Extended release oral dosage composition
View Patent ↗A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.
1. A solid composition comprising: (1) an immediate release layer comprising an anti-allergic effective amount of desloratadine and a desloratadine-protective amount of two pharmaceutically acceptable antioxidants; and (2) a sustained release layer comprising an effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable sustained release agent; wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to about 2% by weight, and wherein at least about 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
2. The solid composition of claim 1 wherein the two pharmaceutically acceptable antioxidants are edetate disodium and citric acid.
3. A solid composition comprising: (1) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable antioxidant; and (2) a sustained release second layer comprising an effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable sustained release agent; wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to about 2% by weight, and wherein at least about 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
4. A solid composition comprising: (1) an immediate release first layer comprising about 2.5 mg of desloratadine and a desloratadine-protective amount of at least one pharmaceutically acceptable antioxidant; (2) a sustained release second layer comprising about 120 mg of pseudoephedrine or a pharmaceutically acceptable salt thereof; and (3) a pharmaceutically acceptable excipient, wherein at least about 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
5. The solid composition of claim 4 wherein the total amount of desloratadine degradation products is less than or equal to about 2% by weight.
6. The solid composition of claim 4 wherein a desloratadine-protective amount of a pharmaceutically acceptable binder is present in the sustained release second layer.
7. The solid composition comprising a first and a second layer wherein the first layer is an immediate release layer comprising:
INGREDIENT
mg/composition
Desloratadine, micronized
5.0
Corn Starch
36.0
Microcrystalline Cellulose
140.7
Edetate Disodium
10.0
Citric Acid
2.0
Talc
6.0
Dye
0.30
TOTAL
200.00
and wherein the second layer is a sustained release layer comprising:
INGREDIENT
mg/composition
Pseudoephedrine Sulfate
120.0
Hydroxypropyl Methylcellulose 2208, 100,000 cps
105.0
Microcrystalline Cellulose
103.5
Hydroxypropyl Methylcellulose 2910
10.5
Edetate Disodium
3.5
Silicon Dioxide
5.0
Magnesium Stearate (Non-Bovine)
2.5
TOTAL
350.0
TOTAL Tablet Weight
550.0
wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to about 2% by weight.
8. A solid composition comprising a first layer and a second layer, wherein the first layer is an immediate release first layer comprising:
INGREDIENT
mg/composition
Desloratadine, micronized
2.5
Corn Starch
18.0
Microcrystalline Cellulose
71.22
Edetate Disodium
5.0
Citric Acid
1.0
Talc
3.0
Dye
0.28
TOTAL
100.00
and wherein the second layer is a sustained release layer comprising:
INGREDIENT
mg/composition
Pseudoephedrine Sulfate
120.0
Hydroxypropyl Methylcellulose 2208
105.0
Microcrystalline cellulose
103.5
Edetate Disodium
3.5
Hydroxypropyl Methylcellulose 2910
10.5
Silicon Dioxide
5.0
Magnesium stearate
2.5
TOTAL
350.0
and wherein total amount of desloratadine degradation products in the solid composition is less than or equal to about 2% by weight.
9. The solid composition of claim 8 wherein at least about 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
10. A method of treating allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 1 .
11. A method of treating the signs and symptoms of nasal congestion associated with allergic and inflammatory conditions of the upper or lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 1 .
12. A method of treating the signs and symptoms of nasal congestion associated with allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 3 .
13. A method of treating the signs and symptoms of nasal congestion associated with allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 4 .
14. A method of treating the signs and symptoms of nasal congestion associated with allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 8 .
15. A method of treating the signs and symptoms of urticaria which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 1 .
16. A method of treating the signs and symptoms of urticaria which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 3 .
17. A method of treating the signs and symptoms of urticaria which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 4 .
18. A method of treating the signs and symptoms of urticaria which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 7 .
19. A method of treating the signs and symptoms of urticaria which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 8 .
20. A method of treating the nasal and non-nasal symptoms of perennial or seasonal allergic rhinitis which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 1 .
21. A method of treating the nasal and non-nasal symptoms of perennial or seasonal allergic rhinitis which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 3 .
22. A method of treating the nasal and non-nasal symptoms of perennial or seasonal allergic rhinitis which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 4 .
23. A method of treating the nasal and non-nasal symptoms of perennial or seasonal allergic rhinitis which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 7 .
24. A method of treating the nasal and non-nasal symptoms of perennial or seasonal allergic rhinitis which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 8 .
25. A method of treating allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 3 .
26. A method of treating allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 4 .
27. A method of treating allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 7 .
28. A method of treating allergic or inflammatory conditions of the upper and lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 8 .
29. A method of treating the signs and symptoms of nasal congestion associated with allergic and inflammatory conditions of the upper or lower airway passages and skin which comprises administering to a patient in need of such treating an effective amount of the solid composition of claim 7 .