法莫替丁的药理研究

Pharmacological Study on Famotidine

法莫替丁为第三代组胺H_2受体阻滞剂,由脒基硫脲经五步反应合成,总收率27.4％。该药A、B二种晶型经药效学和药代动力学参数比较,B晶型优于A晶型。在一定条件下,A、B晶型可互相转晶,并可用BSC仪测定含量,治疗胃溃疡六周及十二指肠溃疡四周有效率分别为96.6％和89.9％。

Famotidine, third generation of histamine H_2-receptor antagonist, was synthesized from amidinothiourea in five steps in ove-all yield of 27.4% and had two different crystalline forms A and B The crystalline form B showed the better parameters in the pharmacodynamic and pharmacokinetic study than that of form A The content of two crystals could be measured by DSC method and the A and B could also be transformed each other under the certain suitable conditions. In clinical trials, the response rate of famotidine to gastric and duodenum ulcer in six and four weeks treatment was 96.6 and 89.8%, respectively.