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吲哚美辛片在男性志愿者中的生物利用度。

Bioavailability of indomethacin tablets in men volunteers.

作者信息

Groth P E, Dunn J M

出版信息

Clin Pharm. 1986 Oct;5(10):820-4.

PMID:3780150
Abstract

Indomethacin bioavailability was compared in 22 healthy men who received two tablet dosage formulations and a capsule formulation of indomethacin in a three-way crossover study. In each study period, 50 mg of the indomethacin formulation (25-mg or 50-mg tablets or 50-mg capsules) was administered as a single dose to fasting subjects. Thirteen blood samples were collected at intervals over 24 hours after each dose. Urine samples were collected for 12 hours before each dose and 48 hours after each dose. Serum indomethacin concentrations were measured by a gas chromatographic procedure. The extent of indomethacin absorption for the two tablet formulations was not significantly different from that for the reference capsule. A trend toward earlier and higher peak serum concentrations with the capsule was observed. There was less than 20% difference in mean values for area under the concentration-time curve (AUC) for the three formulations. More than 75% of the subjects had serum concentrations falling between 75 and 125% of the mean serum concentrations. The extent of absorption of indomethacin from the two tablet formulations was similar to that from the capsule.

摘要

在一项三交叉试验中,对22名健康男性给予两种片剂剂型和一种胶囊剂型的吲哚美辛,比较其生物利用度。在每个研究阶段,将50mg吲哚美辛制剂(25mg或50mg片剂或50mg胶囊)单剂量给予空腹受试者。每次给药后24小时内间隔采集13份血样。在每次给药前12小时和给药后48小时收集尿样。采用气相色谱法测定血清吲哚美辛浓度。两种片剂剂型的吲哚美辛吸收程度与参比胶囊无显著差异。观察到胶囊剂型有血清浓度峰值出现更早、更高的趋势。三种剂型的浓度-时间曲线下面积(AUC)平均值差异小于20%。超过75%的受试者血清浓度在平均血清浓度的75%至125%之间。两种片剂剂型的吲哚美辛吸收程度与胶囊剂型相似。

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