Plasma samples were collected at specific time, used UPLC-MS/MS method to detect. Plasma concentrations were determined using Win NonlinR6.4.0 non-compartment model analysis.The results showed that after oral administration, there was no significant difference between amoxicillin and clavulanate potassium T1/2(1.14±0.24 h and 1.32±0.29 h, respectively). And Cmax were 2.58±0.67 g/m L and 1.91±0.28 g/m L, Tmax were 1.67±0.34 h and 1.46±0.10 h, AUClast were 7.33±1.80 mg/L and 4.98±0.67 mg/L. The average internal bioavailability of amoxicillin and clavulanate potassium were 23% and 26.4%, respectively. The results indicated that the detection method established in this study had high sensitivity and less interference, and was suitable for the detection of amoxicillin and clavulanate potassium in plasma. Pharmacokinetic studies showed that amoxicillin and clavulanate potassium were metabolized quickly and stayed in pigs for a short time.更多还原