Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
First Claim
1. A pharmaceutical composition comprising:
- (1) a plurality of taste-masked particles, wherein each taste-masked particle comprises;
(a) a drug-containing core particle;
(b) a taste-masking membrane disposed on said drug-containing core particle comprising a combination of (i) a water-insoluble polymer and (ii) a gastrosoluble inorganic or organic pore-former at a ratio ranging from about 85/15 to about 65/35, wherein the water-insoluble polymer is selected from the group consisting of ethyl cellulose, polyvinyl acetate, cellulose acetate, cellulose acetate phthalate, cellulose acetate butyrate, methacrylate copolymers and combinations thereof, and the gastrosoluble organic or inorganic pore-former is selected from the group consisting of calcium carbonate, calcium phosphate, calcium saccharide, calcium succinate, calcium tartrate, ferric acetate, ferric hydroxide, ferric phosphate, magnesium carbonate, magnesium citrate, magnesium hydroxide, magnesium oxide, magnesium phosphate and mixtures thereof, 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; and
(2) a plurality of rapidly-dispersing microgranules having an average particle size of not more than about 400 μ
m comprising (i) a disintegrant and (ii) 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 μ
m, 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.
5 Assignments
0 Petitions
Accused Products
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.
-
Citations
26 Claims
-
1. A pharmaceutical composition comprising:
-
(1) a plurality of taste-masked particles, wherein each taste-masked particle comprises; (a) a drug-containing core particle; (b) a taste-masking membrane disposed on said drug-containing core particle comprising a combination of (i) a water-insoluble polymer and (ii) a gastrosoluble inorganic or organic pore-former at a ratio ranging from about 85/15 to about 65/35, wherein the water-insoluble polymer is selected from the group consisting of ethyl cellulose, polyvinyl acetate, cellulose acetate, cellulose acetate phthalate, cellulose acetate butyrate, methacrylate copolymers and combinations thereof, and the gastrosoluble organic or inorganic pore-former is selected from the group consisting of calcium carbonate, calcium phosphate, calcium saccharide, calcium succinate, calcium tartrate, ferric acetate, ferric hydroxide, ferric phosphate, magnesium carbonate, magnesium citrate, magnesium hydroxide, magnesium oxide, magnesium phosphate and mixtures thereof, 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; and (2) a plurality of rapidly-dispersing microgranules having an average particle size of not more than about 400 μ
m comprising (i) a disintegrant and (ii) 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 μ
m, 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
-
-
19. A method of manufacturing a pharmaceutical composition comprising:
-
(a) preparing core particles comprising a drug; (b) coating the core particles by applying a membrane comprising a mixture of (i) water-insoluble polymer and (ii) a gastrosoluble organic or inorganic pore former present at a ratio of from about 85/15 to about 65/35 wherein the water-insoluble polymer is selected from the group consisting of ethyl cellulose, polyvinyl acetate, cellulose acetate, cellulose acetate phthalate, cellulose acetate butyrate, methacrylate copolymers and combinations thereof, and the gastrosoluble organic or inorganic pore-former is selected from the group consisting of calcium carbonate, calcium phosphate, calcium saccharide, calcium succinate, calcium tartrate, ferric acetate, ferric hydroxide, ferric phosphate, magnesium carbonate, magnesium citrate, magnesium hydroxide, magnesium oxide, magnesium phosphate and mixtures thereof; (c) granulating particles of a sugar alcohol or a saccharide, or a combination thereof, each particle of sugar alcohol or saccharide having an average particle diameter of not more than 30 μ
m, with a disintegrant having an average particle diameter of not more than 30 μ
m to produce rapidly-dispersing microgranules with an average particle size of not more than about 400 μ
m, 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;(d) blending the membrane coated particles of step (b) with the rapidly-dispersing microgranules of step (c) at a ratio of about 1/6 to about 1/2; and (e) compressing the blend of step (d) into orally disintegrating tablets. - View Dependent Claims (20, 21, 22, 23, 24, 25, 26)
-
Specification