C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 71/00 (2006.01) A61K 31/58 (2006.01)
Patent
CA 2362669
A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
L'invention concerne une nouvelle forme cristalline (forme H) de l'~pl~r~none, m~dicament antagoniste du r~cepteur de l'aldost~rone, qui possde une vitesse relativement rapide de dissolution dans des milieux aqueux. L'invention concerne ~galement des nouvelles formes cristallines solvat~es d'~pl~r~none, lesquelles, lorsqu'elles sont d~solvat~es, peuvent produire l'~pl~r~none de forme H; elle concerne aussi une ~pl~r~none amorphe, des compositions pharmaceutiques comprenant l'~pl~r~none de forme H ~ventuellement accompagn~e d'au moins une forme ~ l'~tat solide d'~pl~r~none, selon un dosage unitaire total d'~pl~r~none compris environ entre 10 et 100 mg, ainsi qu'un ou plusieurs excipients, acceptables sur le plan pharmacologique. L'invention concerne encore des proc~d~s de pr~paration de l'~pl~r~none de forme H et des compositions comprenant cette ~pl~r~none de forme H, ainsi qu'une m~thode de prophylaxie et/ou de traitement d'un ~tat ou d'une pathologie, induit par l'aldost~rone, cette m~thode consistant ~ administrer ~ un sujet une dose efficace sur le plan th~rapeutique d'~pl~r~none, dans laquelle au moins une fraction de l'~pl~r~none pr~sente est une ~pl~r~none de forme H.
Barton Kathleen P.
Borchardt Thomas B.
Carlos Marlon V.
Desai Subhash
Ferro Leonard J.
Pharmacia Corporation
Sim & Mcburney
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