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贝诺洛芬经直肠给药后的药代动力学及可接受性

The pharmacokinetics and acceptability of benoxaprofen following rectal administration.

作者信息

Jones R W, Waugh A E, Woodage T J, Wild R N, Glynne A

出版信息

J Rheumatol Suppl. 1980;6:20-6.

PMID:6930484
Abstract

The bioavailability of a single 300 mg dose of benoxaprofen was compared after rectal and oral administration in 5 subjects. The total absorption rectally from a suppository was 83% of that achieved orally from a capsule. Six further subjects took a 300 mg benoxaprofen suppository twice daily for 12 d. Steady state plasma levels (mean level 94 microgram/ml) were reached at about 120 h, while the elimination half-life for benoxaprofen was approximately 38 h in this study. The suppositories were well tolerated. The plasma levels obtained compared very favorably with theoretically expected levels and levels obtained after comparable oral doses.

摘要

在5名受试者中比较了单次300毫克剂量的贝诺洛芬经直肠给药和口服给药后的生物利用度。栓剂经直肠的总吸收量为口服胶囊吸收量的83%。另外6名受试者每天两次服用300毫克贝诺洛芬栓剂,共服用12天。约120小时达到稳态血浆水平(平均水平为94微克/毫升),而在本研究中贝诺洛芬的消除半衰期约为38小时。这些栓剂耐受性良好。所获得的血浆水平与理论预期水平以及相当口服剂量后获得的水平相比非常有利。

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