Terazosin capsules

• US 6,110,493 A
• Filed: 05/18/1999
• Issued: 08/29/2000
• Est. Priority Date: 08/01/1996
• Status: Expired due to Term

• Current Assignee: Novartis Corporation (Novartis Ag)
• Original Assignee: Novartis Corporation (Novartis Ag)
• Inventors: Pelloni, Christopher L., Guentensberger, Jeffrey W.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Benston, Jr., William E.
• Application Number:
  US09/313,613
• Time in Patent Office: 469 Days
• Field of Search: 424/451, 424/489, 424/490, 424/456, 514/254, 544/291
• US Class Current: 424/451
• CPC Class Codes: A61K 31/506 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 31/517 ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds

Abstract

A capsule dosage form containing solid form of terazosin in a solid carrier is disclosed. The capsule dosage form is stable under accelerated stability conditions and therapeutically equivalent to known liquid-filled terazosin capsules.

Claims

1. A pharmaceutical solid-filled capsule dosage form containing a fill which consists of a pharmaceutically effective amount of anhydrous terazosin hydrochloride, and a solid carrier, which solid-filled capsule dosage form is therapeutically equivalent to a reference liquid-filled terazosin hydrochloride capsule which is the subject of FDA-approved New Drug Application N20347 comprising an equivalent amount of terazosin and a non-aqueous liquid carrier, and which solid-filled capsule dosage form has an average dissolution at 30 minutes measured according to U.S.P. Method II at 50 r.p.m. in water of at least 85 percent of the label amount with no individual capsule below 80 percent of the label amount after being maintained in a high density polyethylene bottle closed with a screw cap at about 40°

C. and 85 percent relative humidity for twelve weeks.

2. A capsule dosage form of claim 1 wherein the average dissolution at 30 minutes is at least 90 percent of the label amount with no individual capsule below 80 percent of the label amount.

3. A capsule dosage form of claim 1 wherein the average dissolution at 30 minutes is at least 95 percent of an initial average dissolution.

4. A dosage form of claim 1 wherein the solid carrier comprises (a) from 70 to 100 percent by weight of a diluent;

(b) from 0 to 20 percent by weight of a disintegrant; and

(c) 0 to 10 percent by weight of a lubricant.

5. A dosage form of claim 4 wherein the solid carrier comprises (a) from 85 to 97 percent by weight of a diluent;

(b) from 1 to 10 percent by weight of a disintegrant; and

(c) 0.2 to 5 percent by weight of a lubricant.

6. A dosage form of claim 4 wherein the solid carrier comprises (a) from 90 to 97 percent by weight of a diluent;

(b) from 1 to 5 percent by weight of a disintegrant; and

(c) 0.5 to 2 percent by weight of a lubricant.

7. A dosage form of claim 4 wherein the diluent is a monosaccharide, a disaccharide or a polysaccharide.

8. A capsule dosage form of claim 5 wherein the average dissolution at 30 minutes is at least 90 percent of the label amount with no individual capsule below 80 percent of the label amount.

9. A capsule dosage form of claim 6 wherein the average dissolution at 30 minutes is at least 95 percent of an initial average dissolution.

10. A capsule dosage form according to claim 1 which is a hard gelatin capsule.

11. A capsule dosage form of claim 10 wherein the solid carrier comprises microcrystalline cellulose.

12. A capsule dosage form of claim 11 wherein the average dissolution at 30 minutes is at least 90 percent of an initial average dissolution.

13. A capsule dosage form of claim 12 wherein the average dissolution at 30 minutes is at least 95 percent of an initial average dissolution.