磺胺类药物在中国对虾3种组织中的代谢情况
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李金宝(1987-),男,硕士,研究方向为水产药理学,429066587@qq.com

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国家虾产业技术体系(CARS-47);山东省自主创新专项(2013CXC80202);国家高技术研究发展计划(863计划)课题(2012AA10A409)


Pharmacokinetics of sulfa drugs in the three tissues of Fenneropenaeus chinensis
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    摘要:

     采用高效液相色谱法测定中国对虾肝胰腺、肌肉及鳃中磺胺类药物的含量,磺胺类药物包括磺胺二甲嘧啶(SM2)、磺胺嘧啶(SD)及磺胺对甲氧嘧啶(SMD)。3种磺胺类药物单次口服剂量均为l00 mg/kg,养殖期间水温为(24.6±2.4) ℃,比较3种磺胺类药物在中国对虾鳃、肝胰腺及肌肉中的T1/2β、CL、AUC(0—72)和Tmax等各主要参数。SM2在鳃、肝胰腺及肌肉中的T1/2β分别为23.067、34.162和16.559 h;SD在鳃、肝胰腺及肌肉中的T1/2β分别为29.157、34.272和27.929 h;SMD在鳃、肝胰腺及肌肉中的T1/2β分别为47.657、55.271和32.237 h。在同一组织中,SM2的消除速度最快,SD次之,SMD的消除速度最慢。口服同一磺胺类药物,在肌肉中消除速度最快,鳃次之,肝胰腺中的消除速度最慢。SM2在鳃、肝胰腺及肌肉中的CL分别为0.673、0.171和0.464 L/(h·kg);SD在鳃、肝胰腺及肌肉中的CL分别为0.496、0.214和0.463 L/(h·kg);SMD在鳃、肝胰腺及肌肉中的CL分别为0.29、0.082和0.362 L/(h·kg)。所以,同一组织中SMD的清除率最低,同一种磺胺类药物在鳃中清除最快。SM2在鳃、肝胰腺及肌肉中的AUC(0—72)分别为138.476、493.02和206.572 mg/(L·h);SD在鳃、肝胰腺及肌肉中的AUC(0—72)分别为147.919、379.039和186.495 mg/(L·h);SMD在鳃、肝胰腺及肌肉中的AUC(0—72)分别为218.024、629.311和229.819 mg/(L·h)。口服同一种磺胺类药物在肝胰腺中的药物吸收量是最大的,比较同一组织中的3种磺胺类药物的吸收量,SMD较高一些。综上所述,口服3种磺胺类药物,72 h内中国对虾肝胰腺中的药物残留最为严重。本研究为在中国对虾养殖过程中更加科学和合理地使用磺胺类药物提供了参考。[中国渔业质量与标准,2014,4(4):56-62]

    Abstract:

     The pharmacokinetics of sulfamethazine (SM2), sulfamethoxydiazine(SMD) and sulfadiazine(SD) in gill, hepatopancreas and muscle of Fenneropenaeus chinensis were investigated following oral administration (100 mg/kg) at (24.6±2.4) ℃. The results showed that for SM2, the values of T1/2β in gill, hepatopancreas and muscle were 23.067, 34.162 and 16.559 h, respectively. For SD, T1/2β in gill, hepatopancreas and muscle were 29.157, 34.272 and 27.929 h, respectively. For SMD, T1/2β in gill, hepatopancreas and muscle were 47.657, 55.271 and 32.237 h, respectively. The rate of different pharmic elimination in the same tissue was in the following order: SM2>SD>SMD. The rate of pharmic elimination in different tissues for taking orally the same drug was in the following order: muscle > gill > hepatopancreas. For SM2, CL in gill, hepatopancreas and muscle were 0.673, 0.171 and 0.464 L/(h·kg), respectively. For SD, CL in gill, hepatopancreas and muscle were 0.496, 0.214 and 0.463 L/(h·kg), respectively. For SMD, CL in gill, hepatopancreas and muscle were 0.29, 0.082 and 0.362 L/(h·kg), respectively. Therefore, the slowest clearance rate in the same tissue was SD. For the same pharmacokinetics, the fastest clearance rate was in the gill. For SM2, AUC(0—72) in gill, hepatopancreas and muscle were 138.476, 493.02 and 206.572 mg/(L·h), respectively. For SD, AUC(0—72) in gill, hepatopancreas and muscle were 147.919, 379.039 and 186. 495 mg/(L·h), respectively. For SMD, AUC(0—72) in gill, hepatopancreas and muscle were 218.024, 629.311 and 229.819 mg/(L·h), respectively. The AUC of hepatopancreas was higher than other tissues for taking orally the same drug, and the AUC of SMD was larger than others in the same tissue. The results illustrated the metabolism of the three sulfa drugs in gill, hepatopancreas and muscle of F. chinensis, and indicated that hepatopancreas was the main tissue of F. chinensis for sulfa drugs residue within 72 h.This study provides reference for more scientific and reasonable use of sulfa drugs in the breeding process of Fenneropenaeus chinensis.[Chinese Fishery Quality and Standards, 2014, 4(4):56-62]

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李金宝 ,李健*.磺胺类药物在中国对虾3种组织中的代谢情况[J].中国渔业质量与标准,2014,4(4):56-62. LI Jinbao,  LI Jian*. Pharmacokinetics of sulfa drugs in the three tissues of Fenneropenaeus chinensis[J]. Chinese Fishery Quality and Standards,2014,4(4):56-62.

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