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Details for Patent: 8,460,706

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Details for Patent: 8,460,706

Title:Hydrophilic/lipophilic polymeric matrix dosage formulation
Abstract: An oral dosage form comprising a pharmaceutical tablet of one or more layers, one of which carries a biologically active substance; the formulation of said tablet includes different percentages of hydrophilic and lipophilic polymeric materials, and adjuvant substances. The tablets of the present invention show a release rate which is independent from the amounts of active substance present in the tablet.
Inventor(s): Vergnault; Guy (Kembs, FR), Grenier; Pascal (Kappelen, FR), Maggi; Lauretta (Pavia, IT), Conte; Ubaldo (Busto Arsizio, IT)
Assignee: Jagotec AG (Muttenz, CH)
Filing Date:Feb 07, 2011
Application Number:13/022,281
Claims:1. A controlled-release tablet comprising an amount of an active substance, inclusive of pharmaceutically acceptable salts, which tablet exhibits a release rate over approximately 24 hours in vitro as measured using equipment 2, paddle (USP XXIII), working at 100 rpm and utilizing 900 ml of an aqueous dissolution fluid at 37.degree. C., wherein the release rate of the active substance as a percentage is independent of the amount of active substance in said tablet, the tablet comprising an active layer containing: (i) an active substance, (ii) hydrophilic polymeric substances which swell and/or gel and/or erode upon contact with aqueous liquids, (iii) lipophilic substances, and (iv) adjuvant substances, wherein the weight ratio of the hydrophilic polymeric substances to the lipophilic substances contained in said active layer is in the range of 10:1 to 0.5:1; and wherein the active substance is not ropinirole or a pharmaceutically acceptable salt thereof.

2. The tablet of claim 1, in which the weight ratio of the hydrophilic polymeric substances to the lipophilic substances contained in said active layer is in the range of 7:1 to 1:1.

3. The tablet of claim 1, in which said hydrophilic polymeric substances (ii) are contained in a percentage between 1% and 75% of the active layer.

4. The tablet of claim 1, in which said lipophilic substances (iii) are contained in a percentage between 1% and 70% of said active layer.

5. The tablet of claim 1, in which said adjuvants (iv) are contained in a percentage between 5% to 50% of the weight of said active layer.

6. The tablet of claim 1, in which the weight ratio between said active substance (i) and said adjuvant substances (iv) in the active layer is in the range of 0.001:1 to 4:1.

7. The tablet of claim 1, in which one or more barrier layers are applied to one or both surfaces (bases) of the active layer, said one or more barrier layers containing one or more of hydrophilic polymeric substances which swell and/or gel and/or erode upon contact with aqueous liquids, lipophilic substances, and adjuvant substances.

8. The tablet of claim 7, in which the weight ratio of hydrophilic swelling and/or gelling and/or erodible polymeric substances to lipophilic substances contained in the one or more barrier layers is in the range of 1:1 to 7.5:1.

9. The tablet of claim 1, in which the active substance (i) is contained in a weight percentage between 0.01% to 70%.

10. The tablet of claim 9, in which the active substance (i) is contained in a percentage of 0.05% to 20% by weight of the active layer.

11. The tablet of claim 1, in which the active layer contains polymeric material with slow swelling and/or gelification and/or erosion and/or solubility properties.

12. The tablet of claim 1, in which the active layer further contains polymeric substances of a lipophilic nature.

13. The tablet of claim 1 or 7, in which said hydrophilic polymeric substances comprise a pharmaceutically acceptable biocompatible and/or biodegradable material selected from the group consisting of non-cross-linked polyvinylpyrrolidone, hydroxypropylcellulose with a molecular weight of 100,000 to 4,000,000, sodium carboxymethylcellulose, carboxymethylstarch, potassium methacrylate divinylbenzene copolymer, hydroxypropylmethylcellulose of molecular weight between 2,000 and 4,000,000, a polyethyleneglycol of molecular weight between 200 and 15,000, a polyoxyethylene with molecular weight of up to 20,000,000, a carboxyvinylpolymer, a poloxamer (polyoxyethylene-polyoxypropylene copolymer), a polyvinylalcohol, a glucane(glucan), a carrageenan, a scleroglucane (scleroglucan), a mannan, a galactomarman, gellans, xanthans, alginic acid, polyaminoacids, methyl vinyl ether/malefic anhydride copolymer, carboxymethylcellulose, ethylcellulose, methylcellulose, starch, and alpha, beta, or gamma cyclodextrin.

14. The tablet of claim 1, in which said lipophilic substances include a natural fat.

15. The tablet of claim 1, in which the active substance(s) are therapeutic agents for the treatment of chronic diseases drugs acting on the cardiovascular system, antiarrhythmics, cardiac stimulants, vasodilators, anti-hypertensives, anti-adrenergic substances of central and peripheral action or substances acting on the arteriolar musculature, substances acting on the 25 renin-angiotensin system, anti-hypertensives and diuretics in association, anti-Parkinson's Disease agents, diuretics and drugs for the treatment of Alzheimer's disease.

16. The tablet of claim 1, in which the active substance(s) is selected from the group consisting of propranolol, atenolol, pindolol, prazosin, ramipril, spirapril; spironolactone, metipranolol, molsidomine, moxonidina, nadolol, nadoxolol, levodopa, metoprolol, and timolol, inclusive of pharmaceutically acceptable salts thereof.

17. The tablet of claim 1, in which the tablet preparation is carried out by compression of the powder or granular mixture and working between 1000 and 5000 Kg/cm2.

18. The tablet of claim 1, in which the lipophilic substance present in the active layer is selected from hydrogenated castor oil and glyceryl behenate.

19. The tablet of claim 1, in which the active layer consists of components (i) to (iv) wherein the active substance is contained in a percentage of 0.05% to 20% by weight of the active layer, the adjuvant substances are contained in a percentage of 5% to 50% by weight of the active layer, and the weight ratio of the hydrophilic polymeric substances to the lipophilic substances contained in the active layer is in the range of from 7:1 to 1:1.

20. The tablet of claim 1, in which the active layer consists essentially of components (i) to (iv) wherein the active substance is contained in a percentage of 0.05% to 20% by weight of the active layer, the adjuvant substances are contained in a percentage of 5% to 50% by weight of the active layer, and the weight ratio of the hydrophilic polymeric substances to the lipophilic substances contained in the active layer is in the range of from 7:1 to 1:1.

21. The tablet of claim 1, in which the hydrophilic polymeric substance comprises hydroxypropylmethylcellulose of molecular weight 2,000 to 4,000,000, sodium carboxymethylcellulose or calcium carboxymethylcellulose.

22. The tablet of claim 7, wherein the one or more barrier layers contain lipophilic substances.

23. The tablet of claim 22, wherein during the first hour after oral administration or immersion in aqueous liquids, release of the active substance occurs only from the surface of the tablet not covered by the one or more barrier layers.

24. The tablet of claim 7, wherein the barrier layer is applied to both surfaces (bases) of the active layer.

25. The tablet of claim 14, wherein said fat is selected from the group consisting of totally or partially hydrogenated beeswax, polyethoxylated beeswax, a mono-, bi- or tri-substituted glyceride, glyceryl palmitostearate glyceryl behenate, diethyleneglycol palmitostearate, a polyethyleneglycol stearate, a polyoxyethyleneglycol palmitostearate, glyceryl monopalmitostearate, cetyl palmitate, polyethyleneglycol palmitostearate, mono- or di-glyceryl behenate, cetyl alcohol, stearic acid, a saturated or unsaturated fatty acid, and hydrogenated castor oil.
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