发明名称 |
STABLE FORMULATION OF AMORPHOUS PERINDOPRIL SALTS, A PROCESS FOR THEIR PREPARATION, ESPECIALLY INDUSTRIAL PREPARATION, AND THEIR USE IN THE THERAPY OF HYPERTENSION |
摘要 |
There is disclosed a stable formulation of amorphous perindopril erbumine of the formula which is obtained in such a way that perindopril erbumine, which may also be prepared in situ from perindopril and tert-butylamine, or perindopril erbumine hydrate is dissolved in demineralized water or in a mixture of demineralized water and alcohol, to this solution a solution of sodium hydrogen carbonate is added for stabilization, inert ingredients for tabletting are wetted therewith, dried in vacuo by lyophilization or at normal pressure with a stream of warm air at not more than 40°C, hydrophobic additives to facilitate tabletting are added, it is homogenized and the granulate is tabletted. Disclosed is also a stable formulation of amorphous perindopril sodium salt obtained by modification of the drying procedure in the process of preparing the granulate. X-ray powder diffraction investigations show that perindopril erbumine is present in amorphous form and does not contain crystal a, ß and ? forms. |
申请公布号 |
WO2007058634(A1) |
申请公布日期 |
2007.05.24 |
申请号 |
WO2006SI00034 |
申请日期 |
2006.11.08 |
申请人 |
DIAGEN SMARTNO PRI LJUBLJANI, D.O.O.;RUCMAN, RUDOLF;ZUPET, PAVEL |
发明人 |
RUCMAN, RUDOLF;ZUPET, PAVEL |
分类号 |
A61K38/55;A61K9/16;A61K31/401;A61P9/12;C07D209/42 |
主分类号 |
A61K38/55 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|