PHARMACEUTICAL COMPOSITION COMPRISING A PROTEINASE INHIBITOR AND A MONOGLYCERIDE

1. A pharmaceutical composition, comprising (a) a therapeutically effective amount of proteinase inhibitor, pharmaceutically acceptable salts thereof or or esters (including salts thereof) (b) a pharmaceutically acceptable carrier comprising monoglycerides of (C8-C10) medium chain fatty acids, the m...

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1. Verfasser: BAILY, CAROLE, ANNE
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:1. A pharmaceutical composition, comprising (a) a therapeutically effective amount of proteinase inhibitor, pharmaceutically acceptable salts thereof or or esters (including salts thereof) (b) a pharmaceutically acceptable carrier comprising monoglycerides of (C8-C10) medium chain fatty acids, the monoglyceride is present in the amount enough for dissolving proteinase inhibitor. 2. The composition of claim 1, wherein the weight ratio of monoglyceride in (b) to the compound in (a) is at least about 1.5. 3. The composition of claim2, wherein the weight ratio of monoglyceride in (b) to the compound in (a) is at least about 3.0. 4. The composition of any claims 1 to 3, wherein the acid number of the compound (b) is less or equal to about 0,04. 5. The composition of any claims 1 to 4, wherein further comprising polyvinylpyrrolidone. 6. The composition of any claims 1 to 4, wherein the compound (a) is formula N-tert-butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3-(S)-[[N-(2-quinolylcarbonyl)-L-asparginyl]amino]butyl]-(4aS,8aS)-isoquinline-3-carboxamide. 7. The composition of claim 6, further comprising about 0.01 to about 0.5% dl .alpha.-tocopherol by weight of the composition. 8. The pharmaceutical composition of any claim 1 to 7 in the form of a unit dose of said pharmaceutical composition. В заявке описаны композиции, увеличивающие биологическую доступность ингибиторов протеиназы. Композиции содержат фармацевтически приемлемый носитель, включающий моноглицериды жирных кислот со средней длиной цепи.