Stable effervescent bisphosphonate formulations with rapid solubilization characteristics

摘要

A stable effervescent tablet, granule or powder composition free from excipients that may react with an effervescing organic acid component, comprising, an effective amount of a bisphosphonate bone resorption inhibitor, an effervescing organic acid component, an effervescing base component; wherein said composition is free of polyol binders and tableting lubricants; has a loss on drying of 0.25% (m/m) or less; has a complete disintegration time of no more than 180 seconds when placed in 3 to 8 fluid ounces of water at between 5-20° C.; and said bisphosphonate is incorporated as a micronized particle or by spray drying and is completely solubdised in water within 2 minutes without stirring.

主权项

1. A stable effervescent tableted composition, comprising:
an effective amount of micronized sodium alendronate trihydrate of size distribution about X10=2.7 μm, X50=6.2 μm, X90=13 μm, as a bisphosphonate bone resorption inhibitor, an effervescing organic acid component containing citric acid and mono sodium citrate, an effervescing base component;
wherein said tablet has been obtained using a fluidized bed granulation process; has a total weight of 3,500 mg to 6,000 mg, is free from excipients and tableting lubricants which react with said effervescing organic acid component; has a loss on drying of 0.25% (m/m) or less; has a complete disintegration time of no more than 180 seconds when placed in 3 to 8 fluid ounces of water at between 5-20° C.; and said alendronate is completely solubilised in water within 2 minutes without stirring.