Fmc Corporation

Bruno LeClercq

Gregory Thoorens

Thomas A Ruszkay

Peter J Riley

Brian Carlin

Miguel Angel Garcia

Thomas Ruszkay

Coprocessed compositions containing microcrystalline cellulose and calcium carbonate, wherein the weight ratio of microcrystalline cellulose to calcium carbonate is relatively high, are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained, for example, by preparing aqueous slurries or wet masses of microcrystalline cellulose and calcium carbonate and drying such slurries or wet masses to produce particulate products. The coprocessed products exhibit improved recompactibility, as compared to coprocessed products having lower microcrystalline cellulose:calcium carbonate weight ratios or as compared to physical dry blends of the two excipients.

Microcrystalline cellulose and calcium carbonate compositions useful as recompactible pharmaceutical excipients

Compositions containing calcium phosphate and microcrystalline cellulose are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. The recompactibility performance of such compositions is improved through the use of calcium phosphate having a relatively small particle size, e.g., a median particle size of not more than about 20 microns or not more than about 10 microns.

Microcrystalline cellulose and calcium phosphate compositions useful as pharmaceutical excipients

Coprocessed compositions containing calcium phosphate and microcrystalline cellulose are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained by preparing aqueous slurries of microcrystalline cellulose and calcium phosphate and drying such slurries to produce particulate products. The coprocessed products exhibit improved compactibility, as compared to dry physical blends of the same components.

A method for the preparation of microcrystalline cellulose containing tablets by roller compaction followed by tabletting is disclosed. A tablet formulation is converted to a dry granulate by roller compaction, and the dry granulate is lubricated and compacted to a tablet. The tablet formulation comprises at least one active, an microcrystalline cellulose containing material, and, optionally other pharmaceutically acceptable excipients. The microcrystalline cellulose containing material has a maximum primary compaction tensile strength of at least 9 MPa or at least 9.5 MPa and a secondary compaction tensile strength of at least 5 MPa, at least 5.5 MPa, or at least 6 MPa. A method for evaluating binders is also disclosed.

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Brussels, Belgium

Bruno LeClercq