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Publication Number
US-11160772-B2
Publication Date
2021-11-02
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 comprising taste-masked drug containing particles and an orally disintegrating matrix formed by a disintegrant and a sugar alcohol or saccharide. The taste-masked drug containing particles include drug-containing core particles containing racemic amphetamine, or a pharmaceutically acceptable salt or ester thereof, and at least one excipient. The drug-containing core particles are coated with a first taste-masking membrane comprising ethylcellulose and excluding pharmaceutically acceptable gastrosoluble polymers.
The taste-masked drug containing particles further include a second taste-masking membrane disposed on the first taste-masking membrane. The second taste-masking membrane comprises ethylcellulose and an aminoalkyl methacrylate copolymer in a specific wt. ratio, and the membrane is defined by a specified thickness relative to the taste-masked drug containing particle. The composition is formulated such that, after administration at a specified dose of racemic amphetamine sulfate, pharmacokinetic exposure and timing fall within defined AUCinf, Cmax, and Tmax ranges.
The invention addresses the need for taste masking while enabling oral disintegration and appropriate in vivo performance. The overall formulation includes disintegrant and sugar alcohol/saccharide to support oral disintegration of the orally disintegrating pharmaceutical composition.
Claims Coverage
The document includes one independent claim that defines the core formulation architecture, including two sequential ethylcellulose-based taste-masking membranes on drug-containing core particles, together with a disintegrant and a sugar alcohol/saccharide, plus defined post-administration pharmacokinetic performance criteria. Dependent claims further refine the independent formulation by adding constraints on particle size, core composition, microgranule presentation, and ethylcellulose viscosity/grade for a membrane.
Two-stage ethylcellulose taste-masking on drug-containing core particles
Taste-masked drug containing particles comprising drug-containing core particles with racemic amphetamine (or a pharmaceutically acceptable salt or ester) and at least one excipient, coated with a first taste-masking membrane comprising ethylcellulose (excluding pharmaceutically acceptable gastrosoluble polymers) and a second taste-masking membrane comprising ethylcellulose and an aminoalkyl methacrylate copolymer disposed on the first taste-masking membrane.
Orally disintegrating composition components for disintegration and taste balance
The orally disintegrating pharmaceutical composition further comprises a disintegrant and a sugar alcohol or saccharide, or mixture thereof.
Dose-linked pharmacokinetic performance criteria
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: an AUCinf ranging from about 80% to about 125% of about 400-600 hr*ng/mL; a Cmax ranging from about 80% to about 125% of about 25-35 ng/mL; or a Tmax ranging from about 80% to about 125% of about 2-4 hrs.
Overall, claim coverage is focused on an orally disintegrating pharmaceutical composition built around taste-masked drug-containing particles with a defined first ethylcellulose membrane and a defined second ethylcellulose/aminoalkyl methacrylate membrane, together with a disintegrant and a sugar alcohol/saccharide. Claim-dependent limitations additionally narrow particle sizes, microgranule presentation, specific core composition using mannitol with racemic amphetamine sulfate, and an ethylcellulose viscosity value for the second membrane, while the independent claim ties the formulation to defined AUCinf, Cmax, and Tmax ranges at a 30 mg racemic amphetamine sulfate dose.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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