Solubilization of weak bases

Details Solubilization of weak bases Solubilization of weak bases

A - Human Necessities

61

K

A61K 31/415 (2006.01) A61K 9/00 (2006.01) A61K 31/4184 (2006.01) A61K 31/437 (2006.01) A61K 47/12 (2006.01)

Patent

CA 2478470

A pharmaceutical composition for administration to mammals comprising: a weak base compound having a compound pKa below about 7; an acidic buffer with a buffer pKa below 7; and optional pharmaceutically acceptable additives, wherein the composition has a pH below about 4 is provided. Preferred pharmaceutically active compounds are imidazole derivatives, pyridine derivatives, and aniline derivatives. The pharmaceutical compositions have greater water solubility than the weak base.

L'invention porte sur une composition pharmaceutique destinée à être administrée à des mammifères et comprenant: un composé à base faible ayant un pKa inférieur à environ 7; un tampon acide ayant un pKa inférieur à 7. L'invention porte également sur des additifs éventuels acceptables d'un point de vue pharmaceutique. La composition a un pH inférieur à environ 4. Les composés préférés actifs d'un point de vue pharmaceutique sont des dérivés d'imidazole, des dérivés de pyridine et des dérivés d'aniline. Les compositions pharmaceutiques de l'invention ont une plus grande solubilité dans l'eau que la base faible.

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