el-Komy A A
Department of Pharmacology, Faculty of Veterinary Medicine, Zagazig University (Benha Branch), Egypt.
Dtsch Tierarztl Wochenschr. 1995 Jun;102(6):244-8.
The pharmacokinetics of piperacillin (430 mg/kg.b.wt.) and cephapirin (20 mg/kg.b.wt.) were investigated following a single intravenous and intramuscular injection in normal mares. The serum concentration-time curve following a single intravenous injection of both antibiotics obeyed a two-compartment open model. After intravenous dose, piperacillin and cephapirin were transferred from central to peripheral compartment (k12) with values 0.46 and 0.52 h-1, while their passages from peripheral to central compartment (k21) were equal to 0.56 and 0.49 h-1, respectively. The elimination half-lives [t0.5(beta)] following intravenous injection were 6.94 and 3.82 h for piperacillin and cephapirin, respectively. Piperacillin and cephapirin were cleared after intravenous injection by all clearance processes in the body (CItot.) at rates of 5.52 and 0.67 ml/min., respectively. The absorption half-lives [t0.5(ab)] of piperacillin and cephapirin following a single intramuscular injection were 0.46 and 0.88 h., respectively. The calculated maximum [Cmax.] and minimum [Cmin.] serum concentrations to establish a proper multiple dosage regimen were 52.94, 4.50 micromilligrams (for piperacillin) and 10.18, 2.20 micromilligrams (for cephapirin), respectively. The mean systemic bioavailabilities of piperacillin and cephapirin following a single intramuscular injection were 85.47% and 67.89%, respectively. The in-vitro protein binding percent was 19.23% for piperacillin and 52.62% for cephapirin.
在正常母马中单次静脉注射和肌肉注射后,研究了哌拉西林(430毫克/千克体重)和头孢匹林(20毫克/千克体重)的药代动力学。两种抗生素单次静脉注射后的血清浓度-时间曲线均符合二室开放模型。静脉给药后,哌拉西林和头孢匹林从中央室向外周室的转运速率常数(k12)分别为0.46和0.52小时-1,而它们从外周室向中央室的转运速率常数(k21)分别为0.56和0.49小时-1。静脉注射后,哌拉西林和头孢匹林的消除半衰期[t0.5(beta)]分别为6.94和3.82小时。静脉注射后,哌拉西林和头孢匹林通过体内所有清除过程的清除率(CItot.)分别为5.52和0.67毫升/分钟。单次肌肉注射后,哌拉西林和头孢匹林的吸收半衰期[t0.5(ab)]分别为0.46和0.88小时。为建立合适的多剂量给药方案而计算出的最大血清浓度[Cmax.]和最小血清浓度[Cmin.],哌拉西林分别为52.94、4.50微克/毫升,头孢匹林分别为10.18、2.20微克/毫升。单次肌肉注射后,哌拉西林和头孢匹林的平均全身生物利用度分别为85.47%和67.89%。体外蛋白结合率,哌拉西林为19.23%,头孢匹林为52.62%。