STABILISIERTE ARZNEISTOFFE, VERFAHREN ZU IHRER HERSTELLUNG SOWIE STABILE ARZNEIZUBEREITUNGEN.

摘要

N-aminocarbonylmethyl -alpha-amino acid derivs. of formula (I) or their physiologically acceptable salts are stabilised (a) by a protective polymeric coating and/or (b) by addn. of an acceptable buffer which, in a pharmaceutical compsn. in presence of moisture, provides a weakly acidic to weakly basic pH. R is H, 1-4C alkyl or phenyl, R1 is 1-4C alkyl or -(CH2)m-NAB, m is 1-4, A and B are H or 1-4C alkyl, R2 is H, 1-4C alkyl or benzyl, R3 is H or 1-4C alkyl, R4 and R5 together complete a heterocyclic, mono- bi- or tri-cyclic ring system, hydrogenated or partly hydrogenated, contg. one N and 4-15 ring C and opt. substd. by 1 or 2 1-4C alkoxy. (I) is ramipril (Ia, 2-(N-((S)-1-ethoxycarbonyl -3-phenylpropyl-L-alanyl (15,35,55)-2-azabicyclo (3,3,0) octane-3-carboxylic acid).