Taste-masked pharmaceutical compositions
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Publication Number
US-10130580-B2
Publication Date
2018-11-20
Expiration Date
Abstract
There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity in about 60 seconds forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active) applied with a taste-masking membrane comprising a combination of water-insoluble and gastrosoluble polymers release not less than about 60% of the dose is in the stomach in about 30 minutes, thus maximizing the probability of achieving bioequivalence to the reference IR product having rapid onset of action (short Tmax). A process for preparing such compositions for oral administration using conventional fluid-bed equipment and rotary tablet press is also disclosed.
Core Innovation
The invention relates to a pharmaceutical composition that is an orally disintegrating tablet including taste-masked particles. Each taste-masked particle comprises a drug-containing core particle and a taste-masking membrane disposed on the drug-containing core particle, and the membrane comprises a combination of a water-insoluble polymer and a gastrosoluble polymer, wherein the water-insoluble polymer is ethylcellulose and the gastrosoluble polymer is an aminoalkyl methacrylate copolymer.
In the taste-masking membrane, the weight ratio of the water-insoluble polymer to the gastrosoluble polymer is about 50/50, and the taste-masking membrane thickness ranges from about 10% to 30% by weight of the coated particle. The composition also includes rapidly-dispersing microgranules having an average particle size of not more than about 400 μm, wherein each of the disintegrant and the sugar alcohol or saccharide is present as particles having an average particle diameter of not more than about 30 μm.
The composition is defined by dissolution and oral performance criteria, including release of greater than or equal to about 60% of the total amount of drug in 30 minutes in 0.1 N HCl at pH 1.2 when tested using United States Pharmacopoeia Apparatus 2. The invention addresses taste-masking while providing rapid drug release in stomach-relevant acidic conditions.
The orally disintegrating tablet forms a smooth, easy-to-swallow suspension in the buccal cavity with minimal/no aftertaste, and the document describes limited drug release in simulated saliva and rapid release in acidic medium. Comparative cases are described to show that insoluble polymer alone does not achieve the same taste-masking versus rapid release balance.
Claims Coverage
Independent claim clm-00001 defines an orally disintegrating tablet that combines taste-masked particles with rapidly-dispersing microgranules and requires specific dissolution performance and particle-size constraints; no other independent claims are explicitly provided in the partial content.
Taste-masked particles with ethylcellulose and gastrosoluble aminoalkyl methacrylate copolymer membrane
A plurality of taste-masked particles wherein each taste-masked particle comprises a drug-containing core particle and a taste-masking membrane disposed on said drug-containing core particle comprising a combination of a water-insoluble polymer and a gastrosoluble polymer, wherein the water-insoluble polymer is ethylcellulose and the gastrosoluble polymer is an aminoalkyl methacrylate copolymer.
Membrane ratio and thickness for the taste-masking membrane
The weight ratio of the water-insoluble polymer to the gastrosoluble polymer in the taste-masking membrane is about 50/50, and the taste-masking membrane thickness ranges from about 10% to 30% by weight of the coated particle.
Dissolution requirement in 0.1 N HCl at pH 1.2
The pharmaceutical composition releases greater than or equal to about 60% of the total amount of drug in 30 minutes when tested for dissolution using United States Pharmacopoeia Apparatus 2 using paddles at 50 rpm in 900 mL of 0.1 N HCl at pH 1.2.
Rapidly-dispersing microgranules with disintegrant plus sugar alcohol or saccharide
A plurality of rapidly-dispersing microgranules having an average particle size of not more than about 400 μm comprising a disintegrant and a sugar alcohol or a saccharide or a combination thereof, wherein each of said disintegrant and sugar alcohol or saccharide is present in the form of particles having an average particle diameter of not more than about 30 μm.
Orally disintegrating tablet form
The pharmaceutical composition is an orally disintegrating tablet.
The claim coverage centers on an orally disintegrating tablet combining taste-masked drug-containing core particles coated with an ethylcellulose/aminoalkyl methacrylate copolymer membrane (about 50/50 by weight; 10% to 30% membrane thickness by weight of coated particle) with rapidly-dispersing microgranules containing a disintegrant and a sugar alcohol or saccharide with constrained particle sizes. The formulation is additionally required to meet a dissolution threshold in 0.1 N HCl (pH 1.2) using USP Apparatus 2 with specified paddle conditions.
Stated Advantages
Provides limited drug release in simulated saliva while enabling rapid release in acidic stomach-relevant medium.
Produces an orally disintegrating tablet that disintegrates in the buccal cavity to form a smooth, easy-to-swallow suspension with minimal/no aftertaste.
Achieves the required dissolution level of greater than or equal to about 60% of total drug in 30 minutes in 0.1 N HCl at pH 1.2.
Documented Applications
Orally disintegrating tablets for taste-masked drug administration, intended to disintegrate in the oral cavity and release drug in stomach-relevant acidic conditions.
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