复方新诺明在罗氏沼虾中的药代动力学和组织分布

研究了单剂量肌肉注射给药甲氧苄氨嘧啶(SMZ)0 60 mg/kg]、口灌给药磺胺甲基异噁唑(SMZ)100 mg/kg]和复方口灌给药(SMZ 100 mg/kg和TMP 20 mg/kg)三种给药方式下,SMZ和TMP在罗氏沼虾中的代谢动力学,分析了SMZ和TMP血淋巴、肌肉和肝胰腺中的分布特征。结果表明,SMZ以肌肉注射方式给药后的血淋巴中,药物经时浓度曲线符合二室开放房室模型,而SMZ&TMP口灌给药后却不能用房室模型拟合。肌注给药后,SMZ的消除半衰期(t1/2β)为24.92 h,单方和复方口灌给药后SMZ的消除半衰期(t1/2β)分别为40.70和47.197 h。复方口灌给药后TMP的消除半衰期(t1/2β)为28.77 h,TMP对SMZ的药代动力学并无显著影响。口灌给药后,SMZ和TMP在肝胰腺中的药物浓度高于同时间肌肉中的药物浓度,但肌肉和肝胰腺中的SMZ消除速度基本一致。

Pharmacokinetics, Tissue Distribution of Sulfamethoxazole and Trimethoprim in Macrobranchium rosenbergii

The research on pharmacokinetics and metabolism of the sulfamethoxazole(SMZ) and trimethoprim(TMP) was made after intramuscular(SMZ 60 mg/kg) or oral SMZ 100 mg/kg or the combination of SMZ(100 mg/kg) and TMP(20 mg/kg)] administration in Macrobranchium rosenbergii.The hemolymph,muscle and hepatopancreas were sampled.The hemolymph data conformed to a two-com-partment model after intramuscular administration,whereas the hemolymph data after oral(SMZ &TMP) administration could not be fitted with compartmental models.The elimination half-life(t1/2β) of SMZ was 24.92 h after intramuscular administration,and t1/2β of SMZ was 40.70 and 47.197 h after SMZ solely and compound oral administration.t1/2β of TMP was 28.77 h after TMP compound oral administration.The results indicated that oral administration of the combination of SMZ and TMP had no distinct impact on the pharmacokinetics of SMZ in contrast with that of SMZ singly oral administration.Hepatopancreas levels indicated higher SMZ and TMP values than respective muscle levels at all time points after oral administration.The amount of SMZ in muscle and hepatopancreas decreased faster than that of TMP in same tissues.