抗孕唑(DL111-IT)在大鼠体内的吸收、分布和排泄  

Absorption, Distribution and Excretion of DL111-IT, a New Contragestational Agent, in Rats

作　　者：骆文莹[1] 刘志强[1] 李群 王临润[2] 姚磊[2] 

机构地区：[1]浙江医科大学药学系,杭州310006 [2]浙江医科大学药学系毕业班

出　　处：《现代应用药学》1991年第5期1-4,共4页

摘　　要：大鼠im抗孕唑很快被吸收并分布到各组织中,其中以子宫、卵巢含量最高,其次为肺、心、肾、肌肉,脑、骨中含量较少。大鼠iV抗孕唑后24h,从粪、尿中排出原形药量为0.084±0.039％,168h排出0.396±0.071％。12h内从胆汁排泄的原形药量占给药剂量的1.62±2.04％。可见原药进入体内后很快被代谢。im抗孕唑后1h,注射部位肌肉中的余留量约为给药剂量的50％。t_(1/2)(Ke)=228.812±96.112(min)。DL111-IT, 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1, 2, 4,-triazol, is a new contragestational agent. In this paper its absorption, distributions excretion in rats are reported.1h after im administration the peak level of DL111-IT was found in utero-ovaries. The decreasing order of DL111-IT distribution in other organs or tissue was as follows: lungs, heart, kidneys, muscle, brain, femur. Only trace level of DL111-IT was detected in these tissues 8h after im DL111-IT.After iv in rats, the total DL111-IT excreted in urine and feces was found to be 0.39±0.071％ within 168h. 1.62+2.04％ of an iv dose was recovered from the bile collected for 12h.pharmacokinetic parameters of one compartment model im DL111-IT 5mg/kg in 5 rats were t1/2(ke)=228.812±96.112 min.

关 键 词：抗孕唑 抗孕药 DL111-IT 体内分布 排泄 体内吸收 大鼠 

分 类 号：R979.21[医药卫生—药品]