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新型组胺H2受体拮抗剂雷尼替丁对海登海因小胃犬促分泌剂刺激的胃液分泌的影响(作者译)

[Effects of ranitidine, a new histamine H2-receptor antagonist, on secretagogue-stimulated gastric secretion in Heidenhain pouch dogs (author's transl)].

作者信息

Ohtsuki H, Okabe S

出版信息

Nihon Yakurigaku Zasshi. 1981 Dec;78(6):539-47.

PMID:6120885
Abstract

The effects of ranitidine on gastric secretion stimulated with gastric secretagogues were studied in 6 Heidenhain pouch dogs (both male beagle and mongrel). Cimetidine was used as a reference drug. Either histamine 2HCl (40 micrograms/kg), pentagastrin (2 micrograms/kg) or carbachol (2 micrograms/kg) was given intramuscularly, every 15 min for 120 min. Gastric juice was collected at each 15 min interval and analyzed for volume, acidity and pepsin activity. Either ranitidine (0.3, 1 or 10 mg/kg) or cimetidine (1 or 10 mg/kg), packed in a gelatin capsule, was given orally 60 min before the initial injection of each stimulant. Both ranitidine and cimetidine dose-dependently inhibited histamine- and pentagastrin-stimulated gastric secretion (volume, acid and pepsin output). These agents also inhibited the carbachol-stimulated secretion, but the antisecretory effects were weak as compared with their effects on histamine- and pentagastrin-stimulated secretions. The antisecretory effect of ranitidine on each stimulant is roughly 2 to 17 times more potent than cimetidine on the basis of ED50 (anti-secretory dose which inhibits gastric secretion by 50%). The antisecretory effect of ranitidine (10 mg/kg) on pentagastrin-stimulated secretion was observed even 10 hr after its oral administration.

摘要

在6只海登海因小胃犬(雄性比格犬和杂种犬)身上研究了雷尼替丁对胃分泌刺激剂刺激的胃酸分泌的影响。西咪替丁用作对照药物。每隔15分钟肌肉注射2HCl组胺(40微克/千克)、五肽胃泌素(2微克/千克)或卡巴胆碱(2微克/千克),共注射120分钟。每隔15分钟收集一次胃液,并分析其体积、酸度和胃蛋白酶活性。在每次注射每种刺激剂前60分钟口服装入明胶胶囊的雷尼替丁(0.3、1或10毫克/千克)或西咪替丁(1或10毫克/千克)。雷尼替丁和西咪替丁均剂量依赖性地抑制组胺和五肽胃泌素刺激的胃酸分泌(体积、酸和胃蛋白酶分泌量)。这些药物也抑制卡巴胆碱刺激的分泌,但与它们对组胺和五肽胃泌素刺激的分泌的作用相比,其抗分泌作用较弱。基于ED50(抑制胃酸分泌50%的抗分泌剂量),雷尼替丁对每种刺激剂的抗分泌作用比西咪替丁强约2至17倍。雷尼替丁(10毫克/千克)对五肽胃泌素刺激的分泌的抗分泌作用在口服后10小时仍可观察到。

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