Hot melt granulation formulations of poorly water-soluble active agents
AssigneeMylan Laboratories Limited
InventorsChaoju Xiao, Boyong Li
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Abstract
The presently disclosed subject matter is directed to a granule, wherein the granule has an active agent and a wax dispersed therein, and the granule exhibits excellent friability when compressed to form a pharmaceutical composition. The subject matter disclosed herein is also directed to methods of preparing the granules and the pharmaceutical compositions comprising the granules. The compositions and methods disclosed provide granules and pharmaceutical compositions for immediate release of the active agent and do not substantially prolong the release of the active agent from the granule.
Claims30
A pharmaceutical composition, comprising:
- a granule, said granule comprising an active agent and a wax material, wherein said active agent has a water solubility of less than 1 mg/ml and said wax material is present in an amount below about 8% (w/w) of said granule.
-21. (canceled)
A tablet comprising compressed granules, wherein said granules comprise below about 8% (w/w) wax material and an active agent having water solubility of less than 1 mg/ml, wherein said tablet has a friability of about 1%.
-39. (canceled)
A tablet comprising:
- i. from about 30% to about 70% (w/w) active agent;
- ii. from about 2% to about 8% (w/w) wax material;
- and
- iii. from about 22% to about 68% pharmaceutically acceptable excipients;
- wherein said excipients comprise at least one of:
- fillers present in an amount of from about 40% to about 50% (w/w);
- disintegrants present in an amount of about 4% to about 10% (w/w);
- lubricants present in an amount of from about 0.1 to about 1% (w/w) and/or glidants present in an amount of about 0.1% to about 0.5% (w/w);
- wherein said tablet is prepared by hot melt granulation performed using a high sheer mixer.
A tablet comprising:
- i. about 52% disulfiram;
- ii. about 4% stearic acid;
- iii. about 18% microcrystalline cellulose;
- iv. about 18% lactose anhydrous;
- v. about 5% sodium starch glycolate;
- vi. about 0.5% magnesium stearate;
- and
- vii. about 0.25% colloidal silicon dioxide;
- wherein said tablet is prepared by hot melt granulation.
Dependencies are inferred from the claim text.