硫酸头孢喹肟在安格斯牛体内药物代谢动力学研究

Pharmacokinetics of cefquinome sulfate in Angus cattle

关键词:  硫酸头孢喹肟  高效液相色谱  药物代谢动力学  静脉注射  肌肉注射  皮下注射

Key words:  cefquinome sulfate  high performance liquid chromatography  pharmacokinetics  intravenous injection  intramuscular injection  subcutaneous injection

摘要:

为了探究硫酸头孢喹肟在安格斯牛体内的药物代谢动力学，对安格斯牛以2 mg/kg剂量分别进行静脉、肌肉、皮下注射后，于不同时间点颈静脉采血，应用HPLC测定血液中硫酸头孢喹肟的药物浓度，计算药动学参数。静脉、肌肉、皮下注射的消除半衰期（T1/2β）分别为（2.05±0.49）h、（2.17±0.51）h、（2.37±0.47）h，达峰时间（Tmax）分别为（0.75±0.25）h、（0.87±0.25）h、（1±0.37）h，达峰浓度（Cmax）分别为（7.31±1.98）μg/mL、（5.34±1.21）μg/mL、（5.16±1.29）μg/mL，药时曲线下面积（AUC）分别为（24.72±5.31）μg.h/mL、（19.97±3.11）μg.h/mL、（20.51±4.87）μg.h/mL，平均留置时间（MRT）分别为（2.83±0.61）h、（3.02±0.71）h、（3.26±0.89）h，清除率（CL）分别为（0.07±0.02）L/h.kg、（0.09±0.03）L/h.kg、（0.09±0.04）L/h.kg，表观分布容积（Vd）分别为（0.23±0.06）L/kg、（0.31±0.08）L/kg、（0.32±0.09）L/kg。肌肉、皮下注射的绝对生物利用度（F）分别为80.78%、82.96%。表明硫酸头孢喹肟在安格斯牛体内吸收快、消除慢，肌肉注射以及皮下注射的绝对利用度高。

Abstract:

After intravenous, intramuscular and subcutaneous injection of cefquiome sulfate at the dose of 2 mg/kg, plasma samples of Angus cattle was collected from jugular vein at different time points. The concentration of cefquinome sulfate in plasma samples was determined by HPLC. The concentration-time profiling of cefquinome sulfate within the plasma specimens was analyzed by the non-compartmental analysis. The elimination-half-life(T1/2β) of intravenous, intramuscular and subcutaneous injection were (2.05±0.49) h, (2.17±0.51) h, (2.37±0.47) h, respectively. The time to achieve maximum concentration (Tmax) of intravenous, intramuscular and subcutaneous injection were (0.75±0.25) h, (0.87±0.25) h, (1±0.37) h, respectively. The maximum concentration in plasma (Cmax) of intravenous, intramuscular and subcutaneous injection were (7.31±1.98) μg/mL, (5.34±1.21) μg/mL, (5.16±1.29) μg/mL, respectively. The area under the concentration-time curve (AUC) of intravenous, intramuscular and subcutaneous injection were (24.72±5.31) μg.h/mL, (19.97±3.11) μg.h/mL, (20.51±4.87 ) μg.h/ mL, respectively. The mean residence time (MRT) of intravenous, intramuscular and subcutaneous injection were (2.83±0.61) h, (3.02±0.71) h and (3.26±0.89) h, respectively.The clearance (CL) of intravenous, intramuscular and subcutaneous injection were (0.07±0.02) L/h.kg, (0.09±0.03) L/h.kg and (0.09±0.04) L/h.kg, respectively. The apparent volume of distribution (Vd) of intravenous, intramuscular and subcutaneous injection were (0.23±0.06) L/kg, (0.31±0.08) L/kg and (0.32±0.09) L/kg, respectively. The absolute bioavailability (F) of intramuscular and subcutaneous injection were 80.78% and 82.96% respectively. The results showed that cefquinome sulfate has the characteristics of rapid absorption and slow elimination in Angus cattle. The absolute bioavailability of intramuscular and subcutaneous injection was high.