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 an anti-allergic effective amount of desloratadine in a free base form and a desloratadine-protective amount of at least one pharmaceutically acceptable antioxidant, wherein: the desloratadine does not form a pharmaceutically acceptable salt with the antioxidant; about 0.1% to about 10% of the at least one pharmaceutically acceptable antioxidant is present; at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes; and the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
2. A solid composition comprising about 5 mg of desloratadine in a free base form and a desloratadine-protective amount of at least one pharmaceutically acceptable antioxidant, wherein: the desloratadine does not form a pharmaceutically acceptable salt with the antioxidant; about 0.1% to about 10% of the at least one pharmaceutically acceptable antioxidant is present; at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes; and the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
3. A solid composition comprising:
INGREDIENT
mg/composition
Desloratadine, micronized
5.0
Corn Starch
36.0
Microcrystalline Cellulose
132.7
Edetate Disodium
10.0
Citric Acid Anhydrous
10.0
Stearic Acid
6.0
Dye
0.3
TOTAL
200.0
wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
4. The solid composition of claim 3 wherein at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
5. A solid composition comprising:
INGREDIENT
mg/composition
Desloratadine, micronized
2.5
Corn Starch
18.0
Microcrystalline Cellulose
66.35
Edetate Disodium
5.0
Citric Acid
5.0
Stearic Acid
3.0
Dye
0.15
TOTAL
100.00
and wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
6. The solid composition of claim 5 wherein at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
7. 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 2 .
8. A solid composition comprising an anti-allergic effective amount of desloratadine in a free base form and a desloratadine-protective amount of two pharmaceutically acceptable antioxidants, wherein the two pharmaceutically acceptable antioxidants are edetate disodium and citric acid, and wherein: the desloratadine does not form a pharmaceutically acceptable salt with the antioxidant; about 0.1% to about 10% of the two pharmaceutically acceptable antioxidants is present; at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes; and the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
9. A solid composition comprising about 2.5 mg desloratadine in a free base form and a desloratadine-protective amount of at least one pharmaceutically acceptable antioxidant, wherein: the desloratadine does not form a pharmaceutically acceptable salt with the antioxidant; about 0.1% to about 10% of the at least one pharmaceutically acceptable antioxidant is present; at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes; and the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
10. A solid composition 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
0.3
TOTAL
200.0
wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
11. The solid composition of claim 10 wherein at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
12. A solid composition comprising:
INGREDIENT
mg/composition
Desloratadine, micronized
2.5
Corn Starch
18.0
Microcrystalline Cellulose
70.35
Edetate Disodium
5.0
Citric Acid
1.0
Talc
3.0
Dye
0.28
TOTAL
100.00
wherein the total amount of desloratadine degradation products in the solid composition is less than or equal to 2% by weight.
13. The solid composition of claim 12 wherein at least 80% of the desloratadine dissolves in a 0.1N HCl solution at 37° C. in about 45 minutes.
14. 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 .
15. 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 9 .
16. 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 10 .
17. 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 12 .
18. 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 .