Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
AssigneeCassiopea S.P.A.
InventorsMauro Ajani, Luigi Moro
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Abstract
The present invention refers to a new enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17α,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17α-propionate and 9,11-dehydro-cortexolone 17α-butanoate.
Claims21
A pharmaceutical composition comprising cortexolone 17α-propionate in at least one of polymorphic forms I, III, or IV, propylene glycol, cetyl alcohol, glyceryl monostearate, liquid paraffin, tocopherol, polyoxyethylene (80) sorbitan monooleate, and water, wherein:
- a) polymorphic form I is characterized by a DRX with at least peaks at about:
- 7.6, 8.4, 17.0, and 20.1 degrees 2theta;
- b) polymorphic form III is characterized by a DRX with at least peaks at about:
- 6.2, 12.6, 22.4, and 23.7 degrees 2theta;
- and
- c) polymorphic form IV is characterized by DRX with at least peaks at about:
- 4.8, 12.9, and 19.5 degrees 2theta.
Dependencies are inferred from the claim text.