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Publication Number
US-10441554-B2
Publication Date
2019-10-15
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 an orally disintegrating pharmaceutical composition that includes taste-masked drug-containing particles containing racemic amphetamine, or a pharmaceutically acceptable salt or ester thereof. The composition is designed to form an orally dispersing, non-gritty viscous suspension in saliva and to reduce bitterness and aftertaste.
Taste masking is achieved by a two-stage membrane system on the drug-containing core particles. A first taste-masking membrane comprises ethylcellulose and excludes pharmaceutically acceptable gastrosoluble polymers, and a second taste-masking membrane comprises ethylcellulose and aminoalkyl methacrylate copolymer at a 50/50 weight ratio, where the second membrane is disposed on the first membrane.
The composition further includes a disintegrant and a sugar alcohol or saccharide, where the drug-containing particles are combined with rapidly dispersing microgranules. The membrane system remains intact in the mouth but dissolves under gastric conditions to enable release comparable to EVEKEO®, with performance framed using pharmacokinetic acceptance windows for AUCinf, Cmax, and Tmax relative to target values.
Claims Coverage
The independent claim covers a defined orally disintegrating pharmaceutical composition with a specific two-layer ethylcellulose-based taste-masking membrane on racemic amphetamine core particles, along with defined formulation components and pharmacokinetic acceptance ranges tied to a 30 mg racemic amphetamine sulfate dose-equivalent.
Two-stage ethylcellulose taste-masking membranes
A first taste-masking membrane comprising ethylcellulose excluding pharmaceutically acceptable gastrosoluble polymers, and a second taste-masking membrane comprising ethylcellulose and aminoalkyl methacrylate copolymer at a 50/50 weight ratio, disposed on the first membrane.
Racemic amphetamine drug-containing core particles with excipient
Drug-containing core particles comprising a therapeutically effective amount of racemic amphetamine, or a pharmaceutically acceptable salt or ester thereof, and at least one excipient.
Orally disintegrating composition including disintegrant and sugar alcohol or saccharide
The orally disintegrating pharmaceutical composition comprises a disintegrant and a sugar alcohol or saccharide, or mixture thereof.
Pharmacokinetic acceptance windows tied to 30 mg dose-equivalent
Wherein if the orally disintegrating pharmaceutical composition comprises 30 mg of racemic amphetamine sulfate, after administration the composition provides one or more of AUCinf ranging from about 80% to about 125% of about 400-600 hr*ng/mL, Cmax ranging from about 80% to about 125% of about 25-35 ng/mL, or Tmax ranging from about 80% to about 125% of about 2-4 hrs.
Overall, the claim coverage is directed to a taste-masked orally disintegrating composition using a two-layer ethylcellulose membrane system on racemic amphetamine core particles, formulated with a disintegrant and sugar alcohol or saccharide, and meeting specified pharmacokinetic exposure windows for a 30 mg racemic amphetamine sulfate-equivalent dose.
Stated Advantages
Rapid disintegration in saliva to form a smooth, non-gritty viscous suspension with minimal aftertaste.
Reduced bitterness and aftertaste.
Enables release comparable to EVEKEO®.
Provides specified AUCinf, Cmax, and/or Tmax within defined acceptance windows.
Documented Applications
An orally disintegrating pharmaceutical composition for racemic amphetamine sulfate intended to provide rapid oral disintegration and taste-masked delivery with pharmacokinetic performance comparable to a reference listed drug (EVEKEO®).
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