TRWAŁY PREPARAT AMORFICZNYCH SOLI PERYNDOPRYLU, SPOSÓB ICH WYTWARZANIA, ZWŁASZCZA WYTWARZANIA W SKALI PRZEMYSŁOWEJ ORAZ ICH ZASTOSOWANIE W TERAPII NADCIŚNIENIA
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.
