Modified-release dosage forms of 5-ht2c agonists useful for weight management
AssigneeArena Pharmaceuticals, Inc.
InventorsZezhi Jesse Shao, Anthony C. Blackburn, Andrew J. Grottick, Michael E. Morgan, Jaimie Karyn Rueter, Anna Shifrina, Scott Stirn, Libo Yang, Woo Hyun Yoon
Life of this patent
Estimating the term…
Abstract
The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.
Claims18
1-59. (canceled)
A modified-release dosage form comprising a core tablet and a water-insoluble film coating,
- wherein said core tablet comprises:
- (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride salt hemihydrate, Form III in a dose equivalent to 20 mg of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride;
- (hydroxypropyl)methyl cellulose;
- and microcrystalline cellulose,
- wherein said modified-release dosage form is a once daily dosage form, and
- wherein said modified-release dosage form provides an in vitro release rate for which the time to achieve 80% release of said (R) 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (T80%) is at least 3 hours as determined by USP Apparatus I Basket Method in 900 mL of 0.1 N HCl solution at 37° C. and 100 rpm.
A modified-release dosage form comprising a core tablet and a film coating, wherein said core tablet comprises:
- about 7% (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride salt hemihydrate, Form III in a dose equivalent to 20 mg of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride;
- about 50% (hydroxypropyl)methyl cellulose;
- and about 20% microcrystalline cellulose,
- wherein said film coating comprises ethyl cellulose and (hydroxypropyl)methyl cellulose,
- wherein the weight to weight ratio of said core tablet to said coating is about 20:1,
- wherein said modified-release dosage form is a once daily dosage form, and
- wherein said modified-release dosage form provides an in vitro release rate for which the time to achieve 80% release of said (R) 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (T80%) is at least 3 hours as determined by USP Apparatus I Basket Method in 900 mL of 0.1 N HCl solution at 37° C. and 100 rpm.
Dependencies are inferred from the claim text.