COMPOSITIONS AND METHODS OF MAKING RAPIDLY DISSOLVING IONICALLY MASKED FORMULATIONS

• US 20100278901A1
• Filed: 03/04/2010
• Published: 11/04/2010
• Est. Priority Date: 10/21/2005
• Status: Active Grant

• Current Assignee: NEOS Therapeutics Incorporated
• Original Assignee: NEOS Therapeutics Incorporated
• Inventors: McMahen, Russell Lee, TENGLER, Mark
• Granted Patent: US 8,840,924 B2
• Time in Patent Office: Days
• US Class Current: 424/441
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/4402 only substituted in position 2, e.g. pheniramine, bisacodyl
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 31/74 Synthetic polymeric materials
• CPC Class Codes: A61K 31/785 Polymers containing nitrogen
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/58 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
• CPC Class Codes: A61K 47/585 Ion exchange resins, e.g. polystyrene sulfonic acid resin
• CPC Class Codes: A61K 47/59 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
• CPC Class Codes: A61K 9/0002 Galenical forms characterised by the drug release technique; Application systems commanded by energy
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 21/02 Muscle relaxants, e.g. for tetanus or cramps
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system

Abstract

The present invention includes compositions and methods for reduce the taste of the drug in the drug resin complex. The composition may include one or more drug-resin complexes and a highly compressible, free-flowing pharmaceutical excipient. The resin is present in an amount effective to reduce the taste of the drug in the drug resin complex relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient causes release of the drug-resin complex in the mouth.

Claims

1. A taste-masked pharmaceutical composition suitable for oral consumption comprising:

a drug-resin complex and a directly compressible, free-flowing pharmaceutical excipient,

wherein the resin is present in an amount effective to reduce the taste of the drug in the drug resin complex by more than about 15 percent relative to an otherwise identical pharmaceutical composition without the resin;

wherein the directly compressible, free-flowing pharmaceutical excipient aids release of the drug-resin complex in the mouth, and

wherein the composition comprises a chewable tablet, a solid, a dissolvable or disintegrating tablet, a tab, a capsule, a powder, a gum, a lozenge and combinations thereof.

3. The composition of claim 1, wherein the drug in the drug-resin complex comprises dextromethorphan, codeine, morphine, hydrocodone, hyoscyamine, moguisteine, pseudoephedrine, chlorpheniramine, phenylpropanolamine, pharmaceutically acceptable salts of the same and combinations thereof.

5. The composition of claim 1, further comprising one or more flavorants, sweeteners, coolants, dyes, or combinations and mixtures thereof.

6. The composition of claim 1, further comprising one or more excipients, one or more binders or combinations and mixtures thereof.

7. The pharmaceutical of claim 1, wherein the drug-resin complex comprises polistirex, polacrilex and combinations thereof.

8. The pharmaceutical of claim 1, wherein the drug-resin complex comprises pseudoephedrine polistirex and chlorpheniramine polacrilex.

9. The pharmaceutical of claim 1, wherein the resin in the drug-resin complex comprises one or more cationic exchange resins.

10. The pharmaceutical of claim 1, wherein the drug-resin complex comprises a divinylbenzene sulfonic acid cationic exchange resin.

11. The pharmaceutical of claim 1, wherein the composition comprises a hardness of between about 5 and about 15 kPa.

12. The pharmaceutical of claim 1, wherein the composition has at least about 20 percent better mouth-feel.

13. The pharmaceutical of claim 1, wherein the drug-resin complex comprises a diffusion barrier coating.

14. The pharmaceutical of claim 13, wherein the diffusion barrier coating is a time release coating.

23. A taste-masked chewable pseudoephedrine and chlorpheniramine pharmaceutical composition according to claim 1 comprising:

a pseudoephedrine-resin complex;

a chlorpheniramine-resin complex;

one or more amorphous sugars; and

a compressible, free-flowing, pharmaceutical, taste-masking excipient, wherein the highly compressible, free-flowing pharmaceutical excipient aids release of the drug-resin complex in the mouth.

24. The pharmaceutical of claim 23, wherein the pseudoephedrine-resin complex, chlorpheniramine-resin complex or both comprise a polistirex resin, a polacrilex resin and combinations thereof.

25. A rapidly dissolving, taste-masked hyoscyamine pharmaceutical composition according to claim 1 comprising:

a hyoscyamine -resin complex, whereby the hyoscyamine is released when the composition disintegrates; and

one or more amorphous sugars; and

a compressible, free-flowing, pharmaceutical, taste-masking excipient.

26. The composition of claim 25, further comprising one or more flavorants, sweeteners, coolants, dyes, or combinations and mixtures thereof.

27. The composition of claim 25, further comprising one or more excipients, one or more binders or combinations and mixtures thereof.

28. A taste-masked chewable pseudoephedrine and chlorpheniramine pharmaceutical composition according to claim 1 comprising:

a pseudoephedrine-resin complex;

a chlorpheniramine-resin complex;

one or more amorphous sugars; and

a compressible, free-flowing, pharmaceutical, taste-masking excipient, whereby the pseudoephedrine and the chlorpheniramine are slowly released when the composition is chewed, the composition becoming thixotropic when chewed but not fully dissociating for at least 10 seconds when chewed, and the composition slowly dissociates when the composition is chewed, so as to fully dissociate after the mixture is swallowed.

2. (canceled)

4. (canceled)

15. A rapidly dissolving or disintegrating, taste-masked pharmaceutical composition comprising:

a drug-resin complex and a directly compressible, free-flowing, pharmaceutical, taste-masking excipient, wherein the resin is present in an amount effective to reduce the taste of the drug in the drug resin complex relative to an otherwise identical pharmaceutical composition without the resin; and

wherein the directly compressible, free-flowing pharmaceutical excipient causes release of the drug-resin complex in the mouth.

16. The pharmaceutical of claim 15, wherein the drug-resin complex comprises polistirex, polacrilex and combinations thereof.

17. The pharmaceutical of claim 15, wherein the drug-resin complex comprises pseudoephedrine polistirex and chlorpheniramine polacrilex.

18. A chewable tablet comprising:

a pharmaceutically active drug-resin complex, whereby the pharmaceutically active ingredient is slowly released when the tablet is chewed, the tablet becoming thixotropic when chewed but not fully dissociating for at least 30 seconds when chewed, and the tablet slowly dissociates when the tablet is chewed, so as to completely dissociate thereafter once swallowed; and

one or more amorphous sugars.

19. The pharmaceutical of claim 18, wherein the pharmaceutically active drug-resin complex comprises polistirex, polacrilex and combinations thereof.

20. The pharmaceutical of claim 18, wherein the pharmaceutically active drug-resin complex comprises pseudoephedrine polistirex and chlorpheniramine polacrilex.

21. The composition of claim 18, further comprising one or more flavorants, sweeteners, coolants, dyes, or combinations and mixtures thereof.

22. The composition of claim 18, further comprising one or more excipients, one or more binders or combinations and mixtures thereof.