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|Title:||Controlled release and taste masking oral pharmaceutical compositions|
|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.|
|Inventor(s):||Villa; Roberto (Panama City, PA), Pedrani; Massimo (Panama City, PA), Fossati; Mauro Ajani (Panama City, PA), Fossati; Lorenzo (Panama City, PA)|
|Assignee:||Cosmo Technologies Limited (Wicklow, IE)|
1. A controlled release tablet or mini-tablet composition, consisting essentially of: a hydrophilic first matrix comprising a lipophilic phase and an amphiphilic phase,
wherein said lipophilic phase and said amphiphilic phase are in a second matrix together, and said second matrix is dispersed throughout the hydrophilic first matrix, wherein said hydrophilic first matrix consists of compounds selected from the group
consisting of acrylic or methacrylic acid polymers, acrylic copolymers, methacrylic copolymers, alkyl vinyl polymers, hydroxyalkylcellulose, carboxyalkylcellulose, polysaccharides, dextrins, pectines, starches, starch derivatives, alginic acid, natural
gums, synthetic gums, and poylyalcohols, wherein said lipophilic phase is in a granular form and consists of compounds with a melting point between 40 and 90.degree. C. and an active ingredient at least partially incorporated in said lipophilic phase,
wherein said amphiphilic phase comprises an active ingredient at least partially incorporated in said amphiphilic phase.
2. The composition according to claim 1, further comprising compounds that are polar lipids of type I or II, ceramides, glycol alkyl ethers, esters of fatty acids with polyethylene glycols or diethylene glycols.
3. The composition according to claim 1, wherein the lipophilic phase comprises one or more compounds selected from the group consisting of 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.
4. The composition according to claim 1, wherein the hydrophilic matrix consists of hydrogel-forming compounds.
5. The composition according to claim 1, further comprising a gastro-resistant coating.
6. The composition according to claim 5, wherein the gastro-resistant coating consists of methacrylic acid polymers or cellulose derivatives.
7. The composition according to claim 1, wherein said composition is in the form of tablets.
8. The composition according to claim 1, wherein said composition is in the form of minitablets.
9. The composition according to claim 1, in which the active ingredient belongs to the therapeutical classes of analgesics, antitussives, bronchodilators, antipsychotics, selective .beta. 2 antagonists, calcium antagonists, antiparkinson drugs, non-steroidal anti-inflammatory drugs, antihistamines, antidiarrheals and intestinal antiinflammatories, spasmolytics, anxiolytics, oral anti-diabetics, cathartics, antiepileptics, topical antimicrobials.
10. The composition according to claim 1, wherein the active ingredient is selected from the group consisting of mesalazine (5-aminosalicylic acid), budesonide, metformin, octylonium bromide, gabapentin, carbidopa, nimesulide, propionylilcarnitine, isosorbide mono- and dinitrate, naproxen, ibuprofen, ketoprofen, diclofenac, thiaprophenic acid, nimesulide, chlorhexidine, benzydamine, tibezonium iodide, cetylpyridinium chloride, benzalkonium chloride, and sodium fluoride.
11. The composition according to claim 1, further comprising bioadhesive substances.
12. A pharmaceutical composition, comprising the composition according to claim 1, in the form of tablets chewable or erodible in the buccal cavity or in the first portion of the gastrointestinal tract.
13. The method according to claim 1, wherein the amphiphilic matrix comprises 5 to 95% by weight of an active ingredient.