Sustained-release formulations of colchicine and methods of using same
First Claim
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1. A sustained release formulation of colchicine, comprising:
- (a) granules comprising colchicine or a pharmaceutically acceptable salt thereof in an amount of not more than 0.6 mg, and a binder comprising hydroxypropyl methylcellulose (HPMC) 6 mPa·
s in an amount of 1% to 30% (w/w) of the formulation;
(b) a release retarding agent admixed with, or blended with, the granules in an amount of between about 25% and about 30% w/w of the formulation, wherein the retarding agent comprises a combination of equal parts hydroxypropyl methylcellulose (HPMC) with a viscosity grade of 4000 mPa*s and lactose monohydrate; and
(c) at least one additional pharmaceutically acceptable excipient admixed with or blended with the granules, wherein the at least one additional pharmaceutically acceptable excipient is starch, gelatin, polyvinylpyrrolidone (PVP), polyvinyl alcohol, microcrystalline cellulose, hydroxypropyl cellulose (HPC) or a mixture thereof,wherein the sustained release formulation is in a form of a tablet, andwherein the formulation is homogeneous.
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Abstract
Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided.
20 Citations
14 Claims
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1. A sustained release formulation of colchicine, comprising:
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(a) granules comprising colchicine or a pharmaceutically acceptable salt thereof in an amount of not more than 0.6 mg, and a binder comprising hydroxypropyl methylcellulose (HPMC) 6 mPa·
s in an amount of 1% to 30% (w/w) of the formulation;(b) a release retarding agent admixed with, or blended with, the granules in an amount of between about 25% and about 30% w/w of the formulation, wherein the retarding agent comprises a combination of equal parts hydroxypropyl methylcellulose (HPMC) with a viscosity grade of 4000 mPa*s and lactose monohydrate; and (c) at least one additional pharmaceutically acceptable excipient admixed with or blended with the granules, wherein the at least one additional pharmaceutically acceptable excipient is starch, gelatin, polyvinylpyrrolidone (PVP), polyvinyl alcohol, microcrystalline cellulose, hydroxypropyl cellulose (HPC) or a mixture thereof, wherein the sustained release formulation is in a form of a tablet, and wherein the formulation is homogeneous. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9)
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10. A sustained release formulation of colchicine, comprising:
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(a) granules comprising colchicine or a pharmaceutically acceptable salt thereof in an amount of not more than 0.6 mg, and a binder comprising hydroxypropyl methylcellulose (HPMC) 6 mPa·
s in an amount of 1% to 30% (w/w) of the formulation;(b) a release retarding agent admixed with, or blended with, the granules in an amount of between about 25% and about 30% w/w of the formulation, wherein the retarding agent comprises a combination of equal parts hydroxypropyl methylcellulose (HPMC) with a viscosity grade of 4000 mPa*s and lactose monohydrate; and
(c) at least one additional pharmaceutically acceptable excipient admixed with or blended with the granules, wherein the at least one additional pharmaceutically acceptable excipient is starch, gelatin, polyvinylpyrrolidone (PVP), polyvinyl alcohol, microcrystalline cellulose, hydroxypropyl cellulose (HPC) or a mixture thereof,wherein the granules additionally comprise a first filling agent comprising lactose monohydrate in an amount of 10% to 80% (w/w) of the formulation, wherein a second filling agent is admixed or blended with the granules, which comprises lactose monohydrate in an amount of 10% to 30% (w/w) of the formulation, wherein the sustained release formulation is in a form of a tablet, and wherein the formulation is homogeneous. - View Dependent Claims (11, 12, 13, 14)
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Specification