抗菌药物亚迪蚕安宁在蚕体内的药物代谢动力学特征分析  

Pharmacokinetic Analysis on the Antibiotic Agent Yadican'anning in Silkworm

作　　者：康国平[1,2] 赫荣帆[2] 王玉华[1,2] 刘挺[1,2] 钟馗[1,2] 

机构地区：[1]江苏科技大学,江苏镇江212003 [2]中国农业科学院蚕业研究所,江苏镇江212018

出　　处：《蚕业科学》2011年第2期347-351,共5页ACTA SERICOLOGICA SINICA

基　　金：江苏省农业三项工程项目(No.SX2008-111)

摘　　要：蚕用抗菌药剂亚迪蚕安宁是喹诺酮类抗生素药物,研究该药物在蚕体内的药物代谢动力学特征,作为制定蚕病防治合理给药方案的理论依据。分别给家蚕5龄第4天健康幼虫添食2.5、5、10 mg/kg 3种剂量(药物与试验组蚕体总质量比)的亚迪蚕安宁后,于不同时间采集幼虫血样用抗生素微生物法检测血药浓度,药时数据经3P97药动学程序计算AIC值分别为-0.208、11.387和38.806,显示拟合度良好。主要药动学参数:吸收速率常数(ka)分别为0.148、0.190、0.281 h-1,达峰时间(Tmax)分别为3.764、3.993、3.613 h,最高血药浓度(Cmax)分别为2.334、3.576、9.786μg/mL,清除率(Cl)分别为0.089、0.134、0.133 L/h。以实测血药浓度-时间曲线与理论血药浓度-时间曲线的相关系数(R2)和AIC值作为识别模型的指标,拟合家蚕食下亚迪蚕安宁蚕体内的血药浓度-时间曲线,符合一级吸收一室开放式模型。试验结果表明:亚迪蚕安宁在蚕体内具有吸收迅速,达峰时间短,最高血药浓度与添食剂量成正比,消除半衰期较短等药物代谢动力学特征,适合日内多次给药。Yadican＇anning is an quinolone antibiotic agent for silkworm（Bombyx mori）.In order to provide a reasonable theoretical basis for dosage selection to control silkworm disease,pharmacokinetics of Yadican＇anning in silkworm was studied.After administration of 2.5,5,10 mg/kg（the mass ratio of drug to total silkworm body in the test group） Yadican＇anning to day 4 healthy larvae of the 5th instar,blood samples were collected to detect the concentrations of the drug in silkworm larvae with antibiotic-microbiological assay.Through Practical Pharmacokinetic Program 1997,the concentration-time data were calculated and the AIC values were 0.208,11.387 and 38.806 respectively.The result indicated that there was good fitness between the theoretical calculation and actual investigation.The major pharmacokinetic parameters were as follows： the absorption rate constant（ka） was 0.148,0.190 and 0.281 h-1 respectively;the time to reach peak value（Tmax） was 3.764,3.993 and 3.613 h respectively;the maximal blood concentration（Cmax） was 2.334,3.576 and 9.786 μg/mL respectively;and the clearance rate（Cl） was 0.089,0.134 and 0.133 L/h respectively.On the basis of R 2（the correlation coefficient between the measured concentration-time curve and theoretical concentration-time curve） and AIC values,a model was created to simulate the concentration-time curve of Yadican＇anning in silkworm body.The result showed that the pharmacokinetic process fitted to the first order absorption kinetics and one compartment open model.The above results indicated that Yadican＇anning had the pharmacokinetic properties including quick absorption inside the larval body,short time to reach peak value,the maximal blood concentration being proportional to the dosage administered,and shorter elimination half-life,being suitable for multiple administrations within one day.

关 键 词：蚕用药剂 抗菌素 亚迪蚕安宁 药物动力学 微生物法 

分 类 号：R96[医药卫生—药理学]