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    杨德学, 陈良柱, 赖丽虹, 任妙贤, 张桂君, 潘志坤, 方炳虎. 截短侧耳素衍生物BC-7013在鸡体内的药物动力学和生物利用度研究[J]. 华南农业大学学报, 2015, 36(4): 26-31. DOI: 10.7671/j.issn.1001-411X.2015.04.005
    引用本文: 杨德学, 陈良柱, 赖丽虹, 任妙贤, 张桂君, 潘志坤, 方炳虎. 截短侧耳素衍生物BC-7013在鸡体内的药物动力学和生物利用度研究[J]. 华南农业大学学报, 2015, 36(4): 26-31. DOI: 10.7671/j.issn.1001-411X.2015.04.005
    shu
    YANG Dexue, CHEN Liangzhu, LAI Lihong, REN Miaoxian, ZHANG Guijun, PAN Zhikun, FANG Binghu. Research on pharmacokinetics and bioavailability of pleuromutilin derivative BC-7013 in chickens[J]. Journal of South China Agricultural University, 2015, 36(4): 26-31. DOI: 10.7671/j.issn.1001-411X.2015.04.005
    Citation: YANG Dexue, CHEN Liangzhu, LAI Lihong, REN Miaoxian, ZHANG Guijun, PAN Zhikun, FANG Binghu. Research on pharmacokinetics and bioavailability of pleuromutilin derivative BC-7013 in chickens[J]. Journal of South China Agricultural University, 2015, 36(4): 26-31. DOI: 10.7671/j.issn.1001-411X.2015.04.005
    shu

    截短侧耳素衍生物BC-7013在鸡体内的药物动力学和生物利用度研究

    Research on pharmacokinetics and bioavailability of pleuromutilin derivative BC-7013 in chickens

      摘要
    • 摘要:
      目的 研究截短侧耳素衍生物BC-7013在鸡体内的药物动力学(简称药动学)特征及生物利用度.
      方法 6周龄健康白羽肉鸡20只随机分为2组，雌雄各半，分别进行单剂量静脉注射(简称静注，2.5 mg·kg-1)和单剂量口服(15 mg·kg-1)截短侧耳素衍生物BC-7013.以高效液相色谱－串联质谱(HPLC-MS /MS)内标法定量测定血浆中衍生物BC-7013的浓度，采用WinNonlin 5.2药动学软件的非房室模型统计矩原理分析药物浓度-时间数据，并计算其药动学参数.
      结果和结论 鸡静注给药后药动学参数为: t1/2β=(1.37 ± 0.14) h，Vd=(1.87 ± 0.25) L·kg-1，AUC(0→∞)=(2.83 ± 0.56) μg·mL-1·h，CL=(1.14 ± 0.28) L·h-1·kg-1; 鸡口服给药后药动学参数为: tmax= (1.94 ± 0.26) h，Cmax=(126.18 ± 6.54) ng·mL-1，AUC(0→∞)=(1.38 ± 0.21) μg·mL-1·h，MRT=(9.49 ± 0.57) h，F=(10.37 ± 1.48) %.截短侧耳素衍生物BC-7013在鸡体内的药动学特征表现为:静注给药后分布广，消除快; 口服给药后吸收较快但不完全，生物利用度较低.

       

      Abstract:
      Objective The pharmacokinetical characteristics and bioavailability of pleuromutilin derivative BC-7013 in chickens were investigated.
      Method Twenty chickens were randomly divided into two groups for pharmacokinelical experiments after a single intravenous(2.5 mg·kg-1) and oral administra tion(15 mg·kg-1).Blood samples were collected at different intervals after the administration of deriv ative BC-7013.The concentrations of derivative BC-7013 in plasma were determined by high-performance liquid chromatography-tandem mass spectrometry(HPLC-MS /MS) with internal standard method.Plas ma concentration-time profiles of derivative BC-7013 were analyzed by using non-compartmental analysis WinNonlin 5.2 software.
      Result and conclusion The main pharmacokinetical parameters of i.v.ad ministration were as follows: t1/2β=(1.37 ± 0.14) h, Vd=(1.87 ± 0.25) L·kg-1, AUC(0→∞)=(2.83 ± 0.56) μg·L-1·h, CL=(1.14 ± 0.28) L·h-1·kg-1.The major pharmacokinetical parameters of oral administration were as follows: tmax=(1.94 ± 0.26) h, Cmax=(126.18 ± 6.54) ng·mL-1, AUC(0→∞)=(1.38 ± 0.21) μg·mL-1·h, MRT=(9.49 ± 0.57) h, F=(10.37 ± 1.48) %. The results show that the pharmacokinetical characteristics of pleuromutilin derivative BC-7013 in healthy chicken manifest wide distribution, rapid elimination as well as incomplete absorption and low oral bioavailability.

       

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