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Publication Number
US-11896562-B2
Publication Date
2024-02-13
Expiration Date
Abstract
In various embodiments, the present invention is directed to oral pharmaceutical compositions. For example, in some embodiments, the present invention is directed to taste-masked compositions. In some embodiments, the taste masked compositions comprise a highly water soluble drug such as amphetamine, e.g., in the form of a salt such as amphetamine sulfate. In various embodiments, the present invention is directed to taste-masked, orally disintegrating compositions.
Core Innovation
The invention relates to treating attention deficit-hyperactivity disorder (ADHD) by administering an orally disintegrating pharmaceutical composition that includes taste-masked drug containing particles. The taste-masked drug containing particles include drug-containing core particles comprising a therapeutically effective amount of racemic amphetamine, or a pharmaceutically acceptable salt or ester thereof, together with at least one excipient.
The taste-masking system uses two sequential taste-masking membranes disposed directly on the drug-containing core particles and on each other. A first taste-masking membrane comprises a water-insoluble polymer that excludes pharmaceutically acceptable gastrosoluble polymers, and a second taste-masking membrane comprises a water-insoluble polymer and a gastrosoluble polymer at a defined weight ratio.
The orally disintegrating pharmaceutical composition further includes a disintegrant and a sugar alcohol or saccharide, or mixtures thereof. The disclosure emphasizes reducing bitterness and aftertaste and producing an easy-to-swallow viscous suspension upon saliva contact, supported by particle size limits to avoid a gritty mouthfeel, and it is also tied to post-administration pharmacokinetic performance for a composition containing 30 mg racemic amphetamine sulfate.
Claims Coverage
The document includes one independent claim that covers an ADHD treatment method using an orally disintegrating pharmaceutical composition with a specific two-layer taste-masking membrane system, disintegrant and sugar alcohol/saccharide, and defined exposure performance for a composition containing 30 mg racemic amphetamine sulfate.
Orally disintegrating ADHD treatment with taste-masked racemic amphetamine
Treating ADHD in a subject in need thereof by administering an orally disintegrating pharmaceutical composition comprising taste-masked drug-containing particles containing a therapeutically effective amount of racemic amphetamine, or a pharmaceutically acceptable salt or ester thereof, and at least one excipient.
Two-layer first and second taste-masking membranes with defined polymer roles and ratio
Providing a first taste-masking membrane disposed directly on the drug-containing core particles, where the first taste-masking membrane comprises a water-insoluble polymer and excludes pharmaceutically acceptable gastrosoluble polymers, and providing a second taste-masking membrane disposed directly on the first taste-masking membrane, where the second taste-masking membrane comprises a water-insoluble polymer and a gastrosoluble polymer at a specified weight ratio.
Specific water-insoluble polymer selection for the taste-masking membranes
Wherein the water-insoluble polymer is each independently ethylcellulose, cellulose acetate, cellulose acetate butyrate, polyvinyl acetate, or a neutral acrylate-methacrylate copolymer.
Orally disintegrating formulation includes disintegrant and sugar alcohol/saccharide
Including a disintegrant and a sugar alcohol or saccharide, or mixture thereof, in the orally disintegrating pharmaceutical composition.
Pharmacokinetic exposure ranges for a 30 mg racemic amphetamine sulfate composition
Wherein if the orally disintegrating pharmaceutical composition comprises 30 mg of racemic amphetamine sulfate, after administration the orally disintegrating pharmaceutical composition provides one or more of AUCinf, Cmax, or Tmax ranges relative to stated reference values.
Overall, the independent claim requires an orally disintegrating composition for treating ADHD using taste-masked racemic amphetamine with two sequential taste-masking membranes, along with disintegrant and sugar alcohol/saccharide, and it further specifies pharmacokinetic exposure ranges for a 30 mg racemic amphetamine sulfate composition.
Stated Advantages
Reduced bitterness/aftertaste for taste-masked racemic amphetamine formulations.
Easy swallowing via an orally disintegrating formulation intended to disintegrate upon saliva contact.
Improved oral mouthfeel by limiting particle size to avoid gritty mouthfeel.
Specified pharmacokinetic performance for the stated 30 mg racemic amphetamine sulfate composition.
Documented Applications
Treating attention deficit-hyperactivity disorder (ADHD) in a subject in need thereof by administering the orally disintegrating pharmaceutical composition.
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