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US 8,431,155 B1Granted
Bromocriptine formulations
AssigneeVeroScience LLC
InventorsAnthony H. Cincotta, Craig Michael Bowe, Paul Clark Stearns, Laura Jean Weston
Life of this patent
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Abstract
The present application describes pharmaceutical formulations of bromocriptine mesylate and methods of manufacturing and using such formulations. The formulations are useful for improving glycemic control in the treatment of type 2 diabetes.
Claims29
A tablet comprising micronized bromocriptine mesylate and one or more excipients;
- wherein the micronized bromocriptine mesylate is present in an amount that provides a dose of at least about 0.8 mg of bromocriptine per tablet;
- wherein the micronized bromocriptine mesylate has a Dv90 of less than about 10 μm, and wherein not more than about 20% of the bromocriptine mesylate has a particle size of less than about 1 μm;
- and wherein the tablet provides a dissolution profile, when tested in USP Apparatus Type 2 Paddle Method at 50 rpm in 500 mL of 0.1 N hydrochloric acid at about 37° C., wherein not more than about 50% of the bromocriptine mesylate has been released at about 7 minutes, not more than about 75% of the bromocriptine mesylate has been released at about 10 minutes, and at least about 90% of the bromocriptine mesylate has been released at about 30 minutes.
A method for the manufacture of a bromocriptine mesylate tablet comprising:
- processing bromocriptine mesylate to reduce the average particle size of the bromocriptine mesylate to provide bromocriptine mesylate that has a Dv90 of less than about 10 μm and wherein not more than about 20% of the bromocriptine mesylate has a particle size of less than about 1 μm after the processing;
- blending the processed bromocriptine mesylate with excipients to form a mixture wherein the bromocriptine mesylate is substantially evenly distributed in the mixture, and
- compressing the mixture to form a tablet;
- wherein the tablet comprises bromocriptine mesylate in an amount that provides a dose of at least about 0.8 mg of bromocriptine;
- and
- wherein the tablet provides a dissolution profile, when tested in USP Apparatus Type 2 Paddle Method at 50 rpm in 500 mL of 0.1 N hydrochloric acid at about 37° C., wherein at least about 90% of the bromocriptine mesylate has been released at about 30 minutes.
3 more elements
A method for the manufacture of a bromocriptine mesylate tablet comprising:
- determining that bromocriptine mesylate has a particle size distribution equivalent to a volume-based particle size distribution with a Dv90 of less than about 10 μm and wherein not more than about 20% of the bromocriptine mesylate has a particle size of less than about 1 μm;
- blending the bromocriptine mesylate of determined particle size distribution with excipients to form a mixture wherein the bromocriptine mesylate is substantially evenly distributed in the mixture, and
- compressing the mixture to form a tablet;
- wherein the tablet comprises bromocriptine mesylate in an amount that provides a dose of at least about 0.8 mg of bromocriptine;
- and
- wherein the tablet provides a dissolution profile, when tested in USP Apparatus Type 2 Paddle Method at 50 rpm in 500 mL of 0.1 N hydrochloric acid at about 37° C., wherein at least about 90% of the bromocriptine mesylate has been released at about 30 minutes.
3 more elements
A tablet comprising micronized bromocriptine mesylate and one or more excipients;
- wherein the micronized bromocriptine mesylate is present in an amount that provides a dose of at least about 0.8 mg of bromocriptine per tablet;
- wherein the micronized bromocriptine mesylate has a Dv90 of less than about 10 μm, and a volume-based particle size distribution with a span of about 2 or lower;
- and wherein the tablet provides a dissolution profile, when tested in USP Apparatus Type 2 Paddle Method at 50 rpm in 500 mL of 0.1 N hydrochloric acid at about 37° C., wherein at least about 90% of the bromocriptine mesylate has been released at about 30 minutes.
Dependencies are inferred from the claim text.