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吲哚美辛胶囊在人体中的生物利用度。(I):生物利用度及胃酸的影响。

Bioavailability of indomethacin capsules in humans. (I): Bioavailability and effects of gastric acidity.

作者信息

Aoyagi N, Ogata H, Kaniwa N, Ejima A

出版信息

Int J Clin Pharmacol Ther Toxicol. 1985 Sep;23(9):469-74.

PMID:4055157
Abstract

The bioavailabilities of five indomethacin capsules, two commercial and three experimental products, were studied in ten human subjects. The bioavailabilities of the products increased in proportion to their in vitro dissolution rates, although one of the commercial products provided a relatively lower bioavailability than was expected. Comparison of the bioavailabilities between high and low gastric acidity humans revealed that the serum levels of the drug during the absorption phase following oral administration of all the indomethacin products, except for one commercial product, were higher in the low acidity subjects than in the high acidity subjects. Also, the mean peak serum level of the most rapidly dissolving product was 1.6 times higher in the low acidity subjects than in the high acidity ones. These gastric acidity effects indicated enhanced dissolution of indomethacin from the capsules in the stomach of low acidity humans.

摘要

在10名人体受试者中研究了5种吲哚美辛胶囊(2种市售产品和3种实验产品)的生物利用度。产品的生物利用度与其体外溶出速率成正比,尽管其中一种市售产品的生物利用度相对低于预期。高胃酸和低胃酸人群之间生物利用度的比较显示,除一种市售产品外,口服所有吲哚美辛产品后吸收阶段的药物血清水平在低胃酸受试者中高于高胃酸受试者。此外,溶解最快的产品在低胃酸受试者中的平均血清峰值水平比高胃酸受试者高1.6倍。这些胃酸影响表明吲哚美辛在低胃酸人群胃中从胶囊中的溶出增强。

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