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索洛芬的生物利用度和血小板聚集抑制活性。与布洛芬的比较。

Bioavailability and platelet aggregation inhibitory activity of solufenum. A comparison with ibuprofen.

作者信息

Latini R, Villa S, Gerna M, Tognoni G, de Gaetano G

出版信息

Int J Clin Pharmacol Biopharm. 1977 Oct;15(10):492-5.

PMID:924705
Abstract

Bioavailability and platelet aggregation inhibitory activity of the lysine salt of ibuprofen (solufenum) were compared with those of the parent molecule in 5 healthy male volunteers. The study had a randomized, cross-over design. The average peak plasma level and the area under the curve were higher when solufenum was administered orally as compared to the same preparation given i.m. or as compared to oral ibuprofen. However, the bioavailability of the 3 preparations studied was not significantly different. In contrast, the inhibitory effect on adrenaline-induced platelet aggregation appeared significantly different. In contrast, the inhibitory effect on adrenaline-induced platelet aggregation appeared significantly earlier after the administration of both solufenum than after ibuprofen. The clinical relevance of these findings is discussed.

摘要

在5名健康男性志愿者中,比较了布洛芬赖氨酸盐(索洛芬)与其母体分子的生物利用度和血小板聚集抑制活性。该研究采用随机交叉设计。与肌肉注射相同制剂或口服布洛芬相比,口服索洛芬时的平均血浆峰值水平和曲线下面积更高。然而,所研究的3种制剂的生物利用度没有显著差异。相比之下,对肾上腺素诱导的血小板聚集的抑制作用似乎有显著差异。相比之下,服用索洛芬后对肾上腺素诱导的血小板聚集的抑制作用比服用布洛芬后显著更早出现。讨论了这些发现的临床意义。

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