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小鼠、大鼠、仓鼠、兔子、狗、猴子和人类对β-肾上腺素能阻滞剂纳多洛尔的吸收:一种不寻常的物种差异。

Absorption of the beta-adrenergic-blocking agent, nadolol, by mice, rats, hamsters, rabbits, dogs, monkeys, and man: an unusual species difference.

作者信息

Dreyfuss J, Shaw J M, Ross J J

出版信息

Xenobiotica. 1978 Aug;8(8):503-8. doi: 10.3109/00498257809056152.

Abstract
  1. Dogs absorbed [14C]nadolol almost completely (88--104%) after oral administration of 10--75 mg/kg. In contrast, mice, rats, hamsters, and rabbits, given oral doses of 20 mg/kg, absorbed, at most, 25%. After administration of oral doses of 2--75 mg/kg, monkeys absorbed no more than an average of 30%. Six monkeys given oral doses of 10 mg/kg absorbed 12--44%. 2. In rats, [14C]nadolol was orally absorbed to an average of 13.7--17.5%, whether given in suspension or in solution, indicating that absorption was not limited by rate of dissolution nor by solubility. 3. Mildly hypertensive humans given single doses of [14C]nadolol (2 or 80 mg, orally) and normal subjects given single doses (10 mg, orally) absorbed an average of 20.4--33.3%.
摘要
  1. 口服给予10 - 75毫克/千克的[14C]纳多洛尔后,犬几乎完全吸收(88 - 104%)。相比之下,口服给予20毫克/千克剂量的小鼠、大鼠、仓鼠和兔,最多吸收25%。口服给予2 - 75毫克/千克剂量后,猴的平均吸收量不超过30%。6只口服给予10毫克/千克剂量的猴吸收了12 - 44%。2. 在大鼠中,无论给予混悬液还是溶液,[14C]纳多洛尔的口服平均吸收量为13.7 - 17.5%,这表明吸收不受溶解速率或溶解度的限制。3. 轻度高血压患者单次口服给予[14C]纳多洛尔(2毫克或80毫克)以及正常受试者单次口服给予(10毫克),平均吸收量为20.4 - 33.3%。

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