Controlled release dosage forms

Patent metadata

Field	Value
Publication number	US-9233076-B2
Application number	US-201113880841-A
Country	US
Kind code	B2
Filing date	Dec 12, 2011
Priority date	Dec 13, 2010
Publication date	Jan 12, 2016
Grant date	Jan 12, 2016

Abstract

Dosage forms having a core having a surface having means for controlling release(s) on an active agent(s); methods of manufacturing, tools used in manufacturing; and uses of the dosage forms are described.

First claim

What is claimed is:

1. A controlled release dosage form comprising:
a core comprising an active agent and having a surface with not substantially uniform topography comprising structures,
the surface of the core coated with a coating comprising a controlled release material, the coating
(i) completely covering the core and the structures, and
(ii) having weak points in a portion of the coating immediately above the structures, such that the coating ruptures at the weak points at a predetermined time after the dosage form is placed in an aqueous medium to provide passageways in the portion of the coating immediately above the structures, wherein the active agent is then released from the dosage form substantially through the passageways at a predetermined rate for about 6 or more hours,
wherein the structures are visibly discernable without the aid of any magnifying equipment and are selected from the group consisting of peaks, bumps, mounds, serrations, embossments, imprints, and combinations thereof, and
the heights, widths, and/or depths of the structures are from about 1 millimeter to about 4 millimeters.

2. The controlled release dosage form of claim 1 ,
wherein portions of the coating which are not immediately above the structures remain substantially intact and adhered to the core for about 8 to 36 hours after the dosage form is placed in the aqueous medium.

3. The dosage form of claim 1 , wherein the controlled release material comprises a hydrophobic polymer.

4. The dosage form of claim 3 , wherein the hydrophobic polymer is an acrylic polymer, an alkylcellulose or a mixture thereof.

5. The dosage form of claim 1 , wherein the coating comprises from about 1% to about 5% of the dosage form by weight.

6. The dosage form of claim 1 , wherein the coating adheres to the core until at least substantially all of the active agent is released from the dosage form through the passageways.

7. The dosage form according to claim 1 , wherein the active agent is an opioid analgesic.

8. The dosage form according to claim 1 , wherein the core comprises polyethylene oxide.

9. The dosage form of claim 8 , wherein polyethylene oxide comprises from about 67% to 96% of the dosage form by weight.

10. The dosage form of claim 1 , wherein the active agent comprises from about 4% to about 32% of the dosage form by weight.

11. The dosage form of claim 1 , wherein the core consists essentially of the active agent, polyethylene oxide and a lubricant.

12. The dosage form of claim 1 , which releases the active agent at substantially zero order release rate for about 0.5 to about 24 hours after the placement into the aqueous medium.

13. A method of controlling a rate of release of an active agent from a pharmaceutical dosage form, the dosage form comprising a substrate coated with a coating, the method comprising
altering surface morphology of the substrate before the substrate is coated with the coating by creating a surface with a not substantially uniform topography comprising structures selected from the group consisting of peaks, bumps, mounds, serrations, embossments, imprints, and combinations thereof with heights, widths, and/or depths of from about 1 millimeter to about 4 millimeters on the surface of the substrate,
coating the surface with a coating,
wherein the structures are visibly discernable without the aid of any magnifying equipment of a height, width, shape and/or size which causes a rupture and formation of passageways in a portion of the coating immediately above the structures at a predetermined time after the dosage form is placed in an aqueous medium,
and such that the active agent is released from the dosage form substantially through the passageways at a controlled rate for about 6 or more hours.

14. The method of claim 13 , wherein the substrate is cured prior to being coated with the coating.

15. The method of claim 14 , wherein the curing is at a temperature of about 46° C. to about 56° C. and for about 0.5 to 3 hours.

16. The dosage form of claim 1 , wherein the structures are peaks.

17. The method of claim 13 , wherein the structures are peaks.

18. The dosage form of claim 1 , wherein the coating has the same thickness throughout.

19. The method of claim 13 , wherein the coating has the same thickness throughout.

Assignees

• O'Donnell Edward
• Purdue Pharma Lp

Inventors

• O'Donnell Edward

Classifications

• A61K9/2072 Primary

  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 title

• A61K9/50 Primary

  Microcapsules {having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals (A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167)} · CPC title

• A61K31/485

  Morphinan derivatives, e.g. morphine, codeine · CPC title

• A61K9/2846

  Poly(meth)acrylates · CPC title

• A61K9/2866

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title