| 摘要 |
<p>A method for stabilizing a polymorphic form of fluvastatin sodium (I) in solid medicaments (A) involves adjusting the water content and water activity of (A) to specific values and keeping the water activity constant during storage. Independent claims are also included for the following: (1) medicaments (A') containing morphologically pure (I) as the racemate in form C or D or the 3R,5S- or 3S,5R-enantiomer in form B1 or B2 as active agent and at least one auxiliary, where (A') has a water content of at least 8% (preferably 8-12%) and a water activity of 20-60%; (2) medicaments (A') containing morphologically pure (I) as the racemate in form F or the 3R,5S- or 3S,5R-enantiomer in form D as active agent and at least one auxiliary, where (A') has a water content of at least 10% (preferably 10-20%) and a water activity of at least 75% (preferably 75-95%); (3) medicaments (A') containing morphologically pure (I) as the racemate or the 3R,5S- or 3S,5R-enantiomer, both in form A, as active agent and at least one auxiliary, where (A') has a water content of at most 5% (preferably 0-5%) and a water activity of at most 10% (preferably 0-10%); and (4) medicaments (A') containing morphologically pure (I) as the racemate in form E or the 3R,5S- or 3S,5R-enantiomer in form C as active agent and at least one auxiliary, where (A') has a water content of at least 10% (preferably 10-15%) and a water activity of 50-75%. ACTIVITY : Cardiant; antilipemic; antiarteriosclerotic. MECHANISM OF ACTION : HMG-CoA reductase inhibitor; cholesterol biosynthesis inhibitor.</p> |
