| 李海迪,杨先乐,胡鲲,王翔凌.2009.双氟沙星及其代谢产物在中华绒螯蟹体内药物代谢及残留消除规律.动物学杂志,44(2):12-20. |
| 双氟沙星及其代谢产物在中华绒螯蟹体内药物代谢及残留消除规律 |
| Pharmacokinetics and the Elimination Regularity of Difloxacin and its Metabolite Sarafloxacin in Eriocheir sinensis |
| 投稿时间：2008-09-08 修订日期：2008-11-10 |
| DOI： |
| 中文关键词: 中华绒螯蟹 双氟沙星 沙拉沙星 药代动力学 |
| 英文关键词:Eriocheir sinensis Difloxacin Sarafloxacin Pharmacokinetics |
| 基金项目:国家十一五科技支撑计划项目(No.2006BAD03B04) |
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| 中文摘要: |
| 采用高效液相色谱法,在口灌给药途径下,研究双氟沙星及其代谢产物沙拉沙星在中华绒螯蟹(Eriocheir sinensis)体内的药代动力学。中华绒螯蟹以20 mg/kg剂量给药双氟沙星后,其血淋巴、肌肉、肝胰腺、精巢和卵巢中药物-时间曲线关系符合开放性二室模型。双氟沙星在中华绒螯蟹体内吸收迅速,在不同组织中分布较广,达峰时间短。血淋巴、肌肉、肝胰腺、精巢和卵巢中的Vd分别为3.170 L/kg、2.122 L/kg、1.045 L/kg、1.051 L/kg和0.203 L/kg;双氟沙星在中华绒螯蟹体内消除缓慢,在血淋巴、肌肉、肝胰腺、精巢和卵巢中的消除半衰期t1/2β分别为96.316 h、88.228 h、137.524 h、67.021 h和124.679 h;总体清除率CLs分别为0.783 L/h.kg、0.040 L/h.kg、0.013 L/h.kg、0.011 L/h.kg和0.008 L/h.kg。代谢产物沙拉沙星在中华绒螯蟹血淋巴、肌肉、肝胰腺、精巢和卵巢中药物水平的变化趋势与双氟沙星相似,都呈现多峰现象。但肌肉、肝胰腺、精巢和卵巢4种组织中代谢产物沙拉沙星出现药峰的时候恰好是这4种组织中双氟沙星下降缓慢时期。鉴于双氟沙星及其代谢产物沙拉沙星在中华绒螯蟹体内消除缓慢,而可食组织中脂肪含量较高,因此若规定可食组织中双氟沙星的最大残留限量以脂肪中最大残留限量(100μg/kg)为标准,沙拉沙星的最大残留限量为30μg/kg,则建议双氟沙星在中华绒螯蟹中的休药期大于24d,才能保障食用者的安全。 |
| 英文摘要: |
| The pharmacokinetics of difloxacin（DIF） and its metabolite sarafloxacin（SAR） in hemolymph,muscle,hepatopancreas,spermary and ovary of Chinese Mitten-handed Crab（Eriocheir sinensis） were studied by RP-HPLC,after administration by single oral garage of 20 mg/kg.The concentrations versus time in hemolymph,muscle,hepatopancreas,spermary and ovary of E.sinensis were well described by a two-department open model.The results of present studies showed that DIF was rapidly absorbed and extensively distributed in E.sinensis.The apparent volume of distribution（Vd） of DIF of hemolymph,muscle,hepatopancreas,spermary and ovary was 3.170 L/kg,2.122 L/kg,1.045 L/kg,1.051 L/kg and 0.203 L/kg respectively.DIF eliminated slowly.The elimination half-time（t1/2β） was 96.316 h,88.228 h,137.524 h,67.021 h and 124.679 h,respectively,and the total body clearance（CLs） was 0.783 L/h·kg,0.04 L/h·kg,0.013 L/h·kg,0.011 L/h·kg and 0.008 L/h·kg.The metabolite SAR concentration-time profiles of the hemolymph,muscle,hepatopancreas,spermary and ovary presented similar trend.The multipeak phenomenon were observed,but the peak time of the metabolite SAR in hemolymph,muscle,hepatopancreas,spermary and ovary was the time that the eliminating rate of DIF was very low.Considering that the eliminating rate of DIF and metabolite SAR were very low.Withdrawal time was more 24 d when the maximum residue of DIF is 100 μg/kg and of SAR is 30 μg/kg after single oral administration of DIF in E.sinensis. |
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