Terhaag B, Richter K, Diettrich H
Int J Clin Pharmacol Biopharm. 1978 Dec;16(12):607-9.
The concentration in plasma and bile of carbamazepine was determined in four humans with Kerr's T-tube drain after an oral administration of a single dose of 400 mg of Finlepsin (carbamazepine). The mean plasma half-life time was 25 (15-31) hr. The concentration time curves in bile and plasma were parallel with the bile to plasma concentration ratio of 0.62 (0.24-0.82). A negative linear correlation between the lithogenic index and the bile plasma concentration ratio was found. It is suggested that the concentration of carbamazepine in bile is influenced by the saturation of biliary micelles with cholesterol. The amount of carbamazepine eliminated by bile within 72 hr was 4.1 +/- 1.9 mg, i.e., 1% of the administered dose. It is concluded that there is no significant enterohepatic circulation of carbamazepine.
在4名带有克尔T型管引流装置的人体中，口服单剂量400毫克的立痛定（卡马西平）后，测定了血浆和胆汁中卡马西平的浓度。血浆平均半衰期为25（15 - 31）小时。胆汁和血浆中的浓度-时间曲线平行，胆汁与血浆浓度比为0.62（0.24 - 0.82）。发现致石指数与胆汁-血浆浓度比之间呈负线性相关。提示胆汁中卡马西平的浓度受胆汁微胶粒中胆固醇饱和度的影响。72小时内胆汁排出的卡马西平量为4.1±1.9毫克，即给药剂量的1%。结论是卡马西平不存在显著的肝肠循环。
