Anti-depressant crystalline paroxetine hydrochloride hemihydrate

• US 4,721,723 A
• Filed: 10/23/1986
• Issued: 01/26/1988
• Est. Priority Date: 10/25/1985
• Status: Expired due to Term

• Current Assignee: Beecham Group PLC (GlaxoSmithKline PLC)
• Original Assignee: Beecham Group PLC (GlaxoSmithKline PLC)
• Inventors: Richardson, John E., Lynch, Ian R., Wood-Kaczmar, Marian W., Barnes, Roger D., Buxton, Philip C., Curzons, Alan D.
• Primary Examiner(s): Schwartz, Richard A.
• Application Number:
  US06/922,530
• Time in Patent Office: 460 Days
• Field of Search: 546/197, 514/321
• US Class Current: 514/321
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/26 Psychostimulants, e.g. nicotine, cocaine
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 211/22 by oxygen atoms
• CPC Class Codes: C07D 405/12 linked by a chain containing hetero atoms as chain links

Abstract

The invention provides crystalline paroxetine hydrochloride hemihydrate, processes for its preparation, compositions containing the same and its therapeutic use as an anti-depressant.

Claims

1. Crystalline paroxetine hydrochloride hemihydrate.

2. Crystalline paroxetine hydrochloride hemihydrate in substantially pure form.

3. Crystalline paroxetine hydrochloride hemihydrate, having substantially the same X-ray diffractogram as set out in FIG. 1, substantially the same IR spectrum, in a Nujol mull, as set out in FIG. 2, and substantially the same DSC profile as set out in FIG. 3.

4. A process for the preparation of crystalline paroxetine hydrochloride hemihydrate, which process comprises forming a solution of paroxetine hydrochloride and crystallizing said hemihydrate from solution by precipitation or recrystallization.

5. An anti-depressant pharmaceutical composition comprising an effective anti-depressant amount of crystalline paroxetine hydrochloride hemihydrate and a pharmaceutically acceptable carrier.

6. A method of treatment of depression in mammals, which method comprises administering an effective amount of crystalline paroxetine hydrochloride hemihydrate.