引用本文:
【打印本页】   【HTML】   【下载PDF全文】   查看/发表评论  【EndNote】   【RefMan】   【BibTex】
←前一篇|后一篇→ 过刊浏览    高级检索
本文已被:浏览 96次   下载 133 本文二维码信息
码上扫一扫!
分享到: 微信 更多
复方磺胺嘧啶口灌给药在拟穴青蟹(Scylla paramamosain)体内药动学和组织分布与消除
陈进军,王 元,赵 姝,沈锦玉,赵留杰,房文红
作者单位
陈进军 中国水产科学研究院东海水产研究所 农业部东海与远洋渔业资源开发利用重点实验室 上海 200090上海海洋大学水产与生命学院 上海 201306 
王 元 中国水产科学研究院东海水产研究所 农业部东海与远洋渔业资源开发利用重点实验室 上海 200090 
赵 姝 中国水产科学研究院东海水产研究所 农业部东海与远洋渔业资源开发利用重点实验室 上海 200090 
沈锦玉 中国水产科学研究院东海水产研究所 农业部东海与远洋渔业资源开发利用重点实验室 上海 200090 
赵留杰 中国水产科学研究院东海水产研究所 农业部东海与远洋渔业资源开发利用重点实验室 上海 200090上海海洋大学水产与生命学院 上海 201306 
房文红 中国水产科学研究院东海水产研究所 农业部东海与远洋渔业资源开发利用重点实验室 上海 200090 
摘要:
研究了水温为(27±1)℃、盐度为10条件下,单剂量(100 mg/kg)口灌给药复方磺胺嘧啶(磺胺嘧啶SD∶甲氧苄啶TMP=5∶1)后,SD和TMP在拟穴青蟹(Scylla paramamosain)体内的药动学以及在肌肉、肝胰腺和鳃组织中的分布和消除规律。结果显示,拟穴青蟹口灌复方磺胺嘧啶后,血淋巴中SD和TMP药物浓度-时间关系曲线均符合一级吸收二室模型,SD和TMP的峰浓度(Cmax)分别为49.56 mg/L和2.79 mg/L,药时曲线下面积(AUC)分别为1417.6 mg/L·h和82.7 mg/L·h;肝胰腺是SD和TMP峰浓度最高的组织,其Cmax分别为59.36 mg/kg和74.82 mg/kg。由此可见,大量TMP蓄积在肝胰腺中,进入血液循环的TMP很少。在鳃组织中,SD和TMP的Cmax分别为51.89 mg/kg和42.58 mg/kg,消除半衰期分别为23.28 h和25.29 h;鳃组织中药物浓度比较高,且消除速度较快,推测其在药物代谢中承担着消除功能。在肌肉中,SD和TMP的Cmax分别为44.95 mg/kg和 10.09 mg/kg,消除半衰期分别为25.09 h和35.08 h。以0.1 mg/kg和0.05 mg/kg分别为SD和TMP的最高残留限量(MRL),95%置信区间,推算SD和TMP在拟穴青蟹肌肉中的理论休药期分别为290.6 h和302.8 h,在肝胰腺中分别为340.4 h和377.0 h。
关键词:  复方磺胺嘧啶  拟穴青蟹  药动学  组织分布  休药期
DOI:10.11758/yykxjz.20160618001
分类号:
基金项目:
Pharmacokinetics, Tissue Distribution and Elimination of Sulfadiazine and Trimethoprim in Mud Crab (Scylla paramamosain) After Oral Administration
CHEN Jinjun,WANG Yuan,ZHAO Shu,SHEN Jinyu,ZHAO Liujie,FANG Wenhong
Abstract:
The pharmacokinetics, tissue distribution and elimination of sulfadiazine (SD) and trimethoprim (TMP) in mud crab (Scylla paramamosain) were investigated in order to provide scientific data to support its safe use. SD and TMP were orally administrated at a single dose of SD (83.3 mg/kg) and TMP (16.7 mg/kg) at temperature of (27±1) ℃ and seawater salinity of 10. The hemolymph concentration-time curve for SD and TMP were described by a two-compartment model with first order absorption. Peak hemolymph concentration (Cmax) for SD and TMP was 49.56 mg/L and 2.79 mg/L, respectively, and area under curve (AUC) for SD and TMP was 1417.6 mg/L·h and 82.7 mg/L·h, respectively. Of the tissues analyzed, the hepatopancreas was the tissue with the highest SD and TMP concentrations, and Cmax was 59.36 mg/kg and 74.82 mg/kg, respectively. Thus, a large amount of TMP was accumulated in the hepatopancreas, while only a small amount of TMP entered blood circulation. In gill, peak concentration for SD and TMP was 51.89 mg/kg and 42.58 mg/kg, respectively, and elimination half-life was 23.28 h and 25.29 h, respectively. The drug concentration in gill tissue was relatively high and the elimination rate was fast, suggesting crab gill plays a role in drug elimination. In muscle, peak concentration for SD and TMP was 44.95 mg/kg and 10.09 mg/kg, respectively, and elimination half-life was 25.09 h and 35.08 h, respectively. According to SD and TMP elimination and the maximum residue limit of 0.1 mg/kg for SD and 0.05 mg/kg for TMP, the theoretical withdrawal time of SD/TMP in muscle and hepatopancreas, was 290.6 h/302.8 h and 340.4 h/377.0 h, respectively.
Key words:  Sulfadiazine and trimethoprim  Scylla paramamosain  Pharmacokinetics  Tissue distribution  Withdrawal time