不同分散剂对沙咪珠利在比格犬体内暴露量影响的研究

EFFECTS OF DIFFERENT DISPERSANTS ON THE EXPOSURE OF EZL IN BEAGLE DOGS

沙咪珠利(EZL)是由中国农业科学院上海兽医研究所兽用抗感染药物创新团队自主研发的新型三嗪类抗球虫药物。前期的研究表明,沙咪珠利抗球虫效果好、低毒、安全性高,具有广阔的应用和开发前景。为了研究不同分散剂对沙咪珠利在实验动物比格犬体内暴露量的影响,本实验将水、0.5%羧甲基纤维素钠(CMCNa)、聚乙二醇(PEG)200三种分散剂分别制备沙咪珠利口灌液,对比格犬单次经口灌服后采集0～36 h不同时间点的血样,通过DAS3.0软件拟合获得沙咪珠利在比格犬体内主要药代动力学参数。结果表明:沙咪珠利经不同的分散剂制备的口灌液,给比格犬内服后,获得的AUC_((0-t))和C_(max)没有显著性差异(P>0.05),说明三种不同分散剂对沙咪珠利在比格犬体内的暴露量的影响差异不显著。通过暴露量研究,为该药的毒理学评价和临床的合理应用提供了理论参考。

EZL, a new triazine compound, was synthesized by shanghai veterinary research institute, Chinese academy of agricultural science. Previous studies demonstrate that EZL is effective, low-toxicity and safe. Therefore, it has broad application and development prospects. In order to illustrate the influence of EZL exposure of three diverse dispersants in beagle body, we compare the main pharmacokinetic parameters of three diverse dispersants, including water, 0.5%CMANa and PEG200, in beagle body. The results show that it has no obvious influence on durg exposure dissolving in diverse dispersants in beagle body, because AUC(0-t) and Cmax have no marked difference among the three groups (p>0.05). Through the study of exposure, it provides a theoretical reference for toxicological evaluation and rational clinical application of the drug.