物学杂志 Chinese journal d zoology200742(5)62~69 恩诺沙星在罗氏沼虾体内的药物代谢动力学 钱云云唐俊郑宗林杨先乐 (农业部渔业动植物病原库上海水产大学上海200000 摘要:应用反相高效液相色谱法( RP HEC)研究了恩诺沙星在罗氏沼虾( Macrobrachium rosenberg)体内 的药物代谢动力学。实验结果表明,恩诺沙星在血淋巴、肝胰腺、肌肉中的平均回收率分别为86.54%土 2.39%85.43%拉75%95.01%土.99%,其代谢产物环丙沙星在血淋巴、肝胰腺、肌肉中的平均回收 率分别为94.34%8.30%75.17%书.42%80.42%土1.67%;恩诺沙星及其代谢产物环丙沙星在三种 组织中的平均日内精密度分别为3.39%±0.53%和3.92%±1.24%,而日间精密度分别为5.11%± 1.73%和5.28%±.10%。恩诺沙星、环丙沙星的最低检测限分别为0.02ug/m和0.01ug/ml。罗氏沼 虾以10mg/kg虾体重剂量单次肌肉注射给药后,血液中药物浓度即刻达到峰值,并迅速向组织中分布 实验数据经 MCPKP药动学软件分析,恩诺沙星在血淋巴中的主要药物代谢动力学参数为:t1四为0.581 h、为69.315h、d/F为7230L/kg、C/F为0.035L/h恕g、K2为0.01/h、K为0.005/hUC为291.898 ug/ml t、Tm为0.083h、Cmx为6.293μg/ml;恩诺沙星在肝胰腺、肌肉组织中主要药动学参数:为1.941 h0.000h;:1为70.732h59.456h,AUC为30807ug/mh217.039g/mh。三种组织中均能检测到恩 诺沙星的活性代谢产物环丙沙星,但含量均处于较低水平,药物浓度时间数据经 MCPKP药动学软件处 理后,不能用开放性一室模型或二室模型拟合 关键词:恩诺沙星;罗氏沼虾;药物代谢动力学 中图分类号:R917文献标识码:A文章编号:02503263(2007)056208 Pharmacokinetics of Enrofloxacin in Macrobrachium rosenbergii QIAn Yur Yun TANG Jun ZHENG ZongLin YANG XiarLe ( Aquatic Pathogen Collection Center g Ministry g Agnicitume, Shanghai Fisheries Uninersity, Shanghai 200090, Chin Abstract: The pharmacokinetics of enrofloxacin(ENR)and ciprofloxacin(CIP)in hemolymph, hepatopancreas and uscle of the Macrobrachium rosenbergii were investigated using the reverse"phase high performance liquid hromatography(RPHHLC). The average recovery rates of ENR in three tissues were 8654 %+2. 39%,85.43 %+ 2. 75%, and 95.01%+1. 99 % respectively and the average recovery rate of CIP in three tissues were 94 34%+ 8.,. %+5.42 %, and 80. 42 %+1. 67 respectively in the three tissues; The intra day precision rates of ENR and CIP were 3. 39 %+0. 53%and 3. 92 %+1. 24 % respectively, and the inter day precision rates were 5.11%+1. 73 %and 5. 28%+2. 10 %, respectively. The lowest detected limit of enrofloxacin in tissues was 0 02 ug/ml and that of ciprofloxacin was 0 01 Wg/ml. The data were analyzed with the pharmacokinetic computer program MCPKP. The main pharmacokinetic parameters of ENR in hemolymph were tg 0. 581 h, fips 69. 315 h, Va/ F7. 230 基金项目“十五“国家科技攻关计划项目(N.2004BA526B),上海市重点学科建设资助项目(N.Y01),上海市教育委员会E研 究院建设资助项目(B3009) 通讯作者,Emal:yang@asif.edu.cn; 第一作者介绍钱云云,女,硕士研究生;主要从事药物代谢及残留检测研究; Email: yunyun78@ hotmail 收稿日期:20070412,修回日期:2007-0723 201994-2007ChinaAcademicJourmalElectronicPublishingHouse.Allrightsreservedhttp://www.cnki.net动物学杂志 Chinese Journal of Zoology 2007 ,42(5) :62～69 基金项目 “十五”国家科技攻关计划项目(No. 2004BA526B) ,上海市重点学科建设资助项目(No. Y1101) ,上海市教育委员会 E2研 究院建设资助项目(E03009) ; 3 通讯作者 ,E2mail :xlyang @shfu. edu. cn ; 第一作者介绍 钱云云 ,女 ,硕士研究生 ;主要从事药物代谢及残留检测研究 ; E2mail :qyunyun78 @hotmail. com。 收稿日期 :2007204212 ,修回日期 :2007207223 恩诺沙星在罗氏沼虾体内的药物代谢动力学 钱云云 唐 俊 郑宗林 杨先乐 3 (农业部渔业动植物病原库 上海水产大学 上海 200090) 摘要 : 应用反相高效液相色谱法 (RP2HPLC) 研究了恩诺沙星在罗氏沼虾 ( Macrobrachium rosenbergii) 体内 的药物代谢动力学。实验结果表明 ,恩诺沙星在血淋巴、肝胰腺、肌肉中的平均回收率分别为 86154 % ± 2139 %、85143 % ±2175 %、95101 % ±1199 % ,其代谢产物环丙沙星在血淋巴、肝胰腺、肌肉中的平均回收 率分别为 94134 % ±8130 %、75117 % ±5142 %、80142 % ±1167 % ;恩诺沙星及其代谢产物环丙沙星在三种 组织中的平均日内精密度分别为 3139 % ±0153 %和 3192 % ±1124 % ,而日间精密度分别为 5111 % ± 1173 %和 5128 % ±2110 %。恩诺沙星、环丙沙星的最低检测限分别为 0102μgΠml 和 0101μgΠml。罗氏沼 虾以 10 mgΠkg 虾体重剂量单次肌肉注射给药后 ,血液中药物浓度即刻达到峰值 ,并迅速向组织中分布。 实验数据经 MCPKP药动学软件分析 ,恩诺沙星在血淋巴中的主要药物代谢动力学参数为 : t1Π2α为 01581 h、t1Π2β为 691315 h、VdΠF 为 71230 LΠkg、CLΠF 为 01035 LΠh·kg、K12为 0101Πh、K21为 01005Πh、AUC 为 2911898 μgΠml·h、Tmax为 01083 h、Cmax为 61293μgΠml ;恩诺沙星在肝胰腺、肌肉组织中主要药动学参数 : t1Π2α为 11941 h、01000 h ; t1Π2β为 701732 h、591456 h ;AUC 为 308107μgΠml·h、2171039μgΠml·h。三种组织中均能检测到恩 诺沙星的活性代谢产物环丙沙星 ,但含量均处于较低水平 ,药物浓度2时间数据经 MCPKP 药动学软件处 理后 ,不能用开放性一室模型或二室模型拟合。 关键词 : 恩诺沙星 ;罗氏沼虾 ;药物代谢动力学 中图分类号 :R917 文献标识码 :A 文章编号 :025023263 (2007) 05262208 Pharmacokinetics of Enrofloxacin in Macrobrachium rosenbergii QIAN Yun2Yun TANGJun ZHENG Zong2Lin YANG Xian2Le 3 ( Aquatic Pathogen Collection Center of Ministry of Agriculture , Shanghai Fisheries University , Shanghai 200090 , China) Abstract:The pharmacokinetics of enrofloxacin ( ENR) and ciprofloxacin (CIP) in hemolymph ,hepatopancreas and muscle of the Macrobrachium rosenbergii were investigated using the reverse2phase high performance liquid chromatography (RP2HPLC) . The average recovery rates of ENR in three tissues were 86154 % ±2139 % ,85143 % ± 2175 % ,and 95101 % ±1199 % ,respectively ,and the average recovery rate of CIP in three tissues were 94134 % ± 8130 % ,75117 % ±5142 % ,and 80142 % ±1167 % respectively in the three tissues ; The intra2day precision rates of ENR and CIP were 3139 % ±0153 % and 3192 % ±1124 % , respectively , and the inter2day precision rates were 5111 % ±1173 % and 5128 % ±2110 % ,respectively. The lowest detected limit of enrofloxacin in tissues was 0102 μgΠml ,and that of ciprofloxacin was 0101μgΠml. The data were analyzed with the pharmacokinetic computer program MCPKP. The main pharmacokinetic parameters of ENR in hemolymph were t1Π2α 01581 h , t1Π2β 691315 h ,VdΠF 71230