A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/20 (2006.01) A61K 9/16 (2006.01)
Patent
CA 2682638
The present invention relates to a method of forming granules of (2R,3S,4R,5R)-5-(4-amino-2-oxo-2 H -pyrimidin-1-yl)-2-azido-3,4-bis -iso-butyryloxy-tetrahydro-furan-2-ylmethyl isobutyrate; hydrochloride salt (I), comprising mixing I, with a granulating amount of a granulating liquid, and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer as a binder and solubility enhancer to form wet granules which are then dried to remove the granulating liquid.
La présente invention porte sur un procédé de formation de granulés du sel chlorhydrate d'isobutyrate de (2R,3S,4R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-2-azido-3,4-bis-iso-butyryloxy-tétrahydro-furane-2-ylméthyle (I), comprenant l'opération consistant à mélanger I avec une quantité de granulation d'un liquide de granulation et un copolymère à blocs polyéthylène glycol (PEG)/polypropylène glycol (PPG) comme liant et agent augmentant la solubilité, afin de former des granulés humides, lesquels sont ensuite séchés afin d'éliminer le liquide de granulation. N N O NH 3 + O OC(O)-i-Pr OC(O)-i-Pr i-Pr-C(O)O N 3 Cl (I).
Birudaraj Kondamraj
Brandl Michael Thomas
Hegde Shridhar
Sana Felix
Stefanidis Dimitrios
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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