Stable effervescent bisphosphonate formulations with rapid solubilization characteristics

Abstract

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 SOLUBILIZED IN WATER WITHIN 2 MINUTES WITHOUT STIRRING. FIGURE 3