Drug coating providing high drug loading and methods for providing same

• US 20050112195A1
• Filed: 09/23/2004
• Published: 05/26/2005
• Est. Priority Date: 09/26/2003
• Status: Active Grant

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Ruhlmann, Gregory, Bronz, Ryan, Fink, Tracy, Pollock, Brenda, Cruz, Evangeline, Wong, Alfredo M., Garcia, Carmelita, Li, Sherry, Edgren, David
• Granted Patent: US 8,246,986 B2
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• 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 9/2086 Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• 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: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• 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 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention is directed to aqueous drug coatings that include at least one insoluble drug, wherein the drug accounts for about 85 wt % to about 97 wt % of the drug coatings. A drug coating according to the present invention may include only one insoluble drug, two or more insoluble drugs, or one or more insoluble drugs in combination with one or more soluble drugs. The present invention also includes drug coating formulations suitable for providing drug coatings according to the present invention and dosage forms that include a drug coating according to the present invention.

Claims

1. A dosage form comprising:

a core comprising a first drug; and

a coating comprising

a second drug,

hydroxypropyl cellulose, and

a water soluble film former comprising hydroxypropyl methylcellulose, copovidone, a film-forming agent that forms a solid solution with the second drug, or blends thereof;

wherein the second drug comprises an insoluble drug present in the coating in an amount ranging from about 60 wt % to about 97 wt % based on the total weight of the coating, and the water soluble film former accounts for about 3 wt % to about 15 wt % based on the total weight of the coating.

2. The dosage form of claim 1, wherein the second drug comprises an insoluble drug, and the second drug is present in the coating in an amount ranges up to about 97 wt %, based on the total weight of the coating.

3. The dosage form of claim 1, wherein the coating further comprises a viscosity enhancer, surfactant, or a disintegrating agent.

4. The dosage form of claim 1, wherein the insoluble drug comprises a non-steroidal anti-inflammatory drug.

5. The dosage form of claim 1, wherein the insoluble drug comprises acetaminophen.

6. The dosage form of claim 1, wherein the coating further comprises a soluble drug.

7. The dosage form of claim 6, wherein the soluble drug comprises an opioid.

8. The dosage form of claim 7, wherein the opioid comprises hydrocodone.

9. The dosage form of claim 6, wherein the insoluble drug is present in the coating in an amount ranging from about 60 wt % to about 96.99 wt %, based on the total weight of the coating.

10. The dosage form of claim 1, wherein the water soluble film former comprises a blend of hydroxypropyl methylcellulose and copovidone.

11. The dosage form of claim 10, wherein the wt/wt ratio of copovidone to hydroxypropyl methylcellulose is about 1:

1.5.

12. A coating formulation that comprises

an insoluble drug;

hydroxypropyl cellulose;

a water soluble film former comprising hydroxypropyl methylcellulose, copovidone, a film-forming agent that forms a solid solution with the insoluble drug, or blends thereof; and

an aqueous solvent.

13. The coating formulation of claim 12 comprising about 80 wt % of the aqueous solvent and about 20 wt % solids content.

14. The coating formulation of claim 12, wherein the coating formulation further comprises a viscosity enhancer, surfactant, or a disintegrating agent.

15. The coating formulation of claim 12, wherein the insoluble drug comprises a non-steroidal anti-inflammatory drug.

16. The coating formulation of claim 12, wherein the insoluble drug comprises acetaminophen.

17. The coating formulation of claim 12, wherein the coating formulation further comprises a soluble drug.

18. The coating formulation of claim 17, wherein the soluble drug comprises an opioid.

19. The coating formulation of claim 18, wherein the opioid comprises hydrocodone.

20. The coating formulation of claim 12, wherein the water soluble film former comprises a blend of hydroxypropyl methylcellulose and copovidone.

21. The coating formulation of claim 12, wherein the wt/wt ratio of copovidone to hydroxypropyl methylcellulose is about 1:

1.5.