Greenblatt D J, Divoll M K, Harmatz J S, Shader R I
Department of Psychiatry, Tufts University School of Medicine, Boston, Mass.
Pharmacology. 1988;36(2):125-33. doi: 10.1159/000138369.
Twelve young (24-41 years) and 11 elderly (62-77 years) volunteer subjects received a single 1.0-gram dose of antipyrine on three occasions: intravenously, orally in the fasting state and orally following a standard breakfast. Plasma antipyrine concentrations were determined for 24 h after each dose. Compared to young males, elderly men had significantly prolonged elimination half-life (17 vs. 11 h, p less than 0.025) and reduced clearance (32 vs. 54 ml/min, p less than 0.06). However, elderly and young women did not differ in half-life (12 vs. 11 h) or clearance (37 vs. 44 ml/min). After oral dosage in the fasting state, young and elderly groups (regardless of gender) did not differ in peak plasma antipyrine concentration (Cmax) or time of peak concentration (Tmax). Absolute bioavailability was not significantly less than 100% and was not related to age. Postprandial oral dosage of antipyrine caused reduced Cmax and prolonged Tmax in all groups, but absolute bioavailability was not significantly less than 100%. Again, there were no age-related differences. Although aging may lead to reduced clearance of antipyrine among men, there is no evidence that old age is associated with impairment of the rate or extent of antipyrine absorption from the gastrointestinal tract.
12名年轻(24 - 41岁)和11名老年(62 - 77岁)志愿者受试者分三次接受了单次1.0克剂量的安替比林:静脉注射、空腹口服以及标准早餐后口服。每次给药后测定24小时的血浆安替比林浓度。与年轻男性相比,老年男性的消除半衰期显著延长(17小时对11小时,p小于0.025),清除率降低(32毫升/分钟对54毫升/分钟,p小于0.06)。然而,老年女性和年轻女性在半衰期(12小时对11小时)或清除率(37毫升/分钟对44毫升/分钟)方面没有差异。空腹口服给药后,年轻组和老年组(无论性别)的血浆安替比林峰值浓度(Cmax)或达峰时间(Tmax)没有差异。绝对生物利用度并不显著低于100%,且与年龄无关。安替比林餐后口服导致所有组的Cmax降低和Tmax延长,但绝对生物利用度并不显著低于100%。同样,也没有与年龄相关的差异。虽然衰老可能导致男性安替比林清除率降低,但没有证据表明老年与胃肠道安替比林吸收速率或程度受损有关。