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. An aqueous pharmaceutical composition for nasal administration to a human in the form of a suspension comprising (a) mometasone furoate in the form of particles having a mean particle size of from 1 μm to 20 μm, (b) olopatadine hydrochloride, and (c) a hydrocolloid in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25±2° C. and 60±5% relative humidity, wherein the mometasone furoate and olopatadine hydrochloride are the sole active ingredients in the composition.
2. The aqueous pharmaceutical composition of claim 1 , wherein the mean particle size of the mometasone furoate is from 1 μm to 15 μm.
3. The aqueous pharmaceutical composition of claim 1 , wherein the composition has a pH of between 3.3 and 4.1.
4. The aqueous pharmaceutical composition of claim 1 , wherein the composition has an osmolality of 250 mOsm/kg to 350 mOsm/kg.
5. The aqueous pharmaceutical composition of claim 1 , wherein the composition has a viscosity of 20 to 150 cps.
6. An aqueous pharmaceutical composition for nasal administration to a human in the form of a suspension comprising (a) 0.025% to 0.05% by weight of mometasone furoate in the form of particles having a mean particle size of from 1 μm to 20 μm, (b) 0.6% to 0.7% by weight of olopatadine hydrochloride, and (c) a hydrocolloid in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25±2° C. and 60±5% relative humidity, wherein the mometasone furoate and olopatadine hydrochloride are the sole active ingredients in the composition.
7. The aqueous pharmaceutical composition of claim 6 , wherein the mean particle size of the mometasone furoate is from 1 μm to 15 μm.
8. The aqueous pharmaceutical composition of claim 6 , wherein the mometasone furoate is mometasone furoate monohydrate.
9. The aqueous pharmaceutical composition of claim 6 , wherein the hydrocolloid comprises carboxymethylcellulose sodium.
10. The aqueous pharmaceutical composition of claim 6 , wherein the pharmaceutical composition has a viscosity of 20 cps to 150 cps.
11. The aqueous pharmaceutical composition of claim 6 , wherein the composition has a pH of 3.3 to 4.1.
12. The aqueous pharmaceutical composition of claim 6 , wherein the composition has a pH of 3.5 to 3.9.
13. The aqueous pharmaceutical composition of claim 6 , wherein the composition has an osmolality in the range of 250 mOsm/kg to 350 mOsm/kg.
14. An aqueous pharmaceutical composition for nasal administration to a human in the form of a suspension, wherein the composition comprises:
0.025% w/w mometasone furoate monohydrate in the form of particles having a mean particle size of from 1 μm to 20 μm;
0.665% w/w olopatadine hydrochloride;
0.5% w/w carboxymethyl cellulose sodium;
1.2% w/w of a mixture of microcrystalline cellulose and carboxymethyl cellulose sodium;
0.02% w/w benzalkonium chloride;
0.41% w/w sodium chloride;
0.01% w/w di-sodium edetate;
0.94% w/w sodium phosphate heptahydrate; and
0.01% w/w polysorbate 80,
wherein the composition has a pH of 3.3 to 4.1, and wherein the mometasone furoate and olopatadine hydrochloride are the sole active ingredients in the composition.
15. The aqueous pharmaceutical composition of claim 6 , wherein the composition is substantially free of crystals of olopatadine hydrochloride after 3 months of storage at 25±2° C. and 60%±5% relative humidity.
16. The aqueous pharmaceutical composition of claim 6 , wherein the composition is substantially free of crystals of olopatadine hydrochloride after 6 months of storage at 25±2° C. and 60%±5% relative humidity.
17. The aqueous pharmaceutical composition of claim 1 , wherein the composition has a pH of 3.5 to 3.9.
18. The aqueous pharmaceutical composition of claim 1 , wherein the pharmaceutical composition has a viscosity of 20 cps to 60 cps.
19. The aqueous pharmaceutical composition of claim 14 , wherein the composition has a pH of 3.5 to 3.9.
20. The aqueous pharmaceutical composition of claim 14 , wherein the pharmaceutical composition has a viscosity of 20 cps to 60 cps.
21. The aqueous pharmaceutical composition of claim 6 , wherein the composition comprises 0.025% by weight of mometasone furoate.
22. An aqueous fixed dose pharmaceutical composition for nasal administration to a human in the form of a suspension comprising (a) 0.025% w/w mometasone furoate in the form of particles having a mean particle size of from 1 μm to 20 μm, (b) 0.665% w/w olopatadine hydrochloride, and (c) a hydrocolloid in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25±2° C. and 60±5% relative humidity, wherein the mometasone furoate and olopatadine hydrochloride are the sole active ingredients in the composition.