期刊
RESEARCH IN VETERINARY SCIENCE
卷 84, 期 3, 页码 477-482出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.rvsc.2007.07.003
关键词
doxycycline; calves; pharmacokinetic; sustained-release
Doxycycline hyclate (DOX-h) can be regarded as a time-dependant antibacterial. Hence, a parenteral long-acting formulation may be regarded as more pharmacologically sound. A poloxamer-based matrix was used to produce a long-acting injectable preparation (DOX-h-LA) and its serum concentrations vs. time profile investigated after its s.c. injection to calves. Serum concentrations profiles for such a prepartion were compared to the corresponding profiles obtained with an aqueous formulation of DOX-h injected either i.m. or i.v. in 10 calves in a crossover study at dose of 10 mg/kg, with washout periods. DOX-h-LA showed the greatest values for bioavailability (602%); maximum serum concentration (C(max)) value was 1.99 mu g/mL with a time to reach C(max) (T(max)) of 25 h and an elimination half-life of 40.81 h. Considering minimum effective serum concentration of 0.5 mu g/mL a dose-interval of 80 h can be achieved for DOX-h-LA, and only 9.7 h and 17 h after the i.v. or i.m. administration of DOX-h, respectively. (C) 2007 Elsevier Ltd. All rights reserved.
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