【目的】研究三氮脒临床用药的有效性和安全性，测定猪血浆的药物-蛋白结合率.【方法】血浆样品以超滤法分离游离型的药物.以高效液相色谱-紫外法测定药物含量，计算出三氮脒-血浆蛋白结合率.6头猪交叉分别按体质量肌内注射7和14 mg/kg三氮脒注射液，在给药后3、5、15、60 min测定体内三氮脒-血浆蛋白结合率.【结果和结论】体外测定的三氮脒-血浆药物蛋白结合率为74.68%～95.90%.猪给药后体内的药物蛋白结合率为84.11%~89.69%(7 mg/kg剂量组)、82.96%~88.65%(14 mg/kg剂量组)，随着剂量增加可能出现饱和现象.在设计三氮脒应用于猪的给药方案时应充分考虑这一因素.
【Objective】A study on the diminazene-protein binding rate in swine was carried out in this experiment for further clinical application efficiency and safety.【Method】The plasma samples were pretreated to separate free drug by ultrafiltration. A high performance liquid chromatographic-UV (HPLC-UV) method was used to measure the amount of free diminazene in plasma. Then the drug-protein binding rate was accounted. Six swine were administrated intramuscularly at a dosages of 7 and 14 mg/kg. The plasma samples were collected and the protein binding rates in vivo were determination at 3, 5, 15, 60 min.【Result and conclusion】Diminazene-protein binding rate tested in vitro was within the range of 74.68%-95.90%. Although the drug-protein binding rate in vivo was within the range of 84.11%-89.69%（7 mg/kg, i.m.）, and 82.96%-88.65%（14 mg/kg, i.m.） after administration, and saturation phenomenon emerged as dosage increased. These factors should be considered in clinical regimens designing.
李 博,赵吉祥,陈杖榴,路文华,韩可可,徐 维,陈 红.三氮脒在猪血浆的药物 - 蛋白结合研究[J].华南农业大学学报,2014,35(2):24-27复制