A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/4406 (2006.01) C07D 213/30 (2006.01) C07D 213/65 (2006.01) C07D 213/75 (2006.01)
Patent
CA 2382886
There are provided pharmaceutical formulations with improved oral absorptivity and injections that contain, as active ingredients, high concentrations of benzamide derivatives and their pharmaceutically acceptable salts, which are useful as histone deacetylase inhibitors. A pharmaceutical solution is prepared by dissolving a benzamide derivative or a pharmaceutically acceptable salt thereof in an organic solvent and/or acidic liquid, and a pharmaceutical formulation is prepared by adding a surfactant, an acidic substance and/or a polyethylene glycol. The present invention has enabled dissolution of benzamide derivatives or their pharmaceutically acceptable salts at high concentrations, to prepare practical injections and oral liquid formulations and improve absorptivity with oral administration.
La présente invention concerne des formulations pharmaceutiques à absorptivité orale améliorée et des formulations injectables qui contiennent, comme principe actif, des concentrations élevées de dérivés benzamide et de leurs sels, acceptables sur le plan pharmaceutique, qui sont utiles en tant qu'inhibiteurs d'histone déacétylase. La préparation d'une solution pharmaceutique consiste à dissoudre un dérivé benzamide, ou un de ses sels acceptable sur le plan pharmaceutique, dans un solvant organique et/ou dans un liquide acide, et une formulation pharmaceutique consiste à y ajouter un agent tensioactif, une substance acide et/ou un polyéthylène glycol. La présente invention permet la dissolution de dérivés benzamide, ou de leurs sels acceptables sur le plan pharmaceutique, à des concentrations élevées, afin de préparer des injections pratiques et des formulations liquides orales et permet d'améliorer l'absorptivité lors d'administration orale.
Ando Tomoyuki
Ishibashi Masahiko
Sakabe Masahiro
Sakai Ikuo
Suzuki Tsuneji
Bayer Schering Pharma Aktiengesellschaft
Gowling Lafleur Henderson Llp
Schering Aktiengesellschaft
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