发明名称 NOVEL CRYSTALLINE FORMS OF PERINDOPRIL ERBUMINE
摘要 Disclosed are two novel crystalline forms δ and &egr; of perindopril erbumine, which are suitable as therapeutic substances in medicaments used for treating cardiovascular diseases, especially high blood pressure and cardiac insufficiency. Crystalline form &egr; is obtained by crystallizing perindopril erbumine from MTBE containing 1.5 to 2.5 % (v/v) of water at 30 to 45°C, preferably 34 to 45°C, crystallization expediently taking place by stirring. Crystalline form &egr; changes into crystalline form δ if the water is removed, practically by azeotropic distillation, preferably at 35 to 37°C, and stirring continues for at least 15 h at 30 to 45°C, preferably 35 to 37°C. Crystalline form δ can also be obtained by stirring crystalline form in tert-butyl methyl ether containing 0.9 to 1.4 % (v/v) of water at 33 to 38°C while inoculating the same with crystalline form δ. Crystalline form &egr; can further be obtained by stirring crystalline form α or &bgr; in tert-butyl methyl ether containing 0.9 to 1.4 % (v/v) of water at 28 to 35°C while inoculating the same with crystalline form &egr;, or by stirring crystalline form α or &bgr; in tert-butyl methyl ether containing 1.5 to 2.0 % (v/v) of water at 35 to 38°C.
申请公布号 EA008603(B1) 申请公布日期 2007.06.29
申请号 EA20050001859 申请日期 2004.06.18
申请人 LES LABORATOIRES SERVIER 发明人 STRASSLER CHRISTOPH;LELLEK VIT;FASSLER ROGER
分类号 C07D209/42 主分类号 C07D209/42
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