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噁喹酸在凡纳滨对虾体内药动学和对弧菌的体外药效 被引量:3

Pharmacokinetics of oxolinic acid in the Pacific white shrimp(Litopenaeus vannamei) and in vitro antimicrobial activity on Vibrios
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摘要 采用高效液相色谱法,研究了复方噁喹酸粉药饵投喂在凡纳滨对虾体内药动学和组织中消除规律,同时检测了噁喹酸对对虾源弧菌的最小抑菌浓度(MIC),建立了药动/药效(PK/PD)关系,提出了用药方案和休药期建议。结果显示,复方噁喹酸粉拌饵投喂给药,噁喹酸给药剂量为30 mg/kg(体质量),凡纳滨对虾血浆噁喹酸浓度—时间关系曲线均符合一级吸收二室开放动力学模型。血淋巴中噁喹酸达峰浓度(Cmax)、达峰时间(Tmax)、曲线下面积(AUC0-24)和消除半衰期(t1/2z)分别为14.70 mg/L、2 h、244.6 mg/(L·h)和18.56 h;肌肉、肝胰腺和鳃的峰浓度(Cmax)分别为4.11、17.20和7.01 mg/kg,消除半衰期(t1/2z)分别为10.71、12.31和16.75 h。噁喹酸对132株弧菌的MIC主要分布在0.15~1.25μg/mL,MIC50和MIC90分别为0.62和1.25μg/mL。PK/PD相互关系参数Cmax/MIC90和AUC0-24/MIC90分别为11.76和195.7。研究表明,噁喹酸以30 mg/(kg体质量)剂量药饵给药,凡纳滨对虾能很好地吸收噁喹酸,可以有效地防治弧菌引起的细菌性疾病。 The pharmacokinetics and tissue elimination of oxolinic acid(OA) in the Pacific white shrimp,Litopenaeus vannamei, were investigated following oral administration via feed by HPLC method. The minimum inhibitory concentrations(MIC) of OA on the pathogenic Vibrio were detected. The Pharmacokinetics/pharmacodynamics(PK/PD) parameters were calculated, and dosage regime and withdrawal time were developed.The haemolymph OA concentration vs. time after oral administration via feed was best described by a twocompartment model with first absorption following a single dose of 30 mg/kg. The peak concentration(Cmax), peak time(Tmax), area under curve(AUC0-24) and elimination half-life time(t1/2z) for hemolymph were 14.70 mg/L, 2 h244.6 mg/L, and 18.56 h, respectively. Peak concentrations(Cmax)in muscle, hepatopancreas and gill were 4.11mg/kg, 17.20 mg/kg and 7.01 mg/kg, respectively; elimination half-life time(t1/2z) were 10.71 h, 12.31 h and 16.75 h, respectively. The OA MICs of 132 Vibrios isolates varied mainly from 0.15 to 1.25 μg/mL with MIC50 of 0.62μg/mL and MIC90 of 1.25 μg/mL. The ratios of Cmax/MIC90 and AUC0-24/MIC90, which were two important indices for PK/PD relationship, were 11.76 and 195.7, respectively. The results showed that OA dosage of 30 mg/kg by medicated feed could effectively combat bacterial diseases caused by the Vibrios.
出处 《水产学报》 CAS CSCD 北大核心 2016年第3期512-519,共8页 Journal of Fisheries of China
基金 公益性行业(农业)科研专项(201203085) 上海市科技兴农重点攻关项目[沪农科攻字(2014)第3-4号] 中国水产科学研究院基本科研业务费专项(2013A0603)~~
关键词 凡纳滨对虾 弧菌 噁喹酸 药动学 体外药效 Litopenaeus vannamei oxolinic acid pharmacokinetics in vitro pharmacodynamics Vibrios
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