Melt-coated pharmaceutical composition with fast release
Inventors
Kraahs, Peter • Bold, Stefanie • Fahsel, Lars
Assignees
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Publication Number
US-8481060-B2
Publication Date
2013-07-09
Expiration Date
Abstract
The present invention relates to a process for producing a solid, coated pharmaceutical composition by a melt coating process. The process is adapted to provide a solid, coated pharmaceutical composition by melt coating, which has a fast release.
Core Innovation
The invention relates to a process for producing a solid, coated fast-release pharmaceutical composition in which a core containing one or more pharmaceutically active ingredients is spray-coated with a coating composition that includes a taste-masking compound. The taste-masking compound has a melting point of at least 40°C and an HLB value of 10 or less, and is heated to at least 40°C so that the taste-masking compound is in melt phase during coating.
A release compound is provided to act in the gastrointestinal tract to either cause disruption or disintegration of the taste-masking layer or to improve the permeability of the taste-masking layer for the pharmaceutically active ingredients. The process spray-coats the core with the coating composition containing the melt-phase taste-masking compound and with the release compound to yield a solid, coated fast-release pharmaceutical composition.
The dissolution profile is measured according to the European Pharmacopoeia in a USP type 2 paddle apparatus under specified aqueous buffer conditions with an acidic phase at pH=1 and then under conditions at which the active ingredients are soluble. The composition is defined so that after 45 minutes at least 60% of the one or more active ingredients is dissolved.
The taste-masking compound is present in the at least one coating composition in an amount in the range of 70% to 95%, based on the weight of the coating composition, while the release compound is present in the at least one coating composition or in a separate coating composition in an amount in the range of 5% to 30%, based on the weight of the respective coating composition.
Claims Coverage
One independent claim is present. The claim includes four inventive features: melt-phase taste-masking spray coating, GI disruption or permeability improvement using a release compound, a defined dissolution-performance test and threshold, and compositional ranges for the taste-masking and release compounds.
Melt-phase taste-masking spray coating for fast release
Providing a core containing one or more pharmaceutically active ingredients; providing at least one coating composition comprising at least one taste-masking compound having a melting point of at least 40°C and an HLB value of 10 or less, heated to at least 40°C so the taste-masking compound is in melt phase; and spray-coating the core with the coating composition to yield a solid, coated fast-release pharmaceutical composition.
GI disruption or permeability improvement using a release compound
Providing at least one release compound that, in the gastrointestinal tract, causes disruption or disintegration of the taste-masking layer or improves the permeability of the taste-masking layer for the one or more pharmaceutically active ingredients; and spray-coating the core with the release compound together with the taste-masking coating composition.
USP type 2 dissolution performance definition for fast release
Producing a solid, coated fast-release pharmaceutical composition having a dissolution profile measured according to the European Pharmacopoeia in a USP type 2 paddle apparatus under acidic conditions at pH=1 and then under conditions at which the active ingredients are soluble, wherein after 45 minutes at least 60% of the one or more active ingredients is dissolved.
Compositional ranges for taste-masking and release compound
Having the taste-masking compound in the coating composition in an amount of 70% to 95% based on the weight of the coating composition, and having the release compound in the coating composition or in a separate coating composition in an amount of 5% to 30% based on the weight of the respective coating composition.
The claim coverage is directed to melt-phase spray-coating using a taste-masking compound with melting point and HLB limits, combined with a release compound that acts in the gastrointestinal tract to disrupt or disintegrate the taste-masking layer or improve permeability, while meeting a defined European Pharmacopoeia/USP type 2 dissolution profile and specified composition ranges.
Stated Advantages
Improved dissolution for the melt-coated taste-masking formulations that include the release compound, as shown by faster dissolution in examples with versus without the release compound.
Documented Applications
Production of solid, coated fast-release oral dosage forms for pharmaceutically active ingredients where taste-masking is provided and dissolution is improved under gastrointestinal conditions as measured by USP type 2 paddle testing.
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