Controlled release and taste masking oral pharmaceutical composition
AssigneeCosmo Technologies Limited
InventorsRoberto Villa, Massimo Pedrani, Mauro Ajani, Lorenzo Fossati
Life of this patent
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Abstract
Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.
Claims30
A tablet for the treatment of ulcerative colitis consisting essentially of (1) a tableted core, and (2) a coating on said tableted core, wherein said tableted core consists of a dispersion of ingredients, said ingredients comprising:
- (a) 9 mg of budesonide;
- (b) hydroxypropyl methylcellulose;
- and
- (c) magnesium stearate;
- wherein said coating on said tableted core comprises methacrylic acid copolymer type A and methacrylic acid copolymer type B in a weight to weight ratio of from 1:5 to 5:1;
- wherein following oral administration of the tablet to a human, the tablet provides an AUC of said budesonide in said human of about 16.43±10.52 (ng)×(h)/mL;
- and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.
A tablet consisting essentially of (1) a tableted core, and (2) a gastro-resistant coating on said tableted core, wherein said tableted core consists of a dispersion of ingredients, said ingredients comprising:
- (a) 9 mg of budesonide;
- (b) hydroxypropyl methylcellulose;
- (c) magnesium stearate;
- (d) hydroxypropyl cellulose;
- (e) silicon dioxide;
- (f) lactose;
- (g) starch or starch derivative;
- (h) microcrystalline cellulose;
- and
- (i) lecithin;
- wherein said gastro-resistant coating comprises methacrylic acid copolymer type A, methacrylic acid copolymer type B and triethylcitrate, wherein said methacrylic acid copolymer type A and said methacrylic acid copolymer type B are present in said gastro-resistant coating in a weight to weight ratio of from 1:5 to 5:1;
- wherein following oral administration of the tablet to a human, the tablet provides an AUC of said budesonide in said human of about 16.43±10.52 (ng)×(h)/mL;
- and
- wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.
A tablet consisting essentially of (1) a tableted core, and (2) a gastro-resistant coating on said tableted core, wherein said tableted core consists of a dispersion of ingredients, said ingredients comprising:
- (a) 9 mg of budesonide;
- (b) hydroxypropyl cellulose;
- and
- (c) magnesium stearate;
- wherein said gastro-resistant coating comprises methacrylic acid copolymer type A, methacrylic acid copolymer type B and triethylcitrate, wherein said methacrylic acid copolymer type A and said methacrylic acid copolymer type B are present in said gastro-resistant coating in a weight to weight ratio of from 1:5 to 5:1;
- wherein following oral administration of the tablet to a human, the tablet provides an AUC of said budesonide in said human of about 16.43±10.52 (ng)×(h)/mL, a Cmax of said budesonide in said human of about 1.35±0.96 ng/mL, and a Tmax of said budesonide in said human of about 13.3±5.9 hour;
- and
- wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.
Dependencies are inferred from the claim text.