Pharmacokinetics and acetylation of sulfamethoxazole in turbot <Emphasis Type="Italic">Scophthalmus maximus</Emphasis> after intravascular administration

The pharmacokinetic profiles and sulfamethoxazole (SMX) acetylation process in turbot reared at 18°C were investigated. Either SMX (parent drug) or its acetylized metabolite, N₄-acetylsulfamethoxazole (AcSMX), was administered intravascularly to turbot at a dosage of 50 mg/kg BW. Serum concentrations of the parent drug and its metabolite were both measured by HPLC, and the changes in concentration over time were analyzed in two- and non-compartment models because SMX treatment produced multiple peaks. The results demonstrated that the elimination half-life of the parent drugs, SMX and AcSMX, were 159.2 and 5.9 h, respectively. The apparent volume of distribution was 0.2 and 0.8 L/kg, and the clearance was 0.038 and 0.222 L/(h·kg), for SMX and AcSMX, respectively. SMX acetylation in turbot was 2.8%, and the deacetylation of AcSMX was 0.2%. These findings may be useful in optimizing SMX dosage regimens in turbot aquaculture.     

水产用微生态制剂耐药性评估及耐药相关遗传元件检测

以市场上购买的9种水产用微生态制剂为研究对象,采用琼脂稀释法筛选其中的耐药菌株,运用微量肉汤稀释法检测分离菌株对庆大霉素、恩诺沙星、诺氟沙星、氟苯尼考、磺胺嘧啶、磺胺甲基嘧啶、四环素、土霉素、万古霉素9种抗生素的耐药性,结合聚合酶链式反应分析耐药菌株携带的耐药基因和可移动遗传元件(接合性质粒遗传标记、转座子、整合子和插入序列),为微生态制剂的安全生产与监测提供参考。结果显示,9种微生态制剂中都存在耐药菌株,100株分离菌株对除恩诺沙星以外的8种抗生素都存在不同程度的耐药, 46%的株菌同时携带氟喹诺酮类、酰胺醇类、磺胺类、四环素类、氨基糖苷类和糖肽类耐药基因,且有15株菌同时携带整合子-基因盒、质粒、转座子和插入序列,携带两种及两种以上可移动遗传原件的比例为95%。微生态制剂产品可能存在一定的安全隐患,应加强质量监测和市场监管。     

恩诺沙星对脊尾白虾APND、ECOD和GST活性的影响

为研究脊尾白虾(Exopalaemon carinicauda)药物代谢酶对恩诺沙星的响应及其在恩诺沙星代谢过程中的作用,作者以10、20和40 mg/kg恩诺沙星连续投喂脊尾白虾3 d,于投喂后的第1、2天以及停止投喂药物的第1、4、8、12、24、48、72、120小时取样,测定了脊尾白虾肝胰腺、鳃和血清中的氨基比林-N-脱甲基酶(aminopyrine-N-demethylase,APND)、7-乙氧基香豆素-O-脱乙基酶(7-ethoxycoumarinO-Deethylase,ECOD)和谷胱甘肽-S-转移酶(glutathione-S-transferase,GST)的活性。结果表明:不同浓度恩诺沙星对脊尾白虾肝胰腺、鳃和血清中Ⅰ相药物代谢酶APND和ECOD活性均呈现显著抑制作用(P0.05)。投喂药物后,APND和ECOD活性呈现先下降后逐渐上升趋势,3个剂量组酶活性均在最后一次给药后8 h达到最低。与对照组相比,不同浓度恩诺沙星对各组织中Ⅱ相药物代谢酶GST活性呈现显著诱导作用(P0.05),此作用呈现先上升后下降的趋势。恩诺沙星对脊尾白虾APND、ECOD及GST活性的作用均呈现剂量依赖性。本研究表明,脊尾白虾Ⅰ相和Ⅱ相代谢酶均会对药物做出反应,可作为其养殖过程中药物代谢及适用性的指示物。