人体中吲哚美辛的血清浓度。剂量、食物和抗酸剂的影响。
Indomethacin serum concentrations in man. Effects of dosage, food, and antacid.
作者信息
Emori H W, Paulus H, Bluestone R, Champion G D, Pearson C
出版信息
Ann Rheum Dis. 1976 Aug;35(4):333-8. doi: 10.1136/ard.35.4.333.
Abstract
In the use of anti-inflammatory compounds, sustained serum levels are thought to be related to drug efficacy. This study shows that frequent clinical administration of indomethacin can result in sustained serum levels of the drug and that food and antacid may have important modifying effects on serum indomethacin concentrations. After oral ingestion by fasting subjects, indomethacin rapidly appeared in the serum, usually reaching peak concentrations in 30 to 90 minutes. Food delayed and decreased the mean peak level; antacid delayed the peak and slightly enhanced subsequent concentrations. With multiple dose schedules plateau levels were reached after 24 hours. When a total daily dose of 150 mg was given as 25 mg every 4 hours peak concentrations were the same but fluctuations were smaller and average concentrations were higher than with a dosage of 50 mg every 8 hours.
摘要
在使用抗炎化合物时，血清药物浓度持续维持被认为与药物疗效相关。本研究表明，频繁临床给药吲哚美辛可使药物血清浓度持续维持，且食物和抗酸剂可能对血清吲哚美辛浓度产生重要的调节作用。空腹受试者口服吲哚美辛后，药物迅速出现在血清中，通常在30至90分钟内达到峰值浓度。食物会延迟并降低平均峰值水平；抗酸剂会延迟峰值出现并略微提高随后的浓度。采用多剂量方案时，24小时后达到平稳状态。当每日总剂量150毫克以每4小时25毫克给药时，峰值浓度相同，但波动较小，且平均浓度高于每8小时给药50毫克的方案。
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