High ibuprofen content granules and their preparation and their use in pharmaceutical dosage forms
AssigneeSi Group, Inc.
InventorsPatrick C. Hu, Gregory H. Lambeth, Arcelio J. Malcolm
Life of this patent
Estimating the term…
Abstract
Described are granules composed at least of a substantial amount of ibuprofen, at least one pharmaceutically-acceptable super disintegrant, and at least one pharmaceutically-acceptable binder different from the super disintegrant(s), the super disintegrant(s) being substantially uniformly dispersed throughout the granules. The methods for preparing such granules are described. The granules are useful in forming solid dosage forms such as filled capsules or compressed solid dosage forms.
Claims23
Pharmaceutical granules consisting of (i) 75 wt % or more of ibuprofen, (ii) in the range of about 0.5 to about 10 wt % of sodium starch glycolate, (iii) in the range of about 2 to about 14.5 wt % of at least one pharmaceutically-acceptable binder, which binder is different from sodium starch glycolate, (iv) in the range of about 0.01 to about 2.0 wt % of at least one pharmaceutically-acceptable wetting agent, and optionally (v) in the range of about 0.01 to about 0.5 wt % of at least one pharmaceutically-acceptable glidant, and (vi) a moisture content that is less than 5 wt %, wherein sodium starch glycolate is substantially uniformly dispersed in the granules, wherein said granules are devoid of non-crosslinked polyvinylpyrrolidone, wherein said wetting agent remains on the outer surface of said granules, wherein the foregoing percentages of (i), (ii), (iii), (iv), and (v) are based on the dry weight of said granules, and the weight of (vi) is based on the weight of the granules, and wherein said granules are formed by spraying an aqueous solution, dispersion, or suspension of (iii), followed by spraying an aqueous solution, dispersion, or suspension of (iv), onto a fluidized mixture of (i) and (ii).
A pharmaceutical dosage form comprised of
- A) capsules at least partially filled with pharmaceutical granules which granules have been dried to a moisture content that is less than 5 wt % and having a glidant physically mixed therewith, or
- B) compressed solid dosage forms produced using pharmaceutical granules which granules have been dried to a moisture content that is less than 5 wt % and having a glidant physically mixed therewith;
- said pharmaceutical granules consisting of (i) 75 wt % or more of ibuprofen, (ii) in the range of about 0.5 to about 10 wt % of sodium starch glycolate and (iii) in the range of about 2 to about 14.5 wt % of at least one pharmaceutically-acceptable binder, which binder is different from sodium starch glycolate, (iv) in the range of about 0.01 to about 2.0 wt % of at least one pharmaceutically-acceptable wetting agent, and optionally (v) in the range of about 0.01 to about 0.5 wt % of at least one pharmaceutically-acceptable glidant, and (vi) a moisture content that is less than 5 wt %, wherein sodium starch glycolate is substantially uniformly dispersed in said granules, wherein said granules are devoid of non-crosslinked polyvinylpyrrolidone, wherein said wetting agent remains on the outer surface of said granules, and wherein the foregoing percentages of (i), (ii), (iii), (iv), and (v) are based on the dry weight of said granules, and the weight of (vi) is based on the weight of the granules, and wherein said granules are formed by spraying an aqueous solution, dispersion, or suspension of (iii), followed by spraying an aqueous solution, dispersion, or suspension of (iv), onto a fluidized mixture of (i) and (ii).
Dependencies are inferred from the claim text.