Modified-release dosage forms of 5-HT2C agonists useful for weight management

Patent metadata

Field	Value
Publication number	US-10226471-B2
Application number	US-201715429221-A
Country	US
Kind code	B2
Filing date	Feb 10, 2017
Priority date	Sep 1, 2010
Publication date	Mar 12, 2019
Grant date	Mar 12, 2019

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.

First claim

What is claimed is:

1. A modified-release dosage form which is a tablet for once-daily dosing, wherein the dosage form comprises a core tablet and a functional film coating,
wherein said core tablet comprises:
(i) about 7% by weight of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride salt hemihydrate, Form III, and
(ii) about 50% by weight of (hydroxypropyl)methyl cellulose;

wherein said functional film coating comprises ethyl cellulose and (hydroxypropyl)methyl cellulose in a weight ratio of about 85:15; 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.

2. The modified-release dosage form of claim 1 , wherein the weight to weight ratio of said core tablet to said functional coating is about 20:1.

3. The modified-release dosage form of claim 1 or 2 , wherein the core tablet further comprises microcrystalline cellulose.

4. The modified-release dosage form of claim 3 , wherein the core tablet comprises about 20% by weight of microcrystalline cellulose.

5. The modified-release dosage form of claim 1 or 2 , which exhibits a release profile comprising super-case II kinetics under in vitro conditions.

6. The modified-release dosage form according to claim 1 or 2 , wherein the core tablet further comprises mannitol.

7. The modified-release dosage form according to claim 1 or 2 , wherein the core tablet further comprises magnesium stearate.

Assignees

• Arena Pharm Inc

Inventors

• Shao Zezhi Jesse
• Blackburn Anthony C
• Grottick Andrew J
• Morgan Michael E
• Rueter Jaimie Karyn
• Shifrina Anna
• Stirn Scott
• Yang Libo
• Yoon Woo Hyun

Classifications

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61K31/55 Primary

  having seven-membered rings, e.g. azelastine, pentylenetetrazole · CPC title

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title

• C07C233/54

  having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton · CPC title

• A23P20/12

  Apparatus or processes for applying powders or particles to foodstuffs, e.g. for breading; Such apparatus combined with means for pre-moistening or battering · CPC title