Osmotic delivery system

• US 20030161882A1
• Filed: 01/27/2003
• Published: 08/28/2003
• Est. Priority Date: 02/01/2002
• Status: Abandoned Application

• Current Assignee: Kenneth C. Waterman
• Original Assignee: Kenneth C. Waterman
• Inventors: Waterman, Kenneth C.
• Application Number:
  US10/352,258
• Publication Number:
  US 20030161882A1
• Time in Patent Office: Days
• US Class Current: 424/468
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Abstract

An osmotic pharmaceutical tablet is described which comprises a single-layer compressed core surrounded by a water permeable layer having a passageway. The single-layer core contains (i) a non-ripening drug having a solubility per dose less than about 1 mL⁻¹, (ii) about 2.0% to about 30% by weight of a polyethyleneoxide having a weight-average, molecular weight from about 200,000 to about 7,000,000, (iii) an osmagent, and (iv) an optional disintegrant.

Claims

1. An osmotic pharmaceutical tablet comprising

(a) a single-layer compressed core comprising

(i) a non-ripening drug having a solubility per dose less than about 1 mL⁻

1,

(ii) a polyethyleneoxide having a weight-average, molecular weight from about 200,000 to about 7,000,000, and

(iii) an osmagent, wherein said polyethyleneoxide is present in said core from about 2.0% to about 35% by weight and said osmagent is present from about 15% to about 70% by weight;

(b) a water-permeable layer surrounding said core; and

(c) at least one passageway within said layer (b) for delivering said drug to a fluid environment surrounding said tablet.

2. The osmotic tablet of claim 1 wherein said non-ripening drug is non-crystalline.

3. The osmotic tablet of claim 1 wherein said non-ripening drug is crystalline.

4. The osmotic tablet of claim 1 wherein said non-ripening drug is a drug particle comprising a crystalline or non-crystalline drug and an excipient.

5. The osmotic tablet of claim 1 wherein said non-ripening drug is [2-(3,4-dichlorophenoxy)-5-fluorobenzyl]-methylamine hydrochloride.

6. The osmotic tablet of claim 5 wherein said core further comprises tartaric acid.

7. The osmotic tablet of claim 1 wherein said non-ripening drug is sildenafil citrate.

8. The osmotic tablet of claim 7 wherein said osmagent is ascorbic acid.

9. The osmotic tablet of claim 1 wherein said non-ripening drug is sertraline hydrochloride.

10. The osmotic tablet of claim 1 wherein said non-ripening drug is ziprasidone hydrochloride.

11. The osmotic tablet of claim 1 wherein said polyethyleneoxide is present in said core from about 3% to about 20% by weight.

12. The osmotic tablet of claim 1 wherein said polyethyleneoxide is present in said core from about 3% to about 15% by weight.

13. The osmotic tablet of claims 1 wherein said polyethyleneoxide is present in said core from about 3% to about 10% by weight.

14. The osmotic tablet of any one of the preceding claims wherein said osmagent is present in said core from about 30% to about 65% by weight.

15. The osmotic tablet of claim 1 wherein said osmagent is present in said core from about 35% to about 55% by weight.

16. The osmotic tablet of claim 1 wherein said osmagent is present in said core from about 40% to about 50% by weight.

17. The osmotic tablet of claim 1 wherein the combination of said non-ripening drug and said osmagent have an average ductility from about 100 to about 200 Mpa.

18. The osmotic tablet of claim 1 wherein the combination of said non-ripening drug and said osmagent have an average tensile strength from about 0.8 to about 2.0 Mpa.

19. The osmotic tablet of claim 1 wherein the combination of said non-ripening drug and said osmagent have an average brittle fracture index less than about 0.2.

20. The osmotic tablet of any one of the preceding claims wherein said single-layer core further comprises a disintegrant.

21. The osmotic tablet of claim 20 wherein said disintegrant is non-swelling, non-gelling, disintegrant.

22. An osmotic pharmaceutical tablet comprising

(a) a single-layer compressed core consisting essentially of

(i) a non-ripening drug having a solubility per dose less than about 1 mL⁻

1,

(ii) a polyethyleneoxide having a weight-average, molecular weight from about 200,000 to about 7,000,000,

(iii) an osmagent,

(iv) an optional bioavailability enhancing additive, and

(v) an optional pharmaceutically acceptable excipient, carrier or diluent, wherein said polyethyleneoxide is present in said core from about 2.0% to about 35% by weight and said osmagent is present from about 15% to about 70% by weight;

(b) a water-permeable layer surrounding said core; and

(c) at least one passageway within said layer (b) for delivering said drug to a fluid environment surrounding said tablet.