Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
Inventors
Lai, Jin-Wang • Venkatesh, Gopi M. • Qian, Ken Kangyi
Assignees
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Publication Number
US-10471017-B2
Publication Date
2019-11-12
Expiration Date
Abstract
There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more task-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 forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active), coated with a taste-masking membrane comprising a water-insoluble polymer and one or more gastrosoluble inorganic or organic pore-formers (practically insoluble in water and saliva, but soluble in an acidic buffer), exhibit acceptable taste-masking when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.
Core Innovation
The invention provides a pharmaceutical composition in the form of an orally disintegrating tablet that includes a plurality of taste-masked particles and a plurality of rapidly-dispersing microgranules. Each taste-masked particle includes a drug-containing core particle with a taste-masking membrane disposed on the core particle, and the membrane comprises a combination of a water-insoluble polymer and a gastrosoluble pore-former at a specified ratio.
The taste-masking membrane is characterized by releasing greater than or equal to about 60% of the total drug amount within 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 rapidly-dispersing microgranules have an average particle size of not more than about 400 cm and comprise a disintegrant and a sugar alcohol or saccharide, where each component is present as particles having an average particle diameter of not more than about 30 cm.
The ratio of the sugar alcohol or saccharide to the disintegrant in the rapidly-dispersing microgranules is defined from about 90/10 to about 99/1. The composition is thereby configured so that the orally disintegrating tablet combines taste-masked particles with rapidly dispersing microgranules.
Claims Coverage
The partial content includes two independent claims. One claim covers an orally disintegrating tablet composition having specific taste-masked particles and rapidly-dispersing microgranules with defined material lists, ratios, and dissolution/release performance; the other claim covers a corresponding manufacturing method including preparation, membrane coating, granulation, blending, and compression steps with defined particulate and ratio constraints.
Taste-masked particle membrane with polymer and gastrosoluble pore-former ratio and dissolution release threshold
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 pore-former at a ratio ranging from about 85/15 to about 65/35, with specified selections for the polymer and pore-former, and the 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 pH 1.2 buffer.
Rapidly-dispersing microgranules with defined particle size, component forms, and ratio
The pharmaceutical composition comprises a plurality of rapidly-dispersing microgranules having an average particle size of not more than about 400 cm 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 cm, and wherein the ratio of said sugar alcohol, said saccharide or combination thereof to said disintegrant in the rapidly-dispersing microgranules is from about 90/10 to about 99/1; wherein the pharmaceutical composition is an orally disintegrating tablet.
Membrane coating, microgranule granulation, blending, and compression into orally disintegrating tablets
A method of manufacturing a pharmaceutical composition comprising preparing core particles comprising a drug; coating the core particles with a membrane comprising a mixture of water-insoluble polymer and a gastrosoluble pore former at a ratio of from about 85/15 to about 65/35 with specified selections; granulating particles of a sugar alcohol or a saccharide, or a combination thereof, each particle having an average particle diameter of not more than 30 cm, with a disintegrant having an average particle diameter of not more than 30 cm to produce rapidly-dispersing microgranules with an average particle size of not more than about 400 cm, wherein the ratio of sugar alcohol/saccharide to disintegrant is from about 90/10 to about 99/1; blending the membrane coated particles with the rapidly-dispersing microgranules at a ratio of about 1/6 to about 1/2; and compressing the blend into orally disintegrating tablets.
Overall claim coverage centers on (i) a taste-masking membrane made from a water-insoluble polymer plus a gastrosoluble pore-former at a specified ratio together with a defined pH 1.2 dissolution release threshold using USP Apparatus 2, and (ii) rapidly-dispersing microgranules formed from a disintegrant and a sugar alcohol/saccharide with defined particle-size and component ratios, in an orally disintegrating tablet format; the manufacturing claim further specifies the preparation, coating, granulation, blending, and compression sequence using the same defined particulate and ratio constraints.
Stated Advantages
Releases greater than or equal to about 60% of the total amount of drug in 30 minutes in pH 1.2 buffer when tested using United States Pharmacopoeia Apparatus 2 using paddles at 50 rpm in 900 mL.
Documented Applications
No documented applications found
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