Malbe M, Salonen M, Fang W, Oöpik T, Jalakas M, Klaassen M, Sandholm M
Department of Clinical Sciences/Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Helsinki, Finland.
Zentralbl Veterinarmed A. 1996 Aug;43(6):377-86. doi: 10.1111/j.1439-0442.1996.tb00465.x.
Enrofloxacin (Baytril) was injected into arteries supplying the udder of dairy cows. The idea was to avoid primary distribution, metabolism and elimination and thus to deliver the drug to the target organ at higher concentration. Enrofloxacin injected into the abdominal aorta or the external iliac artery resulted in high initial enrofloxacin retention by the udder and high milk concentrations. Injection of enrofloxacin into the abdominal aorta resulted in 2.2 times higher milk peak concentration of the drug than intravenous injection into the jugular vein. Injection of the drug into one of the two external iliac arteries allowed drug concentrations of milk from the udder halves to be compared: when enrofloxacin was injected into the right external iliac artery, the peak milk enrofloxacin concentration from the right udder half was 4.8 times that of the left udder half. The bulk of enrofloxacin was absorbed from the milk compartment of the udder before the next regular milking 6.5 h later. By this time, the metabolite ciprofloxacin had accumulated in milk. Pharmacokinetic values for enrofloxacin and its metabolite ciprofloxacin are given separately for serum and milk whey following three intravascular dosing routes.
恩诺沙星(拜有利)被注入供应奶牛乳房的动脉中。这样做的目的是避免药物的初次分布、代谢和消除,从而以更高的浓度将药物输送到靶器官。将恩诺沙星注入腹主动脉或髂外动脉后,乳房对恩诺沙星的初始保留率很高,且牛奶中的药物浓度也很高。将恩诺沙星注入腹主动脉所产生的牛奶中药物峰值浓度比经颈静脉静脉注射高出2.2倍。将药物注入两条髂外动脉之一,可比较来自乳房两半的牛奶中的药物浓度:当将恩诺沙星注入右髂外动脉时,右半乳房的牛奶中恩诺沙星峰值浓度是左半乳房的4.8倍。在下一次常规挤奶(6.5小时后)之前,大部分恩诺沙星已从乳房的乳区被吸收。此时,代谢产物环丙沙星已在牛奶中蓄积。分别给出了三种血管内给药途径后血清和乳清中恩诺沙星及其代谢产物环丙沙星的药代动力学值。