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    肖田安, 怀彬彬, 李帅鹏, 陈杖榴, 黄显会. 伊维菌素 PLA 及 PLGA 微球混悬液在犬体内的药代动力学研究[J]. 华南农业大学学报, 2014, 35(3): 8-12. DOI: 10.7671/j.issn.1001-411X.2014.03.002
    引用本文: 肖田安, 怀彬彬, 李帅鹏, 陈杖榴, 黄显会. 伊维菌素 PLA 及 PLGA 微球混悬液在犬体内的药代动力学研究[J]. 华南农业大学学报, 2014, 35(3): 8-12. DOI: 10.7671/j.issn.1001-411X.2014.03.002
    shu
    XIAO Tian’an, HUAI Binbin, LI Shuaipeng, CHEN Zhangliu, HUANG Xianhui. Pharmacokinetics of ivermectin loaded PLA/PLGA microspheres suspension in dogs[J]. Journal of South China Agricultural University, 2014, 35(3): 8-12. DOI: 10.7671/j.issn.1001-411X.2014.03.002
    Citation: XIAO Tian’an, HUAI Binbin, LI Shuaipeng, CHEN Zhangliu, HUANG Xianhui. Pharmacokinetics of ivermectin loaded PLA/PLGA microspheres suspension in dogs[J]. Journal of South China Agricultural University, 2014, 35(3): 8-12. DOI: 10.7671/j.issn.1001-411X.2014.03.002
    shu

    伊维菌素 PLA 及 PLGA 微球混悬液在犬体内的药代动力学研究

    Pharmacokinetics of ivermectin loaded PLA/PLGA microspheres suspension in dogs

      摘要
    • 摘要: 【目的】研究并比较伊维菌素微球与伊维菌素普通注射液在犬体内的药代动力学(简称药动学)特征.【方法】18只健康比格犬随机分为3组，分别单次皮下注射伊维菌素聚乳酸（Poly lactic acid，PLA）微球混悬液（3 mg·kg-1），乙交酯丙交酯共聚物（Poly lactic-co-glycolic acid，PLGA）微球混悬液（3 mg·kg-1）及伊维菌素普通注射液（0.3 mg·kg-1），反相高效液相色谱法测定犬血浆内伊维菌素的浓度，运用药动学软件Winnonlin 5.2.1的非房室模型分析方法，计算出有关药动学参数.【结果和结论】伊维菌素普通注射液皮下注射给药后，达峰时间为（1.33±0.21）d，达峰质量浓度为（44.3±5.1）ng·mL-1，药时曲线下面积（AUC0~∞）为（323.26±23.56）ng·mL-1·d；伊维菌素PLA及PLGA微球混悬液皮下注射给药，AUC0~∞ 分别为（1 041.47±73.73）、（1 461.77±102.54）ng·mL-1·d,伊维菌素在犬体内维持血药质量浓度 >1 ng·mL-1 的时间达140 d以上，所制备的PLA微球和PLGA微球具有明显缓释特性.

       

      Abstract: 【Objective】The pharmacokinetics of ivermectin (IVM) loaded in poly lactic acid (PLA) and Poly lactic-co-glycolic acid (PLGA) microspheres (MS) in dogs was investigated. 【Method】Eighteen healthy beagle dogs were divided into 3 groups randomly. PLA and PLGA MS suspensions (s.c) of IVM were given to the animals subcutaneously at a dosage of 3 mg·kg-1 respectively. IVM (0.3 mg·kg-1，s.c) was concluded in the experiment for comparison. The IVM concentration in dog plasma was determined by the reversed-phase HPLC, Pharmacokinetic parameters were estimated using the Winnonlin 5.2.1 software package.【Result and conclusion】The IVM concentration time data were fitted to noncompartment model. After subcutaneous administration of IVM（0.3 mg·kg-1）injection the pharmacokinetic parameters were as follows: the peak concentration Cmax was (44.3±5.1) ng·mL-1, and tmax was (1.33±0.21) d; area under the curve AUC0~∞ was (323.26±23.56) ng·mL-1·d respectively.After subcutaneous injection of IVM-PLA-MS and IVM-PLGA-MS（3 mg·kg-1）, area under the curve AUC0~∞ was(1 041.47±73.73) and (1 461.77±102.54) ng·mL-1·d respectively. PLA/PLGA MS suspensions of IVM have obviously a sustained-release property, with the plasma IVM concentration keeping in a steady state above 1 ng·mL-1 for 140 days after administration.

       

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