Compositions and methods of making rapidly dissolving ionically masked formulations

• US 8,840,924 B2
• Filed: 03/04/2010
• Issued: 09/23/2014
• Est. Priority Date: 10/21/2005
• Status: Active Grant

• Current Assignee: NEOS Therapeutics Incorporated
• Original Assignee: NEOS Therapeutics Incorporated
• Inventors: Tengler, Mark, McMahen, Russell
• Primary Examiner(s): TRAN, SUSAN T
• Application Number:
  US12/717,251
• Publication Number:
  US 20100278901A1
• Time in Patent Office: 1,664 Days
• Field of Search: None
• US Class Current: 424/466
• 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 compressed, orally disintegrating, controlled release taste-masked pharmaceutical composition comprising:

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

wherein the composition effectively masks an unpalatable taste associated with delivery of the drug,

wherein the coated drug-ion-exchange resin complex is coated with a controlled release coating,

and wherein the directly compressible, free-flowing pharmaceutical excipient aids in the liberation of the coated drug-resin complex in the mouth through disintegration.

2. The composition of claim 1, wherein the drug in the drug-ion-exchange resin complex comprises dextromethorphan, codeine, morphine, hydrocodone, hyoscyamine, moguisteine, pseudoephedrine, chlorpheniramine, phenylprop anolamine, pharmaceutically acceptable salts of the same or combinations thereof.

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

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

5. The composition of claim 1, wherein the coated drug-ion-exchange resin complex comprises polistirex, polacrilex or combinations thereof.

6. The composition of claim 1, wherein the composition comprises pseudoephedrine polistirex and chlorpheniramine polacrilex.

7. The composition of claim 1, wherein the resin in the coated drug-ion-exchange resin complex comprises one or more cationic exchange resins.

8. The composition of claim 1, wherein the coated drug-ion-exchange resin complex comprises a divinylbenzene sulfonic acid cationic exchange resin.

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

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

11. The composition of claim 1, wherein the coated drug-ion-exchange resin complex controlled release coating comprises a diffusion barrier coating.

12. The composition of claim 11, wherein the diffusion barrier coating is a time release coating.

13. A compressed, orally disintegrating, controlled release taste-masked hyoscyamine pharmaceutical composition according to claim 1 comprising:

a coated hyoscyamine-ion-exchange resin complex; and

a directly compressible, free-flowing pharmaceutical excipient that aids in the liberation of the coated hyoscyamine-ion-exchange resin complex in the mouth through disintegration.

14. The composition of claim 13, further comprising one or more flavorants, sweeteners, coolants, dyes, or combinations and mixtures thereof.

15. The composition of claim 13, further comprising one or more excipients, one or more binders or combinations and mixtures thereof.

16. The composition of claim 1, wherein the directly compressible, free-flowing pharmaceutical excipient comprises a water-soluble compressible carbohydrate.

17. The composition of claim 1, further comprising one or more amorphous sugars.

18. The composition of claim 1, further comprising a plasticizer.

19. The composition of claim 1, wherein said controlled release coating comprises a delayed release coating.

20. The composition of claim 19, wherein the drug in said drug-ion-exchange resin complex comprises an analgesic drug, anti-inflammatory drug, central nervous system agent, anti-hypertensive drug, or an anti-hyperactive drug.

21. The composition of claim 20, wherein the drug in said drug-ion-exchange resin complex comprises an anti-hyperactive drug.

22. The composition of claim 19, wherein the drug in said drug-ion-exchange resin complex comprises amphetamine.

23. The composition of claim 1, wherein the drug in said drug-ion-exchange resin complex comprises an analgesic drug, anti-inflammatory drug, central nervous system agent, anti-hypertensive drug, or an anti-hyperactive drug.

24. The composition of claim 23, wherein the drug in said drug-ion-exchange resin complex comprises an anti-hyperactive drug.

25. The composition of claim 1, wherein the drug in said drug-ion-exchange resin complex comprises amphetamine.