Goudah A, Sher Shah S, Shin H C, Shim J H, Abd El-Aty A M
Department of Pharmacology, Faculty of Veterinary Medicine, Cairo University, 12211-Giza, Egypt.
J Vet Med A Physiol Pathol Clin Med. 2007 Dec;54(10):607-11. doi: 10.1111/j.1439-0442.2007.00986.x.
The aim of this investigation was to examine the pharmacokinetics and mammary excretion of erythromycin administered to lactating ewes (n = 6) by the intravenous (i.v.), intramuscular (i.m.) and subcutaneous (s.c.) routes at a dosage of 10 mg/kg. Blood and milk samples were collected at pre-determined times, and a microbiological assay method was used to measure erythromycin concentrations in serum and milk. The concentration-time data were analysed by compartmental and non-compartmental kinetic methods. The serum concentration-time data of erythromycin were fit to a two-compartment model after i.v. administration and a one-compartment model with first-order absorption after i.m. and s.c. administration. The elimination half-life (t(1/2beta)) was 4.502 +/- 1.487 h after i.v. administration, 4.874 +/- 0.296 h after i.m. administration and 6.536 +/- 0.151 h after s.c. administration. The clearance value (Cl tot) after i.v. dosing was 1.292 +/- 0.121 l/h/kg. After i.m. and s.c. administration, observed peak erthyromycin concentrations (Cmax) of 0.918 +/- 0.092 microg/ml and 0.787 +/- 0.010 microg/ml were achieved at 0.75 and 1.0 h (Tmax) respectively. The bioavailability obtained after i.m. and s.c. administration was 91.178 +/- 10.232% and 104.573 +/- 9.028% respectively. Erythromycin penetration from blood to milk was quick for all the routes of administration, and the high AUC milk/AUC serum (1.186, 1.057 and 1.108) and Cmax-milk/Cmax-serum ratios reached following i.v., i.m. and s.c. administration, respectively, indicated an extensive penetration of erythromycin into the milk.
本研究的目的是检测以10mg/kg的剂量通过静脉注射（i.v.）、肌肉注射（i.m.）和皮下注射（s.c.）途径给予泌乳母羊（n = 6）后红霉素的药代动力学及在乳腺中的排泄情况。在预定时间采集血液和乳汁样本，并采用微生物测定法测量血清和乳汁中红霉素的浓度。通过房室和非房室动力学方法分析浓度-时间数据。静脉注射后红霉素的血清浓度-时间数据符合二房室模型，肌肉注射和皮下注射后符合具有一级吸收的一房室模型。静脉注射后的消除半衰期（t(1/2β)）为4.502±1.487小时，肌肉注射后为4.874±0.296小时，皮下注射后为6.536±0.151小时。静脉给药后的清除率值（Cl tot）为1.292±0.121 l/h/kg。肌肉注射和皮下注射后，分别在0.75小时（Tmax）和1.0小时达到观察到的红霉素峰值浓度（Cmax），分别为0.918±0.092μg/ml和0.787±0.010μg/ml。肌肉注射和皮下注射后的生物利用度分别为91.178±10.232%和104.573±9.028%。对于所有给药途径，红霉素从血液到乳汁的渗透都很快，静脉注射、肌肉注射和皮下注射后达到的高乳汁AUC/血清AUC（分别为1.186、1.057和1.108）以及乳汁Cmax/血清Cmax比值表明红霉素能广泛渗透到乳汁中。
