生物样品中莱曼宁的气相色谱测定及其在动物体内的药代动力学

本文采用气相色谱法分离并测定了生物样品中莱曼宁的浓度,研究了莱曼宁在动物体内的吸收、分布和排泄过程。小鼠ig莱曼宁后的吸收速率常数为0.73h~(-1)。大鼠4h的胆汁排泄量仅为给药量的0.6％,大鼠尿中32h排泄量为给药量的13.3％。大鼠iv给药后体内过程符合二房室特征。大鼠体内分布以肾脏最高,其次为脾、肝、心、脑,外周组织如脂、肌含量较少。莱曼宁与兔血浆蛋白的结合率为49.2％。

Gas chromatographic determination of lehmannine in biological specimens and its pharmacokinetics of the drug

A method of gas chromato graphy for the determination of lehmannine in biological specimens was developed and used in the studies of the pharmacokinetics of the drug in animals. The method was simple, highly specific and precise.After oral administration, 1hmannine was found to be readily absorbed from the mouse gastro-interstinal tract(t1/2=57 min). The pharmacokinetics of lehmannine in rat was fitted by an open two compartmentmodel. The pharmacokinetic parameters were as follows: t1/2α=1.23 min, t1/2β=28.1 min, k12=0.354 min-1, k10=0.122 min-1, k21=0.113 min-1, Vss=0.768 1/kg, Vb = 0.790 1/kg, Vc=0.158 1/kg, MRT=39.9 min. After iv administration of lehmannine in a dose of 20 mg/kg, about 13.3% of the dose was recovered from the rat urine within 32 hours. And 0.63% of the dose was recovered from the rat bile with 4 hours. At 20 minutes after iv injection in rat, high levels of lehmannine was found in the kidney, moderate in spleen, liver, heart and brain and low in adipose tissue and muscle. These results indicated that lehmannine was dis. tributed widely in the body and eliminatedrapidly. The plasma binding rate in rabbit on five dosage levels were 19.2±1.0%.