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甲氰咪胍(cimetidine; tagamet)是一种新的H_2受体阻断剂,临床实践征明,它确是一个高效抗胃酸分泌药,迄今已被世界113个国家所采用,我国亦已生产并用于临床。去年10月在我国上海举行了甲氰咪胍国际讨论会,对进一步认识此药有较大的助益。有关此药的早期资料曾有过综述,本文试将近几年的动向综述如下。性状甲氰咪胍为无色结晶,分子量252.4,熔点141～142℃,可溶于水(37C、11.4g/L),水溶液pH为9.3,在稀酸中溶解度增大。溶液于室温、pH7.0时至少可稳定一周,但pH<2.0时则不稳定,被水解为胍脲衍生物。本品在37℃、pH9.2时的分配系数为2.5。
Cimetidine (cimetidine; tagamet) is a new H 2 receptor blocker, clinical practice, it is indeed a highly effective anti-gastric acid secretion drugs, so far has been adopted by 113 countries in the world, China has also produced and used In clinical. Last October, an international seminar on cimetidine was held in Shanghai, China, which is of great help to further understanding this medicine. The early data on this drug have been reviewed, this paper tries to review the trend in recent years are as follows. Properties Cimetidine is a colorless crystal with a molecular weight of 252.4 and a melting point of 141-142 ° C. It is soluble in water (37C, 11.4 g / L) and has an aqueous solution pH of 9.3. The solubility in dilute acids is increased. The solution is stable for at least a week at pH 7.0, but unstable at pH <2.0 and is hydrolyzed to the guanidinium derivative. This product at 37 ℃, pH9.2 when the distribution coefficient of 2.5.