Mapongpeng Roipim, Laovechprasit Weerapong, Poapolathep Amnart, Giorgi Mario, Junchompoo Chalatip, Sakulthaew Chainarong, Jermnak Usuma, Passadurak Wanida, Poapolathep Saranya
Department of Pharmacology, Faculty of Veterinary Medicine, Kasetsart University, Bangkok, Thailand.
Eastern Marine and Coastal Resources Research and Development Center, Rayong, Thailand.
J Vet Pharmacol Ther. 2019 Jan;42(1):104-110. doi: 10.1111/jvp.12723. Epub 2018 Oct 11.
Green sea turtles are widely distributed in tropical and subtropical waters. Adult green sea turtles face many threats, primarily from humans, including injuries from boat propellers, being caught in fishing nets, pollution, poaching, and infectious diseases. To the best of our knowledge, limited pharmacokinetic information to establish suitable therapeutic plans is available for green sea turtles. Therefore, the present study aimed to describe the pharmacokinetic characteristics of ceftriaxone (CEF) in green sea turtles, Chelonia mydas, following single intravenous and intramuscular administrations at two dosages of 10 and 25 mg/kg body weight (b.w.). Blood samples were collected at assigned times up to 96 hr. The plasma concentrations of CEF were measured by liquid chromatography tandem mass spectrometry. The concentrations of CEF in the plasma were quantified up to 24 and 48 hr after i.v. and i.m. administrations at dosages of 10 and 25 mg/kg b.w., respectively. The C values of CEF were 15.43 ± 3.71 μg/ml and 43.48 ± 4.29 μg/ml at dosages of 10 and 25 mg/kg, respectively. The AUC values increased in a dose-dependent fashion. The half-life values were 2.89 ± 0.41 hr and 5.96 ± 0.26 hr at dosages of 10 and 25 mg/kg b.w, respectively. The absolute i.m. bioavailability was 67% and 108%, and the binding percentage of CEF to plasma protein was ranged from 20% to 29% with an average of 24.6%. Based on the pharmacokinetic data, susceptibility break-point and PK-PD index (T > MIC, 0.2 μg/ml), i.m. administration of CEF at a dosage of 10 mg/kg b.w. might be appropriate for initiating treatment of susceptible bacterial infections in green sea turtles.
绿海龟广泛分布于热带和亚热带水域。成年绿海龟面临许多威胁，主要来自人类，包括被船桨打伤、被渔网捕获、污染、偷猎和传染病。据我们所知，目前可用于绿海龟制定合适治疗方案的药代动力学信息有限。因此，本研究旨在描述头孢曲松（CEF）在绿海龟（蠵龟）体内单次静脉注射和肌肉注射10和25毫克/千克体重两种剂量后的药代动力学特征。在长达96小时的指定时间采集血样。通过液相色谱串联质谱法测定血浆中CEF的浓度。分别在静脉注射和肌肉注射10和25毫克/千克体重剂量后24和48小时内对血浆中CEF的浓度进行定量。在10和25毫克/千克剂量下，CEF的C值分别为15.43±3.71微克/毫升和43.48±4.29微克/毫升。AUC值呈剂量依赖性增加。在10和25毫克/千克体重剂量下，半衰期值分别为2.89±0.41小时和5.96±0.26小时。肌肉注射的绝对生物利用度分别为67%和108%，CEF与血浆蛋白的结合率在20%至29%之间，平均为24.6%。根据药代动力学数据、药敏断点和PK-PD指数（T＞MIC，0.2微克/毫升），以10毫克/千克体重的剂量肌肉注射CEF可能适合开始治疗绿海龟的敏感细菌感染。
