Taste-masked pharmaceutical compositions
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Publication Number
US-11452689-B2
Publication Date
2022-09-27
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 an orally dispersing tablet comprising a plurality of taste-masked particles and a plurality of rapidly-dispersing microgranules. 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 with a specified ratio and membrane weight gain.
The orally dispersing tablet further includes rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol or a saccharide, or combinations thereof. The ratio of the sugar alcohol or saccharide to the disintegrant is constrained, and each of the disintegrant and the sugar alcohol or saccharide is present as particles having an average particle diameter not more than 30 µm. The ratio of rapidly-dispersing microgranules to taste-masked particles is also specified.
The tablet is defined by a dissolution performance requirement that the ODT releases greater than or equal to 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 pH 1.2 buffer. The invention also includes a method of manufacturing the ODT by preparing core particles comprising a drug, coating with the specified membrane, granulating sugar alcohol or saccharide with a disintegrant to produce rapidly-dispersing microgranules, blending the coated microparticles with the microgranules, and compressing the blend into orally disintegrating tablets.
Claims Coverage
The document provides two independent claims: an orally dispersing tablet composition and a method of manufacturing that tablet. Across the independent claims, the inventive features are driven by five features: a mixed taste-masking membrane, rapidly-dispersing microgranules with constrained particle properties, a blend ratio of microgranules to taste-masked particles, a dissolution release threshold, and the corresponding manufacturing steps.
Taste-masked particles with mixed membrane polymers and membrane loading
An orally dispersing tablet comprising taste-masked particles in which each taste-masked particle comprises a drug-containing core particle and a taste-masking membrane disposed on the drug-containing core particle, the membrane comprising a combination of a water-insoluble polymer and a gastrosoluble polymer, with a specified ratio and membrane weight gain.
Rapidly-dispersing microgranules with constrained disintegrant and sugar alcohol or saccharide properties
An orally dispersing tablet comprising rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol or a saccharide, or combinations thereof, with a specified ratio, and each of the disintegrant and the sugar alcohol or saccharide present as particles having an average particle diameter not more than 30 µm.
Blend ratio of rapidly-dispersing microgranules to taste-masked particles
An orally dispersing tablet wherein the ratio of rapidly-dispersing microgranules to taste-masked particles is specified.
Dissolution release threshold in USP Apparatus 2 (pH 1.2 buffer)
An orally dispersing tablet wherein the ODT releases greater than or equal to 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 pH 1.2 buffer.
Method of preparing coated core particles, rapidly-dispersing microgranules, blending, and compressing into ODTs
A method of manufacturing an orally dispersing tablet comprising preparing core particles comprising a drug, coating the core particles by applying a membrane comprising a mixture of water-insoluble polymer and gastrosoluble polymer with a specified ratio and membrane amount, granulating particles of a sugar alcohol or saccharide with a disintegrant to produce rapidly-dispersing microgranules, blending the membrane-coated microparticles with the rapidly-dispersing microgranules at a specified ratio, and compressing the blend into orally disintegrating tablets.
Overall, the claim coverage centers on an ODT that combines taste-masked particles having a specific mixed polymer membrane with rapidly-dispersing microgranules having constrained disintegrant and sugar alcohol or saccharide properties. The tablet and the method producing it are further constrained by a dissolution performance requirement using USP Apparatus 2 in pH 1.2 buffer to release at least 60% of the total drug within 30 minutes.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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