Taste-masked pharmaceutical compositions
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Publication Number
US-10568832-B2
Publication Date
2020-02-25
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 includes 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 core particle, and the membrane comprises a combination of a water-insoluble polymer and a gastrosoluble polymer in a defined ratio.
The rapidly-dispersing microgranules comprise a disintegrant and a sugar alcohol or a saccharide, with both components provided as particles having an average particle diameter of not more than about 30 μm. The composition is formulated such that the taste-masked particles provide taste masking while the rapidly-dispersing microgranules promote rapid dispersion, with stated performance targets including saliva residence disintegration and rapid gastric release.
A manufacturing method is also provided in which drug core particles are prepared and coated with the taste-masking membrane having the defined water-insoluble and gastrosoluble polymer combination and ratio. Sugar alcohol and/or saccharide particles are granulated with a disintegrant to produce rapidly-dispersing microgranules having a defined average particle size, and the coated microparticles are blended with the microgranules and compressed into orally disintegrating tablets.
Claims Coverage
The partial content identifies two independent claims: a pharmaceutical composition claim with defined taste-masked particles and rapidly-dispersing microgranules, and a manufacturing method claim for producing an orally disintegrating tablet. The inventive features center on the specific taste-masking membrane polymer combination and ratio, the microgranule structure using a disintegrant plus a sugar alcohol or saccharide with defined particle size limits, and the blending and compression into orally disintegrating tablets.
Taste-masking membrane with defined water-insoluble and gastrosoluble polymer ratio
The taste-masking membrane disposed on a drug-containing core particle comprises a combination of a water-insoluble polymer selected from ethylcellulose, polyvinyl acetate, cellulose acetate, cellulose acetate phthalate, cellulose acetate butyrate, methacrylate copolymers and combinations thereof, and a gastrosoluble polymer selected from maltodextrin, aminoalkyl methacrylate copolymer, polyvinylacetate diethylaminoacetate, and combinations thereof, wherein the ratio of the water-insoluble polymer to the gastrosoluble polymer is from about 95/5 to about 50/50.
Rapidly-dispersing microgranules with disintegrant and sugar alcohol or saccharide
Rapidly-dispersing microgranules have an average particle size of not more than about 400 μm and comprise a disintegrant and a sugar alcohol or a saccharide or a combination thereof, wherein each of the disintegrant and the sugar alcohol or saccharide is present in the form of particles having an average particle diameter of not more than about 30 μm.
Blending coated microparticles with microgranules and compressing into orally disintegrating tablets
Taste-masking membrane coated microparticles are blended with the rapidly dispersing microgranules at a ratio of about 1/6 to about 1/2, and the blend is compressed into orally disintegrating tablets.
Overall, the claims coverage is centered on taste-masked particles formed by coating drug-containing core particles with a membrane made from a specified water-insoluble polymer plus a specified gastrosoluble polymer in a defined ratio, together with rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol or saccharide with defined particle size constraints. The method claim uses the same membrane and microgranule constructs, blends them at a defined ratio, and compresses them into orally disintegrating tablets.
Stated Advantages
Smooth easy-to-swallow suspension with no gritty/chalky aftertaste.
Low taste-masking release in simulated saliva, with a stated taste-masking criterion of not more than about 10% release in about 3 minutes.
Rapid gastric release, with a stated gastric release criterion of at least about 60% release in about 30 minutes.
Saliva residence disintegration in about 60 seconds.
Bioequivalence to reference immediate release.
Friability of not more than about 1%, optionally not more than about 0.5%.
Documented Applications
Orally disintegrating tablets comprising taste-masked, drug-containing core microparticles and rapidly-dispersing microgranules.
Use of the composition for performance behavior including saliva disintegration and rapid gastric release, as measured using simulated saliva and acidic buffers under USP dissolution testing conditions.
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