Compositions and methods of making rapidly dissolving ionically masked formulations
Inventors
Tengler, Mark • McMahen, Russell
Assignees
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Publication Number
US-8840924-B2
Publication Date
2014-09-23
Expiration Date
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.
Core Innovation
The invention relates to a compressed, orally disintegrating, controlled release taste-masked pharmaceutical composition. The composition includes a coated drug-ion-exchange resin complex and a directly compressible, free-flowing pharmaceutical excipient, and it effectively masks an unpalatable taste associated with delivery of the drug.
The coated drug-ion-exchange resin complex is coated with a controlled release coating. The directly compressible, free-flowing pharmaceutical excipient aids in the liberation of the coated drug-resin complex in the mouth through disintegration, while maintaining controlled release characteristics from the resin complex coating.
In described embodiments, the compositions are formed from drug-ion-exchange resin complexes combined with highly compressible, free-flowing pharmaceutical excipients, including amorphous sugars and compressible carbohydrates. The document further discusses example drug-resin complexes, including pseudoephedrine/chlorpheniramine and hyoscyamine, with polistirex/polacrilex-type resins, and reports dissolution and release behavior showing liberation of the drug components over time.
The document also elaborates that chewing may provide a thixotropic behavior in certain embodiments, while maintaining taste-masked controlled release performance. Additional discussion includes different resin, matrix, and coating types, and dosage form applicability to chewable tablet and orally disintegrating dosage forms, including tablet and suspension formats.
Claims Coverage
The independent claim covers a compressed, orally disintegrating, controlled release taste-masked pharmaceutical composition with a coated drug-ion-exchange resin complex and a directly compressible, free-flowing excipient, yielding mouth disintegration-assisted liberation while masking unpalatable taste. The dependent claims further refine the controlled release coating and define performance and physical attributes of the excipient and the compressed composition.
Compressed orally disintegrating taste-masked controlled release resin composition
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, where the composition effectively masks an unpalatable taste associated with delivery of the drug.
Controlled release coating on the drug-ion-exchange resin complex
The coated drug-ion-exchange resin complex is coated with a controlled release coating.
Disintegration-assisted liberation in the mouth
The directly compressible, free-flowing pharmaceutical excipient aids in the liberation of the coated drug-resin complex in the mouth through disintegration.
Diffusion barrier controlled release coating
The coated drug-ion-exchange resin complex controlled release coating comprises a diffusion barrier coating.
Time release diffusion barrier coating
The diffusion barrier coating is a time release coating.
Water-soluble compressible carbohydrate excipient
The directly compressible, free-flowing pharmaceutical excipient comprises a water-soluble compressible carbohydrate.
Hardness range for the compressed composition
The composition comprises a hardness of between about 5 and about 15 kPa.
Overall, the claim set centers on a compressed orally disintegrating taste-masked formulation using a coated drug-ion-exchange resin complex and a directly compressible, free-flowing excipient that promotes mouth disintegration-assisted liberation, with dependent refinements specifying diffusion barrier and time release controlled coatings, defining the excipient as a water-soluble compressible carbohydrate, and constraining hardness and mouth-feel performance.
Stated Advantages
Effectively masks an unpalatable taste associated with delivery of the drug.
Aids in liberation of the coated drug-resin complex in the mouth through disintegration.
Provides controlled release via a controlled release coating on the coated drug-ion-exchange resin complex.
Improves mouth-feel (at least about 20 percent better mouth-feel).
Documented Applications
Taste-masked orally disintegrating/chewable controlled release pharmaceutical compositions for administration with unpalatable taste masking and liberation in the mouth through disintegration.
Tablet and suspension dosage form applicability for taste-masked orally disintegrating dosage forms.
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