Controlled release and taste masking oral pharmaceutical composition

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.

1. A controlled release and taste-masking oral pharmaceutical composition comprising:
 budesonide as an active ingredient incorporated into a matrix structure consisting essentially of: 
 a) a lipophilic matrix consisting of lipophilic compounds with a melting point between 40° C. and 90° C. in which the active ingredient is at least partially inglobated; 
 b) an amphiphilic matrix; 
 c) an outer hydrophilic matrix consisting of hydrogels in which the lipophilic matrix and the amphiphilic matrix are dispersed; and 
 a gastro-resistant coating wherein the active ingredient is dispersed both in the hydrophilic matrix and in the lipophilic/amphiphilic matrix, and the composition is in the form of tablets, capsules or minitablets. 
 
     
     
       2. The composition according to  claim 1 , wherein the active ingredient is mixed and at least partially inglobated in the amphiphilic matrix. 
     
     
       3. The composition according to  claim 1 , wherein the active ingredient is mixed and at least partially inglobated in the lipophilic matrix. 
     
     
       4. The composition according to  claim 1 , wherein the lipophilic matrix consists of C6-C20 alcohols or C8-C20 fatty acids or esters of fatty acids with glycerol or sorbitol or other polyalcohols with carbon atom chain not higher than six. 
     
     
       5. The composition according to  claim 1 , wherein the amphiphilic matrix consists amphiphilic compounds selected from the group consisting of polar lipids of type I or II, ceramides, glycol alkyl ethers, esters of fatty acids with polyethylene glycols, and diethylene glycols. 
     
     
       6. The composition according to  claim 1 , wherein the lipophilic matrix consists of a compound selected from unsaturated or hydrogenated alcohols or fatty acids, salts, esters or amides thereof, mono-, di- or triglycerides of fatty acids, the polyethoxylated derivatives thereof, waxes, and cholesterol derivatives. 
     
     
       7. The composition according to  claim 1 , wherein the hydrophilic matrix consists of compounds selected from acrylic or methacrylic acid polymers or copolymers, alkylvinyl polymers, hydroxyalkylcellulose, carboxyalkylcellulose, polysaccharides, dextrins, pectins, starches and derivatives, alginic acid, natural or synthetic gums, polyalcohols. 
     
     
       8. The composition according to  claim 1 , wherein the gastro-resistant coating consists of acrylic and methacrylic acid polymers or copolymer or cellulose derivatives. 
     
     
       9. The composition according to  claim 1 , further comprising bioadhesive substances. 
     
     
       10. The composition according to  claim 1 , wherein the composition is in tablet form, and said tablet form is chewable or erodible in the buccal cavity or in the first portion of the gastrointestinal tract. 
     
     
       11. A method for the treatment a subject suffering from Inflammatory Bowel Disease and Irritable Bowel Syndrome, comprising administering an effective amount of the pharmaceutical composition according to  claim 1  to a subject in need of such a treatment.