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Claims for Patent: 4,782,047

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Claims for Patent: 4,782,047

Title: Aqueous steroid formulations for nasal administration
Abstract:A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.
Inventor(s): Benjamin; Eric (Sunnyvale, CA), Anik; Shabbir (Mountain View, CA), Lin; Ya-Yun T. (Cupertino, CA)
Assignee: Syntex Pharmaceuticals International Ltd. (Hamilton, BM)
Application Number:06/866,171
Patent Claims: 1. A stable, effectively preservable, substantially non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration, which formulation comprises:

an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v);

propylene glycol in an amount between about 2% and about 10% (w/v);

PEG 400 in an amount between about 10% and about 25% (w/v);

polysorbate 20 in an amount between about 1% and about 4% (w/v);

an effective amount of preservative;

an effective amount of antioxidant;

an effective amount of stabilizer;

water; and

pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.

2. The formulation of claim 1 which comprises:

3. The formulation of claim 1 which comprises:

preservative in an amount between about 0.02% and about 0.08% (w/v);

antioxidant in an amount between about 0.001% and about 0.05% (w/v); and

stabilizer in an amount between about 0.005% and about 0.05% (w/v).

4. The formulation of claim 3 wherein said anti-inflammatory steroid is flunisolide in an amount of about 0.025% (w/v).

5. The formulation of claim 4 wherein:

said preservative is benzalkonium chloride;

said stabilizer is disodium EDTA; and

said antioxidant is BHT.

6. The formulation of claim 5 which further comprises sorbitol in an amount between about 0.001% and about 5% (w/v).

7. The formulation of claim 6 wherein said pH buffering agent comprises:

citric acid in an amount between about 0.001% and about 0.05% (w/v); and

sodium citrate dihydrate in an amount between about 0.001% and about 0.05% (w/v).

8. A stable, effectively preservable, substantially non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration, which formulation comprises:

flunisolide hemihydrate in an amount of about 0.025% (w/v);

propylene glycol in an amount of about 5% (w/v);

PEG 400 in an amount of about 20% (w/v);

polysorbate 20 in an amount of about 2.50% (w/v);

benzalkonium chloride in an amount of about 0.035% (w/v);

disodium EDTA in an amount of about 0.01% (w/v);

BHT in an amount of about 0.01% (w/v);

citric acid in an amount of about 0.005% (w/v);

sodium citrate dihydrate in an amount of about 0.00765% (w/v);

sorbitol in an amount of about 2.00% (w/v); and

water, wherein the pH of the resulting solution is adjusted to about 5.2.

9. A method of treating inflammation of the nasal mucosa without inducing stinging, which method comprises intranasally administering to a subject in need thereof a substantially non-stinging aqueous anti-inflammatory steroid formulation comprising

an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v);

propylene glycol in an amount between about 2% and about 10% (w/v);

PEG 400 in an amount between about 10% and about 25% (w/v);

polysorbate 20 in an amount between about 1% and about 4% (w/v);

an effective amount of preservative;

an effective amount of antioxidant;

an effective amount of stabilizer;

water; and

pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.

10. The method of claim 9 wherein said formulation comprises:

preservative in an amount between about 0.02% and about 0.08% (w/v);

antioxidant in an amount between about 0.001% and about 0.05% (w/v); and

stabilizer in an amount between about 0.005% and about 0.05% (w/v).

11. The method of claim 10 wherein said anti-inflammatory steroid is flunisolide in an amount of about 0.025% (w/v).

12. The method of claim 11 wherein:

said preservative comprises benzalkonium chloride;

said stabilizer comprises disodium EDTA; and

said antioxidant comprises BHT.

13. The method of claim 12 which further comprises sorbitol in an amount between about 0.001% and about 5% (w/v).

14. The method of claim 13 wherein said pH buffering agent comprises:

citric acid in an amount between about 0.001% and about 0.05% (w/v); and

sodium citrate dihydrate in an amount between about 0.001% and about 0.05% (w/v).

15. A method of treating inflammation of the nasal mucosa without inducing stinging, which method comprises intranasally administering to a subject in need thereof a substantially non-stinging aqueous anti-inflammatory steroid formulation comprising

flunisolide hemihydrate in an amount of about 0.025% (w/v);

propylene glycol in an amount of about 5% (w/v);

PEG 400 in an amount of about 20% (w/v);

polysorbate 20 in an amount of about 2.50% (w/v);

benzalkonium chloride in an amount of about 0.035% (w/v);

disodium EDTA in an amount of about 0.01% (w/v);

BHT in an amount of about 0.01% (w/v);

citric acid in an amount of about 0.005% (w/v);

sodium citrate dihydrate in an amount of about 0.00765% (w/v);

sorbitol in an amount of about 2.00% (w/v); and

water, wherein the pH of the resulting solution is adjusted to about 5.2.
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