Queneau P, Decousus H, Ollagnier M, Cherrah Y, Perpoint B, Hocquart J
Rev Rhum Mal Osteoartic. 1985 Jun;52(6):403-8.
The aim of the study was to evaluate a possible chronokinetic phenomenon of ketoprofen administered orally and by continuous intravenous infusion. In the first part of the study, ketoprofen was administered orally to 8 healthy male volunteers aged between 25 and 45 years, at a dose of 2 X 50 mg at 7:00 a.m. (time I), 1:00 p.m. (time II), 7:00 p.m. (time III) and 1:00 a.m. (time IV), on the same day of the week at an interval of 2 weeks, during the first three months of the year. The order of administration was randomised, each subject acted as his own control and received ketoprofen at the four times mentioned above. A total of 14 venous blood samples were taken over 12 hours. The results indicate that the maximal serum concentration (Cmax) was significantly higher at time I (13.4 +/- 14.1) than at times II, III and IV (6.9 +/- 1.1, 7.2 +/- 0.7, 6.4 +/- 0.5 mg/l) (p less than 0.01). The time required to reach this concentration (Tmax) was significantly longer for time IV (135.0 +/- 16,8) than for times I, II and III (73,1 +/- 14.1, 75,0 +/- 16.6; 82.5 +/- 12.7 minutes) (p less than 0.05). The excretion half-life (t 1/2B) was significantly longer for time IV (4.3 +/- 0.6) than for times II and III (2.8 +/- 0.5, 2.5 +/- 0.2 hours) (p less than 0.05). Statistically significant differences were also observed in the area under the curve measured at midday (AUC 12) and in the total clearance (CIT) for the various sample times.(ABSTRACT TRUNCATED AT 250 WORDS)
该研究的目的是评估口服和持续静脉输注酮洛芬时可能存在的时间动力学现象。在研究的第一部分,对8名年龄在25至45岁之间的健康男性志愿者口服酮洛芬,剂量为2×50毫克,于上午7点(时间I)、下午1点(时间II)、晚上7点(时间III)和凌晨1点(时间IV)服用,在一年的前三个月中,于同一周的同一天每隔2周给药一次。给药顺序是随机的,每个受试者作为自身对照,在上述四个时间点接受酮洛芬。在12小时内共采集了14份静脉血样。结果表明,时间I时的最大血清浓度(Cmax)(13.4±14.1)显著高于时间II、III和IV时(6.9±1.1、7.2±0.7、6.4±0.5毫克/升)(p<0.01)。达到该浓度所需的时间(Tmax),时间IV(135.0±16.8)显著长于时间I、II和III(73.1±14.1、75.0±16.6;82.5±12.7分钟)(p<0.05)。排泄半衰期(t 1/2B),时间IV(4.3±0.6)显著长于时间II和III(2.8±0.5、2.5±0.2小时)(p<0.05)。在中午测量的曲线下面积(AUC 12)以及不同采样时间的总清除率(CIT)方面也观察到了统计学上的显著差异。(摘要截取自250字)