磺胺二甲嘧啶及其N_4-乙酰化代谢物在兔的药动学研究

PHARMACOKINETICS OF SULFADIMIDINE AND ITS N_4-ACETYL METABOLITE IN RABBITS

快速静注200mg/kg后,磺胺二甲嘧啶(SM_2)在兔体内迅速发生消除,t_(1/2)β为1.6±1.3h。N_4^-乙酰化代谢是其主要的消除方式,消除所给剂量62.1％。12.7±1.1和2.8±1.8％的药物以原型分别从肾脏和胃肠道排泄。N_4^-乙酰基磺胺二甲嘧啶(N_4SM_2)的形成和消除都很迅速,t_(1/2)分别为0.6±0.4和2.2±1.1h。SM_2及其N_4SM_2的药动学特性是由兔的生理生化特点所决定,临床用药时要注意。

Sulfadimidine ( SM2 ) is one of the extensively used drugs in animal production. Its phar-macokinetic behavior difiers among the species. SM3 is often used for therapeutic and prophylactic purposes in rabbit diseases, but there has been no report on its pharmacokinetics in rabbits. The present study showed that SM2 was eliminated fast in rabbits with an elimination half-life time of 1.6±1.3h following iatraveaous bolus injection of a single dose of 200 mg/kg. It was metabolized in the liver to N4-acetyl metabolite ( N4SM2 ) which accounted for 62.1 per cent of the administered dose. Of the administered dose, 12.7±1.1 and 2.8±1.8 per cent were excreted in the original form by the kidney and gastro-intestinal tract, respectively. The haltlives of the formation and the elimination of N4SM2 were 0.6±0.4 and 2.2±1.1 h ,respectively. Such pharmacokinetic behaviors of SM2 and N4SM2 was due to the physiologic and biochemical peculiarities of the rabbit.