普拉西坦在动物体内的药物代谢动力学  

Pharmacokinetics of Pramiracetam in Animals

作　　者：方治平[1] 刘小康[1] 肖逸[1] 蒋维[1] 

机构地区：[1]华西医科大学基础医学院药理学教研室,成都610041

出　　处：《华西医科大学学报》1999年第4期411-413,共3页Journal of West China University of Medical Sciences

摘　　要：为研究普拉西坦在犬和大鼠体内药代动力学规律，给犬灌服普拉西坦后，抽取不同时间的血液，分离血浆，用ＨＰＬＣ测定血浆中药物浓度，采用３ｐ８７ 程序计算药代参数；应用ＨＰＬＣ测定大鼠灌服普拉西坦后各组织和胆汁、尿、粪中药物浓度。结果显示：血药浓度－时间曲线符合一室开放模型，其体内的Ｔ１／２为２．３～３．９ 小时；大鼠灌服普拉西坦后３ 小时各组织中有较高的浓度，以肾脏为最高，肝脏次之，依序为肠、肺、肌、心、生殖腺、脾、脂肪；脑组织也能测到一定的量。２４小时从胆汁排泄原形药物占给药量的０．７％ ，７２小时从尿和粪中排出原形药物量分别占给药量的２８．２６％ 和６．３５％ 。用平衡透析法测定普拉西坦的血浆蛋白结合率约为２０．１％ ～２２．２％ 。以上结果表明，普拉西坦吸收快，分布广，消除也快。Pharmacokinetic rules of pramiracetam were studied here. After giving pramiracetam orally to dogs, we drew their blood at various times. The drug concentrations in blood plasma were detected by HPLC. 3p87 program was used to calculate the pharmacokinetic parameters.The time concentration curve corresponded to one apartment model. T 1/2 was about 2.3 3.9 hours in various doses. After pramiracetam was given to rats per os, high concentrations of pramiracetam were detected in the rats' tissues.The kidney had the highest concentration of pramiracetam; the liver had the next highest concentration, and then the intestine, lung, muscle, heart, gonad, spleen and sebum had the high concentration in order. The drug was also detected in the brain. 0.7% of the given dose was excreted in unchanged form in bile in 24 hours. 28.26% and 6.35% were excreted in urine and feces respectively in 72 hours. The plasma protein combining rate detected by the method of balance dialysis was 20.1 22.2%.

关 键 词：普拉西坦 药代动力学参数 组织分布 血浆蛋白结合率 

分 类 号：R971[医药卫生—药品]