Inclusion complexes of aryl-heterocyclic salts

Details Inclusion complexes of aryl-heterocyclic salts Inclusion complexes of aryl-heterocyclic salts

C - Chemistry, Metallurgy

08

B

C08B 37/16 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/724 (2006.01) A61K 47/48 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2251912

Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40 % w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.

On décrit des compositions d'une substance comprenant un sel d'un composé aryl-hétérocyclique, acceptable sur le plan pharmacologique, comme la ziprasidone, inséré dans une cyclodextrine. Des cyclodextrines préférées sont représentées par SBECD et HPBCD. La composition peut comporter un mélange sec, un complexe d'insertion sec ou une solution aqueuse. De préférence, le complexe d'insertion sel/cyclodextrine donne une dose de ziprasidone d'au moins 2,5 mgA par ml lorsque l'on dissout ce complexe dans de l'eau présentant une concentration en cyclodextrine de 40 % en poids du volume total de la solution. Les sels de ziprasidone que l'on préfère comprennent le mésylate, l'ésylate, le bésylate, le tartrate, le napsylate et le tosylate.

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