Kuo S H, Johnson G E
Can J Physiol Pharmacol. 1975 Oct;53(5):888-94. doi: 10.1139/y75-122.
The biliary excretion rates of [14C]acetylprocaine amide ethobromide (acetyl-PAEB) and [3H]taurocholate, either administered alone or in combination to adult male Wistar rats, were studied. Their renal pedicles were ligated, and the common bile duct and one jugular vein cannulated. Acetyl-PAEB, 20 mg/kg, and sodium taurocholate, 70 mg/kg, were infused over a 5-min period. Blood and bile samples were collected every 10 min for 60 min. Liver samples were taken at 10 and 20 min. Approximately 100% of the administered taurocholate was excreted within 50 min. The simultaneous administration of acetyl-PAEB did not significantly alter the taurocholate excretion. The amount of the acetyl-PAEB dose excreted in 1 h was 9.4%. This was increased significantly to 16.5% when taurocholate was given concomitantly. The concentration of acetyl-PAEB in the bile increased significantly when taurocholate was given, and the ratios of its concentrations in bile-liver and bile-plasma were also increased. Taurocholate did not alter the liver-plasma concentration ratio of acetyl-PAEB. It is suggested that the concomitant administration of taurocholate increased the biliary excretion of acetyl-PAEB by facilitating its secretion by the liver into the bile.
研究了成年雄性Wistar大鼠单独或联合给予[14C]乙酰普鲁卡因酰胺乙溴化物(乙酰 - PAEB)和[3H]牛磺胆酸盐后的胆汁排泄率。结扎它们的肾蒂,并插入胆总管和一条颈静脉。在5分钟内输注20mg/kg的乙酰 - PAEB和70mg/kg的牛磺胆酸钠。每10分钟采集一次血液和胆汁样本,共采集60分钟。在10分钟和20分钟时采集肝脏样本。大约100%的给予的牛磺胆酸盐在50分钟内排泄。同时给予乙酰 - PAEB并没有显著改变牛磺胆酸盐的排泄。1小时内排泄的乙酰 - PAEB剂量为9.4%。当同时给予牛磺胆酸盐时,这一比例显著增加到16.5%。给予牛磺胆酸盐时,胆汁中乙酰 - PAEB的浓度显著增加,其在胆汁 - 肝脏和胆汁 - 血浆中的浓度比也增加。牛磺胆酸盐没有改变乙酰 - PAEB的肝脏 - 血浆浓度比。提示同时给予牛磺胆酸盐通过促进肝脏将其分泌到胆汁中而增加了乙酰 - PAEB的胆汁排泄。