Gepirone dosage form

• US 5,478,572 A
• Filed: 09/06/1994
• Issued: 12/26/1995
• Est. Priority Date: 09/06/1994
• Status: Expired due to Term

• Current Assignee: Fabre-Kramer Pharmaceuticals Incorporated
• Original Assignee: Bristol-Myers Squibb Company
• Inventors: Chou, Joseph C. H., David, Stephen T., Gallian, Claude E.
• Primary Examiner(s): GRIFFIN, RONALD
• Application Number:
  US08/301,281
• Time in Patent Office: 476 Days
• Field of Search: 514/252, 514/256, 514/963, 514/964, 514/965, 424/468, 424/469, 424/470, 424/474, 424/480, 424/484, 424/488, 424/494
• US Class Current: 424/468
• CPC Class Codes: A61K 31/506 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/26 Psychostimulants, e.g. nicotine, cocaine

Abstract

Gepirone compositions having extended release properties contain a gepirone salt, a cellulosic polymer matrix and suitable quantities of pharmaceutical excipients. Dosage forms based thereon require 18 to 24 hours for release of 90 to 95% of gepirone.

Claims

1. A pharmaceutical composition useful for making an oral extended release gepirone dosage form comprising:

(a) from about 0.5 to about 12.0 wt % gepirone hydrochloride;

(b) from about 70 to about 85 wt % of a pharmaceutically acceptable cellulosic polymer matrix; and

(c) suitable amounts of one or more pharmaceutically acceptable excipients, wherein the release rate of gepirone from the dosage form is such that about 18 to 24 hours are required to attain from about 90 to about 95% absorption of gepirone.

2. The composition of claim 1 wherein (c) includes at least one of:

colorant, microcrystalline cellulose, colloidal silica and magnesium stearate.

3. The composition of claim 2 wherein (b) is hydroxypropylmethylcellulose having a viscosity of from about 15,000 cps to about 100,000 cps.

4. The composition of claim 3 consisting essentially of:

(a) from about 0.5 to about 11.0 wt % gepirone hydrochloride;

(b) from about 72.0 to about 83.0 wt % hydroxypropylmethylcellulose;

(c) about 01 to about 0.7% total colorant;

(d) about 10.0 to about 20.0% microcrystalline cellulose;

(e) about 0.3 to about 0.6% colloidal silica; and

(f) about 0.3 to about 1.0% magnesium stearate.

5. The composition of claim 4 containing:

(a) about 5.3 wt % gepirone hydrochloride;

(b) about 77.3 hydroxypropylmethylcellulose having a viscosity of about 100,000 cps;

(c) from about 0.1 to about 0.2% iron oxide pigments;

(d) about 16.5% microcrystalline cellulose;

(e) about 0.4% colloidal silica; and

(f) about 0.3% magnesium stearate.

6. An oral dosage form comprising the pharmaceutical composition of claim 5.

7. The composition of claim 4 containing:

(a) about 2.7 wt % gepirone hydrochloride;

(b) about 80.0% hydroxypropylmethylcellulose, having a viscosity of about 100,000 cps;

(c) from about 0.6 to about 0.9% total colorant;

(d) about 0.4% colloidal silicon; and

(f) about 0.3% magnesium stearate.

8. An oral dosage form comprising the composition of claim 7.

9. An improved method for administering gepirone comprising oral administration of a dosage form made from the composition of claim 1.

10. An improved method for administering gepirone comprising oral administration of a dosage form made from the composition of claim 5.

11. An improved method for administering gepirone comprising oral administration of a dosage form made from the composition of claim 7.

12. An oral dosage form comprising micropellets of the composition of claim 1, which micropellets are tableted or filled into capsules.

13. The dosage form of claim 12 wherein the micropellets are overcoated with a pharmaceutically acceptable coating adjuvant.

14. An oral dosage form comprising direct compressed tablets of the composition of claim 1.

15. An oral dosage form comprising directly compressed tablets of the composition of claim 5.

16. An oral dosage form comprising directly compressed tablets of the composition of claim 7.