The present invention relates to a pharmaceutical composition for the treatment of type 2 diabetes in mammals including human beings, wherein the pharmaceutical composition contains (R)-7-[3-amino-4-(2,4,5-trifluo-phenyl)-butyryl]-3-trifluomethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylic acid methyl ester or its pharmaceutically acceptable salts and rosiglitazone or pioglitazone or their pharmaceutically acceptable salts, preparation method thereof and a method of treating type 2 diabetes in mammals including human beings with the composition.本發明公開了治療包括人類之哺乳動物中第2型糖尿病的醫藥組成物,特別是含有(R)-7-[3-胺基-4-(2,4,5-三氟-苯基)-丁醯基]-3-三氟甲基-5,6,7,8-四氫-咪唑並[1,5-a]吡嗪-1-羧酸甲酯或其藥學上可接受的鹽和羅格列酮或吡格列酮或它們藥學上可接受的鹽的固定劑量組合的醫藥組成物,製備該醫藥組成物的方法和該醫藥組成物治療包括人類之哺乳動物中第2型糖尿病的用途。