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曲硫秦(TR)在人体中的生物利用度及其与胃液分泌和胃泌素血浆水平的关系。

Bioavailability of trithiozine (TR) in man and its relation to gastric secretion and gastrin plasma level.

作者信息

Gibiński K, Rybicka J, Górny E, Bielecka W

出版信息

Int J Clin Pharmacol Biopharm. 1979 Jan;17(1):48-52.

PMID:761954
Abstract

Pharmacokinetics and gastric secretion suppressing properties of a new drug, trithiozine (TR), were studied in man. Its availability, if taken orally, is prompt and very good; its blood plasma level lasts for over 5 hr. In basal conditions volume of gastric juice is suppressed by TR as it is by propantheline bromide (PPB). In contradistinction to PPB, TR reduces basal acid output. After histamine stimulation TR is not as effective as PPB in reducing both volume and acid output. TR did not appear to affect the plasma gastrin level. Lack of typical anticholinergic side-effects such as dryness in mouth, vision blurring, etc., on the one hand, and antisecretory activity limited to basal conditions on the other, seem to offer a new modification of the old approach to therapy of gastroduodenal ulcer. Clinical trials seem justified.

摘要

对一种新药三硫噻嗪(TR)的药代动力学和抑制胃分泌特性进行了人体研究。口服该药后,其吸收迅速且良好;血浆水平持续超过5小时。在基础状态下,TR可抑制胃液分泌,作用与溴丙胺太林(PPB)相似。与PPB不同的是,TR可降低基础胃酸分泌量。组胺刺激后,TR在减少胃液分泌量和胃酸分泌量方面不如PPB有效。TR似乎不影响血浆胃泌素水平。一方面,缺乏典型的抗胆碱能副作用,如口干、视物模糊等;另一方面,其抗分泌活性仅限于基础状态,这似乎为治疗胃十二指肠溃疡的传统方法提供了一种新的改良方式。临床试验似乎是合理的。

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