Pharmaceutical formulations cytidine analogs and derivatives

A - Human Necessities – 61 – K

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A61K 31/724 (2006.01) A61K 31/7072 (2006.01)

Patent

CA 2590013

The present invention provides pharmaceutical formulations of cytidine analogs and derivatives, such as 5~-azacytidine, 5-aza-2~-deoxy-2~,2~- difluorocytidine, 5-aza-2~-deoxy-2~-fluorocytidine, 2~-deoxy- 2~,2~~difluorocytidine, and cytosine 1-~-D-arabinofuranoside, as well as methods of manufacturing the formulations. In particular, the cytidine analog or derivative is formulated with a cyclodextrin compound to stabilize and/or enhance solubility of the drug. Kits and methods for using the pharmaceutical formulations are also provided, including methods of administering the cytidine analog or derivative to treat conditions or diseases, such as cancer and hematological disorders.

La présente invention a trait à des formulations pharmaceutiques d'analogues de cytidine et dérivés, tels que 5-azacytidine, 5-aza-2'-deoxy-2',2'-difluorocytidine, 5-aza-2'-deoxy-2'-fluorocytidine, 2'-deoxy-2',2'-difluorocytidine, et cytosine 1-ß-D-arabinofuranoside, ainsi qu'à des procédés de fabrication des formulations. En particulier, l'analogue ou dérivé de cytidine est formulé avec un composé à base de cyclodextrine en vue de la stabilisation et/ou de l'amélioration de la solubilité du médicament. L'invention a également trait à des trousses et des procédés d'utilisation des formulations pharmaceutiques, comprenant des procédés d'administration de l'analogue ou dérivé de cytidine pour le traitement de conditions, telles que le cancer et des troubles hématologiques.

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