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Claims for Patent: 6,979,463

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Claims for Patent: 6,979,463

Title: Stable extended release oral dosage composition
Abstract:A film-coated extended release solid oral dosage composition containing a nasal decongestant, pseudoephedrine or salt thereof, e.g., pseudoephedrine sulfate in a core effective to provide a geometric maximum plasma concentration of pseudoephedrine of about 345 ng/mL to about 365 ng/mL at a time of about 7.60 hrs to about 8.40 hrs and having two or three film-coatings on the core, the second one containing an amount of the non-sedating antihistamine, desloratadine, effective to provide a geometric maximum plasma concentration of desloratadine of about 2.15 ng/mL to about 2.45 ng/mL at a time of about 4.0 hours to about 4.5 hours, and use of the composition for treating patients showing the signs and symptoms associated with allergic and/or inflammatory conditions of the skin and airway passages are disclosed.
Inventor(s): Kou; Jim H. (Basking Ridge, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Application Number:10/175,460
Patent Claims: 1. An extended release solid oral dosage composition comprising (a) a core comprising an effective amount of pseudoephedrine or pharmaceutically acceptable salt thereof, (b) a first coating covering the core and comprising a water-swellable film-forming neutral or cationic copolymeric ester, a film modifier and a lubricant, and (c) a second coating covering the first coating and comprising an effective amount of desloratadine, wherein the amount of pseudoephedrine or pharmaceutically acceptable salt thereof is effective to produce a geometric maximum plasma concentration of pseudoephedrine of about 345 ng/mL to about 365 ng/mL at a time of about 7.60 hours to about 8.40 hrs, and the amount of desloratadine is effective to produce a geometric maximum plasma concentration of desloratadine of about 2.10 ng/mL to about 2.45 ng/mL at a time of about 4.0 hours to about 4.5 hours after administration of a single dose of said composition.

2. The extended release solid oral dosage composition of claim 1 wherein the amount of desloratadine is effective to produce a geometric maximum plasma concentration of 3-hydroxydesloratadine of about 0.75 ng/mL to about 1.15 ng/mL at a time of about 5.50 hours to about 6.25 hours after administration of a single dose of said composition.

3. The extended release solid oral dosage composition of claim 1 wherein the core is a matrix core and wherein the first coating uniformly covers the matrix core and the second coating uniformly covers the first coating.

4. The extended release solid oral dosage composition of claim 3 wherein (a) the first coating comprises (1) a water-swellable film-forming neutral or cationic co-polymeric ester; (2) a lubricant; (3) a film-modifier; and (4) optionally, an anti-foaming agent;

and wherein (b) the second coating comprises: (1) an effective amount of desloratadine sufficient to produce a geometric maximum plasma concentration of desloratadine of about 2.10 ng/mL to about 2.45 ng/mL at a time of about 4.0 hours to about 4.5 hours after administration of a single dose of said composition; (2) a water-swellable film-forming neutral or cationic co-polymeric ester; (3) a lubricant; (4) a water soluble film-modifier; and (5) optionally, an anti-foaming agent.

5. The extended release solid oral dosage composition of claim 4 wherein the amount of desloratadine is effective to produce a geometric maximum plasma concentration of 3-hydroxydesloratadine of about 0.75 ng/mL to about 1.15 ng/mL at a time of about 5.50 hours to about 6.25 hours after administration of a single dose of said composition.

6. The extended release solid oral dosage composition of claim 4 which further comprises a third coating covering the second coating, said third coating comprising: (1) a pharmaceutically acceptable dye; (2) a water-swellable film-forming neutral or cationic copolymeric ester; (3) a lubricant; (4) at least one water soluble film-modifier; and (5) optionally, an anti-foaming agent.

7. The extended release solid oral dosage composition of claim 6 wherein the water-soluble film-modifier is a low viscosity hydroxypropyl methylcellulose, hydroxyethyl methyl cellulose or sodium carboxymethyl cellulose or a polyethylene glycol selected from polyethylene glycol 200 to a polyethylene glycol 8000, or mixtures thereof.

8. The extended release solid oral dosage composition of claim 4 wherein the matrix core comprises a water-insoluble calcium, magnesium or aluminum salt, wherein the water-insoluble calcium, magnesium or aluminum salt is a carbonate, phosphate, silicate or sulfate of calcium, magnesium or aluminum or mixtures thereof.

9. An extended release solid oral dosage composition comprising (a) a core comprising about 240 mg of pseudoephedrine or pharmaceutically acceptable salt thereof, (b) a first coating covering the core and comprising a water-swellable film-forming neutral or cationic copolymeric ester, a film modifier and a lubricant, and (c) a second coating covering the first coating and comprising about 5 mg of desloratadine wherein total desloratadine degradation products in the extended release oral dosage composition is less than or equal to about 2.0% by weight.

10. The extended release solid oral dosage composition of claim 9 wherein the total desloratadine degradation products comprise less than or about 0.3 to about 0.4% by weight of N-methyldesloratadine, and less than or about 0.4 to about 0.5% by weight of N-formyldesloratadine.

11. The extended release solid oral dosage composition of claim 9 wherein total desloratadine degradation products in the extended release oral dosage composition comprise less than or about 0.8 to about 1.0 weight percent of the composition.

12. The extended release solid oral dosage composition of claim 9 wherein total pseudoephedrine degradation products in the extended release oral dosage composition comprise less than about 0.5 weight percent to no more than about 1.1 weight percent of the composition.

13. The extended release oral dosage composition of claim 1 wherein the matrix core comprises:

14. The extended release oral dosage composition of claim 4 wherein the first film coating comprises: (1) a neutral copolymer of ethyl acrylate and methyl acrylate; (2) a lubricant selected from talc, silicon, polyethylene glycol 200 to polyethylene glycol 8000; (3) a polyethylene glycol selected from polyethylene glycol 200 to polyethylene glycol 8000; and (4) optionally, a pharmaceutically acceptable mixture of homologous liquid methyl siloxane polymers and silica gel.

15. The extended release oral dosage composition of claim 4 wherein the second film coating comprises: (1) an amount of desloratadine effective to produce a geometric maximum plasma concentration of desloratadine of about 2.10 ng/mL to about 2.45 ng/mL at a time of about 4.0 hours to about 4.5 hours after administration of a single dose of said composition; (2) a neutral copolymer of ethyl acrylate and methyl acrylate; (3) a lubricant selected from talc, silicon dioxide and magnesium stearate; (4) a polyethylene glycol selected from polyethylene glycol 200 to a polyethylene glycol 8000; and (5) optionally, a pharmaceutically acceptable mixture of homologous liquid methyl siloxane polymers and silica gel.

16. The extended release oral dosage composition of claim 6 wherein the third coating comprises: (1) a neutral copolymer of ethyl acrylate and methyl acrylate; (2) a lubricant selected from talc, silicon dioxide and magnesium stearate; (3) an effective amount of a water-soluble film-modifying agent is a low viscosity hydroxypropyl methylcellulose, hydroxyethyl methylcellulose or sodium carboxymethyl cellulose, or a polyethylene glycol selected from polyethylene glycol 200 to a polyethylene glycol 8000, or mixtures thereof; (4) a pharmaceutically acceptable dye; and (5) optionally, a pharmaceutically acceptable mixture of homologous liquid methyl siloxane polymers and silica gel.

17. An extended release solid oral dosage composition comprising (a) a core comprising about 240 mg of pseudoephedrine or pharmaceutically acceptable salt thereof, and (b) a first coating comprising a water-swellable film-forming neutral or cationic copolymeric ester, a film modifier and a lubricant covering the core; and (c) a second coating covering the first coating comprising about 5 mg of desloratadine; wherein more than about 90% of the desloratadine in solid oral dosage composition dissolves into a stirred 0.1N HCl solution at 37.degree. C. in about 45 minutes, and more than about 90% of the pseudoephedrine sulfate in solid oral dosage composition dissolves into a stirred 0.1 N HCl solution at 37.degree. C. (1.sup.st hour) and thereafter in a stirred phosphate buffer having a pH of 7.5 at 37.degree. C. over 16 hours.

18. An extended release solid oral dosage composition comprising (a) a core comprising an effective amount of pseudoephedrine or pharmaceutically acceptable salt thereof, (b) a first coating covering the core and comprising a water-swellable film-forming neutral or cationic copolymeric ester, a film modifier and a lubricant, and (c) a second coating covering the first coating and comprising an effective amount of desloratadine wherein the amount of pseudoephedrine or pharmaceutically acceptable salt thereof is effective to produce a geometric mean steady state maximum plasma concentration of pseudoephedrine of about 382 ng/mL to about 664 ng/mL at a time of about 5.25 hrs to about 7.99 hrs after administration of a daily dose of said composition for at least about 10 consecutive days and the amount of desloratadine is effective to produce a geometric mean steady state maximum plasma concentration of desloratadine of about 1.59 ng/mL to about 3.39 ng/mL at a time of about 2.24 hours to about 5.12 hours after administration of a daily dose of said composition for at least about 12 consecutive days.

19. The extended release solid oral dosage composition of claim 18 wherein the geometric mean steady state maximum plasma concentration of pseudoephedrine is about 418 ng/mL to about 628 ng/mL at a time of about 5.32 hrs to about 7.98 hrs after administration of a daily dose of said composition for at least about 10 consecutive days and the geometric mean steady state maximum plasma concentration of desloratadine is about 1.95 ng/mL to about 2.93 ng/mL at a time of about 2.94 hours to about 4.42 hours after administration of a daily dose of said composition for at least about 12 consecutive days.

20. The extended release solid oral dosage composition of claim 18 wherein the amount of desloratadine is effective to produce a geometric mean steady state maximum plasma concentration of 3-hydroxy-desloratadine of about 1.25 ng/mL to about 1.87 ng/mL at a time of about 3.44 hours to about 5.86 hours and a geometric mean steady state value for the area under the plasma concentration-time curve from 0-24 hours for 3-hydroxy-desloratadine was about 20.3 ng hr/mL to about 3.11 ng hr/mL after administration of a daily dose of said composition for at least about 12 consecutive days.

21. The extended release solid oral dosage composition of claim 18 wherein the geometric mean steady state value for the area under the plasma concentration-time curve from 0 to 24 hours for desloratadine was about 23.0 ng hr/mL to about 46.6 ng hr/mL.

22. The extended release solid oral dosage composition of claim 18 wherein the geometric mean steady state value for the area under the plasma concentration-time curve from 0 to 24 hours for desloratadine was about 27.8 ng hr/mL to about 41.8 ng hr/mL.

23. The extended release solid oral dosage composition of claim 18 wherein the geometric mean steady state value for the area under the plasma concentration-time curve from 0 to 24 hours for pseudoephedrine was about 6244 ng hr/mL to about 11346 ng hr/mL.

24. The extended release solid oral dosage composition of claim 18 wherein the geometric mean steady state value for the area under the plasma concentration-time curve from 0 to 24 hours for psudoephedrine was about 7030 ng hr/mL to about 10554 ng hr/mL.

25. An extended release solid oral dosage composition comprising (a) a core comprising an effective amount of pseudoephedrine or pharmaceutically acceptable salt thereof, (b) a first coating covering the core and comprising a water-swellable film-forming neutral or cationic copolymeric ester, a film modifier and a lubricant, and (c) a second coating covering the the first coating and comprising an effective amount of desloratadine, wherein the amount of pseudoephedrine or pharmaceutically acceptable salt thereof is effective to produce a geometric mean steady state minimum plasma concentration of pseudoephedrine of about 82 ng/mL to about 243 ng/mL after administration of a daily dose of said composition for at least about 10 consecutive days and the amount of desloratadine is effective to produce a geometric mean steady state minimum plasma concentration of desloratadine of about 0.307 ng/mL to about 1.095 ng/mL after administration of a daily dose of said composition for at least about 12 consecutive days.

26. The extended release solid oral dosage composition of claim 25 wherein the geometric mean steady state minimum plasma concentration of pseudoephedrine is about 129 ng/mL to about 193 ng/mL after administration of a daily dose of said composition for at least about 10 consecutive days and the geometric mean steady state minimum plasma concentration of desloratadine is about 0.624 ng/mL to about 0.946 ng/mL after administration of a daily dose of said composition for at least about 12 consecutive days.

27. The extended release solid oral dosage composition of claim 25 wherein the amount of desloratadine is effective to produce a geometric mean steady state minimum plasma concentration of 3-hydroxy-desloratadine of about 0.503 ng/mL to about 0.875 ng/mL after administration of a daily dose of said composition for at least about 12 consecutive days.

28. The extended release solid oral dosage composition of claim 25 wherein the amount of desloratadine is effective to produce a geometric mean steady state minimum plasma concentration of 3-hydroxy-desloratadine of about 0.551 ng/mL to about 0.827 ng/mL after administration of a daily dose of said composition for at least about 12 consecutive days.

29. A method of treating allergic and inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treatment an effective amount of the extended release solid composition of claim 1.

30. A method of treating nasal congestion associated with allergic and inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treatment an effective amount of the extended release solid composition of claim 1.

31. A method of treating urticaria which comprises administering to a patient in need of such treatment an effective amount of the extended release solid composition of claim 1.

32. A method of treating the nasal and non-nasal symptoms of perennial and seasonal allergic rhinitis which comprises administering to a patient in need of such treatment an effective amount of the extended release solid composition of claim 1.
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