Shevchenko R V, Litvin A A, Kolyvanov G B, Boĭko S S, Zherdev V P
Eksp Klin Farmakol. 2014;77(7):23-6.
Interspecies differences in pharmacokinetics of the original neuroleptic drug dilept have been studied in experimental animals (rabbits and rats) and volunteers after single oral administration of tablets and tablet mass of the drug. Parent drug in the rabbit blood plasma was detected for 4 h, in the rat plasma for about 2 h, and in the human blood plasma for about 1 h after drug administration. The degrees of dilept biotransformation into metabolites (defined as metabolism intensity, AUCM/AUCP) in rats were 21.3 (for M-1) and 1645 (for M-2), in human volunteers - 5.8 and 658.5, and in rabbits - 1.6 and 125.8, respectively. Thus, the intensity of drug metabolism in experimental animals and volunteers was different and decreased in the series rats humans rabbits.
在实验动物(兔子和大鼠)及志愿者单次口服原抗精神病药物二联苯哌啶片剂和片剂制剂后,对其药代动力学的种间差异进行了研究。给药后,在兔血浆中可检测到母体药物4小时,在大鼠血浆中约为2小时,在人血浆中约为1小时。二联苯哌啶转化为代谢产物的程度(定义为代谢强度,AUCM/AUCP)在大鼠中,M-1为21.3,M-2为1645;在人类志愿者中分别为5.8和658.5;在兔子中分别为1.6和125.8。因此,实验动物和志愿者体内药物代谢强度不同,且按大鼠、人类、兔子的顺序递减。