ORAL DOSAGE FORM FOR CONTROLLED DRUG RELEASE

• US 20110135695A1
• Filed: 12/13/2010
• Published: 06/09/2011
• Est. Priority Date: 02/12/2002
• Status: Active Grant

• Current Assignee: Glaxo Group Limited (GSK plc)
• Original Assignee: Glaxo Group Limited (GSK plc)
• Inventors: Re, Vincenzo, Willy, Helen Anne, Martini, Luigi, Li, Chi Leung
• Granted Patent: US 9,144,547 B2
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/22 for herpes viruses

Abstract

An oral dosage form comprising,

• (i) an erodable core, which core comprises a pharmaceutically active weak base or a pharmaceutically acceptable salt or solvate thereof; and
• (ii) an erodable coating surrounding said core, which coating comprises one or more openings extending substantially completely through said coating but not penetrating said core and communicating from the environment of use to said core;
  characterised in that release of the pharmaceutically active weak base or a pharmaceutically acceptable salt or solvate thereof from the dosage form occurs through the said opening(s) by the erosion of said erodable core and through erosion of said erodable coating under pre-determined pH conditions; a process for preparing such a dosage form and the use of such a dosage form in medicine.

Claims

1. An oral dosage form comprising:

(i) an erodable core, which core comprises a pharmaceutically active weak base or a pharmaceutically acceptable salt or solvate thereof; and

(ii) an erodable coating around said core, which coating comprises one or more openings about 10 to 70% of the total face area of the dosage form extending substantially completely through said coating but not penetrating said core and communicating from the environment of use to said core;

wherein release of the pharmaceutically active weak base or a pharmaceutically acceptable salt or solvate thereof from the dosage form occurs through the one or more openings by the erosion of said erodable core and through erosion of said erodable coating at pH>

4.5.

2. The oral dosage form according to claim 1, wherein the erodable coating is selected from a polymethacrylate polymer, coprocessed polyvinylacetate phthalate, cellulose acetate trimellitate, cellulose acetate phthalate, shellac, a hydroxyropyl-methylcellulose phthalate polymer and their copolymers, and blends thereof.

3. The oral dosage form according to claim 1, wherein the erodable coating has a thickness in the range 0.05 to 0.5 mm.

4. The oral dosage form according to claim 1, wherein the size of each of the one or more openings is in the range 0.5 mm to 8 mm.

5. The oral dosage form according to claim 1, wherein the erodable coating comprises two openings.

6. The oral dosage form according to claim 1, wherein the erodable core is in a multi-layered form.

7. The oral dosage form according to claim 1, wherein the core is predominantly comprised of hydroxypropylmethyl cellulose and lactose.

8. The oral dosage form according to claim 1, wherein the pharmaceutically acceptable weak base is selected from bupropion, ondansetron, paroxetine, valaciclovir, and 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, or a pharmaceutically acceptable salt or solvate thereof.

9. An oral dosage form according to claim 1, in which the pharmaceutically acceptable weak base is 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione or a pharmaceutically acceptable salt or solvate thereof.

10. A process for the preparation of an oral dosage form according to claim 1, which process comprises:

(a) preparing an erodable tablet core;

(b) coating the core with a material with pH-dependent erodability; and

(c) creating one or more openings in the coating, wherein said one or more openings extend substantially completely through said coating but not penetrating said core and communicating from the environment of use to said core.