Krause W, Mechelke B
Research Laboratories of Schering Aktiengesellschaft, Berlin, Fed. Rep. of Germany.
Arzneimittelforschung. 1992 Sep;42(9):1079-82.
The placental transfer of abecarnil (isopropyl 6-(benzyloxy)-4- (methoxymethyl)9H-pyrido(3,4-b)indole-3-carboxylate, ZK 112 119, CAS 11184-1-85-1) was studied in the rabbit after i.v. injection of 0.1 mg/kg and oral dosing of 10 mg/kg using 14C-labeled drug and HPLC with fluorescence detection for measurement of the unchanged drug. Abecarnil easily passed the placental barrier and achieved high concentrations in the fetus. The concentration ratio C(fetus)/C(dam plasma) was 24 +/- 12 for all animals and time points. Metabolites were not able to cross the placental barrier to the same extent as the unchanged drug (ratio 1 +/- 2). The time courses of drug concentration and total radioactivity in the fetus were parallel to the respective time courses in the dams plasma. Accumulation of drug and metabolites upon multiple dosing, therefore, should not differ from that observed in the dam.
在兔体内静脉注射0.1mg/kg及口服给药10mg/kg后，使用14C标记药物和带荧光检测的高效液相色谱法测定原形药物，研究了阿贝卡尼（异丙基6-(苄氧基)-4-(甲氧基甲基)-9H-吡啶并(3,4-b)吲哚-3-羧酸酯，ZK 112 119，CAS 11184-1-85-1）的胎盘转运情况。阿贝卡尼很容易通过胎盘屏障并在胎儿体内达到高浓度。所有动物和时间点的胎儿与母体血浆浓度比C(胎儿)/C(母体血浆)为24±12。代谢产物不能像原形药物那样同等程度地通过胎盘屏障（比值为1±2）。胎儿体内药物浓度和总放射性的时间进程与母体血浆中的相应时间进程平行。因此，多次给药后药物和代谢产物的蓄积情况应与母体中观察到的情况无差异。
