Martínez José, Escudero Elisa, Badillo Elena, Yuste María Teresa, Galecio Juan Sebastián, Marin Pedro
Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, 30100 Murcia, Spain.
Escuela de Medicina Veterinaria, Colegio de Ciencias de la Salud, Universidad San Francisco de Quito, Quito EC 170157, Cumbayá, Ecuador.
Animals (Basel). 2024 Aug 20;14(16):2416. doi: 10.3390/ani14162416.
Doxycycline is a second-generation tetracycline, marketed in different species for treating infections caused by susceptible bacteria. Little information is available on the pharmacokinetics of doxycycline in lactating goats. The objective of this study was to establish the disposition kinetics of doxycycline after parenteral administration (intravenous and intramuscular) in dairy goats and its elimination in milk. A cross-over model was designed ( = 6). Doxycycline was dosed at 5 mg/kg for intravenous administration and 20 mg/kg for extravascular administrations. Noncompartmental pharmacokinetic methods were used to calculate plasma concentration-time data. The V value suggests a moderate distribution of this antibiotic in goats, with a value of 0.85 L/kg. A low bioavailability (F = 45.60%) of doxycycline following an intramuscular injection was observed, with all animals exhibiting signs of lameness. Doxycycline rapidly crossed the blood-milk barrier, but exposure to the antimicrobial and the concentrations reached in milk were lower than those obtained in plasma. Although PK/PD ratios may be low with the pharmacokinetic data obtained with this formulation of doxycycline, at this dose and route of administration, doxycycline after IM administration could be useful for infections by moderate or highly susceptible bacteria in the mammary gland of goats. However, it may be necessary to test different doses of doxycycline or other routes of administration to achieve better surrogate markers and to establish repeated dosing regimens and clinical efficacy.
强力霉素是第二代四环素类药物,在不同物种中用于治疗由易感细菌引起的感染。关于强力霉素在泌乳山羊体内的药代动力学信息很少。本研究的目的是确定强力霉素在奶山羊经肠胃外给药(静脉注射和肌肉注射)后的处置动力学及其在乳汁中的消除情况。设计了一个交叉模型(n = 6)。静脉注射时强力霉素的剂量为5 mg/kg,血管外给药时为20 mg/kg。采用非房室药代动力学方法计算血浆浓度-时间数据。V值表明该抗生素在山羊体内分布适中,值为0.85 L/kg。观察到肌肉注射后强力霉素的生物利用度较低(F = 45.60%),所有动物均表现出跛行迹象。强力霉素能迅速穿过血乳屏障,但乳汁中抗菌药物的暴露量和达到的浓度低于血浆中的浓度。尽管根据该强力霉素制剂获得的药代动力学数据,PK/PD比值可能较低,但在此剂量和给药途径下,肌肉注射后的强力霉素可能对山羊乳腺中中度或高度易感细菌引起的感染有用。然而,可能有必要测试不同剂量的强力霉素或其他给药途径,以获得更好的替代指标,并建立重复给药方案和临床疗效。