Controlled release oral dosage form

• US 7,771,750 B2
• Filed: 03/01/2005
• Issued: 08/10/2010
• Est. Priority Date: 02/26/1999
• Status: Expired due to Fees

• Current Assignee: Andrx Pharmaceuticals LLC (Abbvie Incorporated)
• Original Assignee: Andrx Pharmaceuticals LLC (Abbvie Incorporated)
• Inventors: Chen, Chih Ming, Cheng, Xiu Xiu, Li, Boyong, Nangia, Avinash
• Primary Examiner(s): Sheikh; Humera N
• Application Number:
  US11/069,435
• Publication Number:
  US 20050147678A1
• Time in Patent Office: 1,988 Days
• Field of Search: None
• US Class Current: 424/490
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/1676 having a drug-free core with discrete complete coating layer containing drug adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61K 9/5084 Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077
• CPC Class Codes: A61P 25/34 Tobacco-abuse

Abstract

A once a day bupropion hydrochloride formulation is disclosed.

Claims

1. A pharmaceutical composition comprising:

(A) at least one pellet consisting of;

(i) a core which comprises an inert carrier, wherein said inert carrier is coated with bupropion or a pharmaceutically acceptable salt or stereoisomer thereof, and

(ii) a sustained release coating surrounding said core wherein said sustained release coating comprises at least one controlled release polymer for controlled release delivery of said bupropion or a pharmaceutically acceptable salt or stereoisomer thereof,

(B) said pharmaceutical composition further comprising bupropion or a pharmaceutically acceptable salt or stereoisomer thereof in an immediate release form, and

wherein the pharmaceutical composition is designed for once daily dosing.

2. The composition of claim 1 wherein the core further comprises at least one binder.

3. The composition of claim 2 wherein said binder comprises hydroxypropyl methylcellulose.

4. The composition of claim 1 wherein said controlled release polymer is water insoluble.

5. The composition of claim 4 wherein said water insoluble polymer comprises a methacrylic acid copolymer.

6. The composition of claim 4 wherein said water insoluble polymer comprises ethylcellulose.

7. The composition of claim 1 wherein said controlled release polymer is insoluble below about pH 7.

8. The composition of claim 1 wherein the composition is a tablet, caplet, or capsule.

9. The composition of claim 1, wherein said composition provides 24-hour efficacy with once daily dosing, with less than 50% of the bupropion released at 10 hours.

10. The composition of claim 1, wherein said composition provides therapeutic plasma levels for 12 to 24 hours.

11. The composition of claim 4 wherein said water insoluble polymer is selected from the group consisting of cellulose acylate, cellulose diacylate, cellulose triacylate, cellulose acetate, cellulose diacetate, cellulose triacetate, cellulose acetate butyrate, mono-, di- and tri-cellulose arylates.