【摘要】 将18头健康成年中国荷斯坦奶牛随机分成高、中、低3组,每组每头分别肌肉注射氨基丁三醇前列腺素F2α注射液10(50mg),5(25mg),2.5mL(12.5mg),采用酶联免疫吸附法(ELISA)测定血药浓度,用残数法逐头奶牛拟合药动学曲线方程并计算药动学参数,研究氨基丁三醇前列腺素F2α在奶牛体内的药代动力学。结果表明,药时数据符合有吸收一室模型,高,中,低组的主要药动学参数:吸收速率常数Ka分别为(18.22±2.17),(15.30±0.64),(20.09±5.03)h-1;吸收半衰期t1/2Ka分别为(0.04±0.004),(0.05±0.002),(0.04±0.01)h;分布和消除速率常数Ke分别为(1.32±0.14),(1.27±0.12),(1.40±0.16)h-1;消除半衰期t1/2Ke分别为(0.53±0.06),(0.55±0.05),(0.50±0.06)h;达峰时间tmax均为0.17h;达峰质量浓度Cmax分别为(6.34±0.59),(5.94±0.27),(4.81±0.16)μg/L;药时曲线下面积AUC0~t分别为(14.40±2.19),(10.14±1.07),(13.15±4.34)μg/(L·h)。奶牛单剂量肌肉注射氨基丁三醇前列腺素F2α注射液后,机体对药物吸收迅速,消除快,浓度约10min达到峰值,100min后达到注射前的水平。根据药时曲线峰浓度,AUC值及相关的临床药效学试验结果,建议临床使用剂量为5mL(25mg)。更多还原

【Abstract】 To study the pharmacokinetics of prostaglandin F2αtromethamine in cows,18 healthy adult Holstein cows were divided into three groups injected with a single dose of injection of the drug 10,5,2.5 mL,respectively.ELISA was used to carry out the determination of serum drug concentration.The serum concentration-time data derived from experiments were analyzed by residual method based on statistical moment theory.The kinetics of prostaglandin F2αpromethamine was fitted to one compartment model with first order.The main parameters of the high,medium and low groups were as follows:Ka(18.22±2.17),(15.30±0.64),(20.09±5.03)h-1;t1/2Ka(0.04±0.004),(0.05±0.002),(0.04±0.01)h;Ke(1.32±0.14),(1.27±0.12),(1.40±0.16)h-1;t1/2Ke(0.53±0.06),(0.55±0.05),(0.50±0.06)h;tmax0.17h;Cmax(6.34±0.59),(5.94±0.27),(4.81±0.16)μg/L;AUC0~t(14.40±2.19),(10.14±1.07),(13.15±4.34)μg/(L·h).After treated with the prostaglandin F2αtromethamine,its concentration of the serum reached the Cmaxat 10 min,and recovered at 100 min.According to the concentration-time data and clinical pharmacodynamics studies,it is proposed that a single dose of IM injection of the drug should be 5mL(25mg).更多还原