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Claims for Patent: 7,927,624

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Claims for Patent: 7,927,624

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 (Loechle, FR), Grenier; Pascal (Kappelen, FR), Maggi; Lauretta (Pavia, IT), Conte; Ubaldo (Busto Arsizio, IT)
Assignee: Jagotec AG (Muttenz, CH)
Application Number:11/717,502
Patent Claims: 1. A multi-layer controlled release tablet, consisting of: (a) one active layer which consists of: (i) 0.05-20% by weight of ropinirole, inclusive of pharmaceutically acceptable salts thereof, (ii) hydrophilic polymeric substances which swell and gel and/or erode upon contact with aqueous liquids, (iii) lipophilic substances, and (iv) 5-50% by weight of 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 7:1 to 1:1, and in which said hydrophilic polymeric substances (ii) are contained in a percentage between 30% and 75% of the weight of the active layer, and (b) one or more barrier layers which limit the release surface of the active layer, which barrier layers contain 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; which tablet is optionally coated.

2. The multi-layer controlled release tablet of claim 1, wherein the active substance is ropinirole hydrochloride.

3. The multi-layer controlled release tablet of claim 1, in which said lipophilic substances (iii) are contained in a percentage between 5% and 55% of the weight of the active layer.

4. The multi-layer controlled release tablet of claim 1, in which said adjuvant substances (iv) are contained in a percentage between 10% to 40% of the weight of the active layer.

5. The multi-layer controlled release tablet of claim 1, 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, 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 galactomannan, gellans, xanthans, alginic acid, polyaminoacids, methyl vinyl ether/maleic anhydride copolymer, carboxymethylcellulose, ethylcellulose, methylcellulose, starch, and alpha, beta or gamma cyclodextrin.

6. The multi-layer controlled release tablet of claim 1, wherein the hydrophilic polymeric substances in the active layer comprise: (a) one or more of the following: hydroxypropylcellulose with a molecular weight between 100,000 and 4,000,000, hydroxypropylmethylcellulose (HPMC) with a molecular weight between 2,000 and 4,000,000, ethylcellulose or methylcellulose; and b) sodium carboxymethylcellulose, carboxymethylcellulose, hydroxypropylcellulose with a molecular weight of from 100,000 to 4,000,000, a carboxyvinyl polymer, a carrageenan, a xanthan, alginic acid, ethylcellulose, methylcellulose, dextrin and/or maltodextrin.

7. The multi-layer controlled release tablet of claim 6, wherein the hydrophilic polymeric substances in the active layer include hydroxypropylmethylcellulose and sodium carboxymethylcellulose.

8. The multi-layer controlled release tablet of claim 5, wherein the hydrophilic polymeric substances in the active layer comprise hydroxypropylmethylcellulose having a molecular weight in the range 20,000 and 500,000 or a 2% viscosity in the range of 80,000 to 120,000 mPa.sec.

9. The multi-layer controlled release tablet of claim 8, wherein the hydrophilic polymeric substances in the active layer comprise hydroxypropylmethylcellulose having a molecular weight of about 250,000.

10. The multi-layer controlled release tablet of claim 5, wherein the hydroxypropylmethylcellulose in the active layer is a gellable hydroxypropylmethylcellulose.

11. The multi-layer controlled release tablet of claim 1, in which said lipophilic substances include a natural fat as such or totally or partially hydrogenated, beeswax, polyethyoxylated 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/or hydrogenated castor oil.

12. The multi-layer controlled release tablet of claim 11, in which the lipophilic substance present in the active layer is selected from hydrogenated castor oil and glyceryl behenate.

13. The multi-layer controlled release tablet of claim 1, in which the active substance is ropinirole inclusive of pharmaceutically acceptable salts thereof contained in a percentage of 0.05% to 20% by weight of the active layer, (ii) the hydrophilic polymeric substance comprises hydroxypropylmethylcellulose, sodium carboxymethylcellulose or calcium carboxymethylcellulose, (iii) the lipophilic substance comprises hydrogenated castor oil or glyceryl behenate, and (iv) 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.

14. The multi-layer controlled release tablet of claim 1, in which the weight ratio of hydrophilic swelling and/or gelling and/or erodable polymeric substances to lipophilic substances contained in the barrier layer is in the range of 1:1 to 7.5:1.

15. The multi-layer controlled release tablet of claim 1, in which the amount of ropinirole present, inclusive of pharmaceutically acceptable salts thereof, is up to 12.0 mg, measured as the amount of ropinirole base present.

16. The multi-layer controlled release tablet of claim 15, in which the amount of ropinirole present, inclusive of pharmaceutically acceptable salts thereof, is from 0.75 mg to 12 mg, measured as the amount of ropinirole base present.

17. The multi-layer controlled release tablet of claim 1, in which said one or more barrier layers are applied to one or both surfaces (bases) of the active layer.

18. The multi-layer controlled release tablet of claim 17, wherein a barrier layer is applied to both surfaces (bases) of the active layer

19. The multi-layer controlled release tablet of claim 1, wherein release of ropinirole during the first hour after oral administration or immersion in aqueous liquids occurs only from the surface of the tablet not covered by the one or more barrier layers.

20. The multi-layer controlled release tablet of claim 1, which consists of an active layer and two barrier layers, one barrier layer being applied to each surface (base) of the active layer, wherein the active layer weighs about 150 mg and consists essentially of up to 12 mg ropinirole HCl (measured as the amount of ropinirole base present), 41% HPMC type 2208 (100,000 cps), 10% carboxylmethylcellulose sodium, 5% maltodextrin, 10% hydrogenated castor oil, 1% magnesium stearate, 0.6% colloidal silicon dioxide and lactose monohydrate quantum sufficiat, and wherein the barrier layers weigh between 120-170 mg, the barrier layers consisting essentially of 23.6% mannitol, 25% glyceryl behenate, 5% polyvinylpyrrolidone, 1% magnesium stearate, 0.4% colloidal silicon dioxide, HPMC type 2208 (100,000 cps) and optionally a colouring agent ana quantum sufficiat, wherein said controlled release tablet is optionally film coated with about 13.80 mg of a coating agent.

21. The multi-layer controlled release tablet of claim 20, wherein the active layer weighs 150 mg and consists of up to 12 mg ropinirole HCl (measured as the amount of ropinirole base present), 41% HPMC type 2208 (100,000 cps), 10% carboxylmethylcellulose sodium, 5% maltodextrin, 10% hydrogenated castor oil, 1% magnesium stearate, 0.6% colloidal silicon dioxide and lactose monohydrate quantum sufficiat, and wherein the barrier layers weigh between 120-170 mg, the barrier layers consisting of 23.6% mannitol, 25% glyceryl behenate, 5% polyvinylpyrrolidone, 1% magnesium stearate, 0.4% colloidal silicon dioxide, HPMC type 2208 (100,000 cps) and optionally a colouring agent ana quantum sufficiat, wherein said controlled release tablet is optionally film coated with 13.80 mg of a coating agent.

22. The multi-layer controlled release tablet of claim 21, wherein one barrier layer weighs about 170 mg and the other barrier layer weighs about 140 mg.

23. The multi-layer controlled release tablet of claim 22, wherein one barrier layer weighs 170 mg and the other barrier layer weighs 140 mg.

24. The multi-layer controlled release tablet of claim 23, wherein said tablet is film coated with 13.80 mg of a coating agent.

25. The multi-layer controlled release tablet of claim 21, wherein one barrier layer weighs about 130 mg and the other barrier layer weighs about 120 mg.

26. The multi-layer controlled release tablet of claim 25, wherein one barrier layer weighs 130 mg and the other barrier layer weighs 120 mg.

27. The multi-layer controlled release tablet of claim 26, wherein said tablet is uncoated.

28. The multi-layer controlled release tablet of claim 21, wherein said barrier layers contain a colouring agent.

29. The multi-layer controlled release tablet of claim 28, wherein said colouring agent is yellow ferric oxide.

30. The multi-layer controlled release tablet of claim 21, wherein the amount of ropinirole HCl in the active layer is 0.75-12 mg, measured as the amount of ropinirole free base present.

31. The multi-layer controlled release tablet of claim 1, which tablet is not coated by a film of gastroresistant and enterosoluble polymeric material.

32. The multi-layer controlled release 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/cm.sup.2.

33. A method of treating Parkinson's Disease comprising administering to a human in need of such treatment one or more multi-layer controlled release tablets as defined in any preceding claim.

34. The method of claim 33, in which one or more multi-layer controlled release tablets are administered once per day to the human in need of such treatment.

35. The method The claim 34, in which a single multi-layer controlled release tablet is administered once per day to the human in need of such treatment.
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