Divoll M, Ameer B, Abernethy D R, Greenblatt D J
J Am Geriatr Soc. 1982 Apr;30(4):240-4. doi: 10.1111/j.1532-5415.1982.tb07093.x.
Twenty-eight healthy volunteers (age range, 22-78 years) received 650 mg of acetaminophen (AAP) on three separate occasions. The modes of administration were 1) intravenous, 5-minute infusion; 2) oral, with two 325-mg tablets; and 3) oral, with 650 mg as an elixir preparation. Plasma levels of AAP were determined in blood samples drawn up to 12 hours after the dose. The mean (+/- sd) kinetic variables for absorption of AAP from tablets in young and elderly were peak plasma concentration, 11.8 (+/- 4.2) vs 10.9 (+/- 4.1) micrograms/ml; peak time, 0.79 (+/- .54) vs 0.69 (+/- .40) hours after the dose; absorption half-life, 12.6 (+/- 9.8) vs. 8.2 (+/- 5.3) minutes; and absolute systemic availability, 79 (+/- 9) vs 72 (+/- 11) per cent. For AAP elixir, the corresponding values were 12.6 (+/- 5.4) vs 13.7 (+/- 6.0) micrograms/ml; 0.52 (+/- .24) vs 0.54 (+/- .51) hours; 8.6 (+/- 6.2) vs 6.1 (+/- 6.6) minutes; and 87 (+/- 9) vs 80 (+/- 9) per cent. Absolute bioavailability of both oral dosage forms was significantly less then 100 per cent in all groups. Elderly subjects tended to show lower availability of both oral preparations, but the difference was of borderline significance (P less than .50). Age did not influence any other measures of absorption. Since the absorption rate of acetaminophen may be indicative of the gastric emptying rate, age does not appear to alter this rate-limiting step in drug absorption.
28名健康志愿者(年龄范围22 - 78岁)分三次接受650毫克对乙酰氨基酚(AAP)。给药方式分别为:1)静脉注射,5分钟输注;2)口服,两片325毫克片剂;3)口服,650毫克酏剂制剂。在给药后长达12小时采集的血样中测定AAP的血浆水平。年轻和老年受试者从片剂中吸收AAP的平均(±标准差)动力学变量为:血浆峰浓度,11.8(±4.2)对10.9(±4.1)微克/毫升;达峰时间,给药后0.79(±0.54)对0.69(±0.40)小时;吸收半衰期,12.6(±9.8)对8.2(±5.3)分钟;绝对全身可用性,79(±9)对72(±11)%。对于AAP酏剂,相应值为12.6(±5.4)对13.7(±6.0)微克/毫升;0.52(±0.24)对0.54(±0.51)小时;8.6(±6.2)对6.1(±6.6)分钟;87(±9)对80(±9)%。所有组中两种口服剂型的绝对生物利用度均显著低于100%。老年受试者两种口服制剂的可用性往往较低,但差异具有临界显著性(P小于0.50)。年龄不影响任何其他吸收指标。由于对乙酰氨基酚的吸收速率可能指示胃排空速率,年龄似乎不会改变药物吸收中的这一限速步骤。