Sustained release pharmaceutical preparations and methods for producing the same

• US 7,125,563 B2
• Filed: 04/12/2002
• Issued: 10/24/2006
• Est. Priority Date: 04/12/2002
• Status: Expired due to Fees

• Current Assignee: DAVA Pharmaceuticals, Inc. (Endo International PLC)
• Original Assignee: DAVA Pharmaceuticals, Inc. (Endo International PLC)
• Inventors: Patel, Hiren, Pandya, Harish B., Kumbhani, Davejibhai
• Primary Examiner(s): Hartley, Michael G.
• Assistant Examiner(s): YOUNG, MICAH PAUL
• Application Number:
  US10/120,501
• Publication Number:
  US 20030198670A1
• Time in Patent Office: 1,656 Days
• Field of Search: 424464-472, 424/473, 424/486, 424/480, 424/451, 424/456, 424/474, 424/494, 424/457, 424/488
• US Class Current: 424/468
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators

Abstract

An extended release tablet comprising a core including albuterol sulfate and extended release agent; and an extended release coating on the core to provide for sustained release of the albuterol sulfate.

Claims

1. An extended release tablet comprising:

a core including albuterol sulfate and extended release agent, said extended release agent comprising an extended release agent hydrophobic polymer comprising ethyl cellulose; and

an extended release coating associated with the core to provide for sustained release of the albuterol sulfate, said extended release coating comprising a layer including extended release coating hydrophobic polymer comprising ethyl cellulose and hydrophilic polymer comprising methyl cellulose.

2. The extended release tablet according to claim 1 wherein ethanol is utilized as a solvent for preparing the core and the extended release coating.

3. The extended release tablet according to claim 1 wherein the core includes an anhydrous sulfate.

4. The extended release tablet according to claim 3 wherein the anhydrous sulfate comprises calcium sulfate.

5. The extended release tablet according to claim 1 wherein the core includes lactose monohydrate.

6. The extended release tablet according to claim 1 comprising an albuterol dissolution profile for a formulation containing 8 mg of albuterol of:

7. The extended release tablet according to claim 1 comprising an albuterol dissolution profile for a formulation containing 4 mg of albuterol of:

8. The extended release tablet according to claim 1 having bioequivalency to an albuterol sulfate osmotic device formulation.

9. An extended release tablet comprising:

a core including albuterol sulfate and extended release agent;

an extended release coating associated with the core to provide for sustained release of the albuterol sulfate, said extended release coating comprising a layer including extended release coating hydrophobic polymer and hydrophilic polymer; and

the hydrophobic polymer and the hydrophilic polymer of said extended release coating are present in a weight ratio of 55–

65;

45–

35 of said extended release coating hydrophobic polymer to said hydrophilic polymer.

10. The extended release tablet according to claim 9 wherein the extended release agent comprises an extended release agent hydrophobic polymer.

11. The extended release tablet according to claim 10 wherein the extended release agent hydrophobic polymer comprises ethyl cellulose.

12. The extended release tablet according to claim 9 wherein the extended release coating hydrophobic polymer comprises ethyl cellulose, the hydrophilic polymer comprises methyl cellulose, and the extended release agent comprises an extended release hydrophobic polymer comprising ethyl cellulose.

13. The extended release tablet according to claim 9 wherein the hydrophobic polymer and hydrophilic polymer of said extended release coating are present in a weight ratio of 57:

43 of said extended release coating hydrophobic polymer to said hydrophilic polymer.

14. The extended release tablet according to claim 9 wherein the hydrophobic polymer and hydrophilic polymer of said extended release coating comprise ethyl cellulose and methyl cellulose, respectively.

15. The extended release tablet according to claim 13 wherein the hydrophobic polymer and hydrophilic polymer of said extended release coating comprise ethyl cellulose and methyl cellulose, respectively.

16. The extended release tablet according to claim 9 wherein the extended release coating has a weight of about 5 to 25 mg.

17. The extended release tablet according to claim 16 wherein the extended release coating has a weight of about 8 to 13 mg.

18. The extended release tablet according to claim 16 wherein the extended release coating hydrophobic polymer comprises ethyl cellulose and the hydrophilic polymer comprises methyl cellulose.