Stable fixed dose pharmaceutical composition comprising mometasone and olopatadine
The present invention relates to a stable fixed dose aqueous pharmaceutical composition (e.g., contained in a container) for nasal administration to a human, comprising mometasone or its salt, olopatadine or its salt. The composition may further include a hydrocolloid. The invention also relates to a process for preparing the pharmaceutical composition, and the use of the pharmaceutical composition in the treatment of rhinitis in a subject.
1. A stable fixed dose aqueous pharmaceutical composition for nasal administration to a human, the composition being a suspension which comprises (a) mometasone or its salt in particulate form; (b) olopatadine or its salt in dissolved form; wherein the pharmaceutical composition, upon nasal administration of a dose equivalent to 2400 mcg of olopatadine or its salt to a human, results in (a) an area under the curve (AUC) 0-∞ for olopatadine or its salt of about 42.5 ng·hr/mL to about 116.5 ng·hr/mL, (b) a C max for olopatadine or its salt of about 10.3 ng/mL to about 24.1 ng/ml, or (c) any combination of any of the foregoing.
2. The pharmaceutical composition of claim 1 , wherein the composition, upon nasal administration of a dose equivalent to 2400 mcg of olopatadine or its salt to a human, results in a T max for olopatadine or its salt of about 15 mins to about 120 mins.
3. The pharmaceutical composition of claim 1 , wherein the AUC 0-∞ for olopatadine or its salt is from about 56.7 ng·hr/mL to about 99.8 ng·hr/mL.
4. The pharmaceutical composition of claim 1 , wherein the mometasone salt is mometasone furoate and the olopatadine salt is olopatadine hydrochloride.
5. The pharmaceutical composition of claim 1 , wherein the composition comprises about 0.025% w/w to about 0.05% w/w of mometasone or its salt and about 0.6% w/w to about 0.7% w/w olopatadine or its salt.
6. The pharmaceutical composition of claim 1 , wherein the C max of olopatadine is from about 13.8 ng/mL to about 20.7 ng/mL.
7. The pharmaceutical composition of claim 1 , further comprising a hydrocolloid.
8. The pharmaceutical composition of claim 1 , wherein the composition has a viscosity in the range of about 20 cps to about 150 cps.
9. A stable fixed dose aqueous pharmaceutical composition for nasal administration to a human, the composition being a suspension which comprises (a) mometasone or its salt, (b) olopatadine or its salt, and (c) a fibrillar network comprising a cellulosic material.
10. The pharmaceutical composition of claim 9 , wherein the fibrillar network further comprises interfibrillar spaces.
11. The pharmaceutical composition of claim 9 , wherein the mometasone or its salt is present in particulate form having an average particle size of less than about 15 μm.
12. The pharmaceutical composition of claim 10 , wherein the interfibrillar spaces contain one or more mometasone particles.
13. The pharmaceutical composition of claim 12 , wherein the mometasone particles are equidistantly, or substantially equidistantly, spaced within the fibrillar network.
14. The pharmaceutical composition of claim 9 , wherein the composition delivers consistent dosing for at least 30 inhalations.
15. The pharmaceutical composition of claim 14 , wherein the composition delivers consistent dosing for 60 inhalations.
16. The pharmaceutical composition of claim 14 , wherein the composition delivers consistent dosing for 120 inhalations.
17. The pharmaceutical composition of claim 9 , further comprising a hydrocolloid.
18. The pharmaceutical composition of claim 17 , wherein the hydrocolloid comprises carboxymethylcellulose.
19. The pharmaceutical composition of claim 18 , wherein the carboxymethylcellulose is present in the amount of from about 0.1% w/w to about 2% w/w.
20. The pharmaceutical composition of claim 1 , wherein the pH of the composition is from about 3.3 to about 4.1.
21. The pharmaceutical composition of claim 20 , wherein the pH of the composition is from about 3.5 to about 3.7.