Claims for Patent: 10,517,880

Summary for Patent: 10,517,880

Title:	Stable fixed dose pharmaceutical composition comprising mometasone and olopatadine
Abstract:	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.
Inventor(s):	Dhuppad; Ulhas R. (Maharashtra, IN), Katkurwar; Ashok (Maharashtra, IN), Gupta; Yashwant (Maharashtra, IN), Ankam; Rajesh (Maharashtra, IN), Dhatrak; Chandrakant (Maharashtra, IN)
Assignee:	GLENMARK SPECIALTY S.A. (La Chaux-de-Fonds, CH)
Application Number:	15/703,801
Patent Claims:	1. A sprayer containing an aqueous pharmaceutical composition in the form of a single phase suspension comprising mometasone or its salt and olopatadine or its salt, wherein the sprayer delivers a spray of the composition to a human nose that results in a spray pattern having a longest axis of 15-75 mm, a shortest axis of 10-65 mm, and an ellipticity of 1-2. 2. A sprayer containing an aqueous pharmaceutical composition in the form of a suspension comprising mometasone furoate and olopatadine hydrochloride, wherein the sprayer delivers a spray of the composition to a human nose that results in a spray pattern having a longest axis of 15-75 mm, a shortest axis of 10-65 mm, and an ellipticity of 1-2. 3. The sprayer of claim 2, wherein each spray of the pharmaceutical composition from the sprayer comprises 25 mcg mometasone furoate form and 665 mcg olopatadine hydrochloride. 4. The sprayer of claim 3, wherein the pharmaceutical composition further comprises a hydrocolloid. 5. The sprayer of claim 4, wherein the hydrocolloid comprises carboxymethylcellulose sodium. 6. The sprayer of claim 3, wherein the pharmaceutical composition has a viscosity of 20 cps to 150 cps. 7. The sprayer of claim 4, wherein the hydrocolloid is in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25.+-.2.degree. C. and 60.+-.5% relative humidity. 8. The sprayer of claim 2, wherein the mometasone furoate is in particulate form and has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 9. The sprayer of claim 2, wherein the composition has a pH of 3.3 to 4.1. 10. The sprayer of claim 2, wherein the composition has a pH of 3.5 to 3.9. 11. The sprayer of claim 2, wherein the composition has an osmolality in the range of 250 mOsm/kg to 350 mOsm/kg. 12. The sprayer of claim 2, wherein the composition is a single phase aqueous suspension comprising: 0.025% w/w mometasone furoate monohydrate; 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. 13. A sprayer containing an aqueous pharmaceutical composition in the form of a single phase suspension comprising mometasone furoate and olopatadine hydrochloride, wherein the sprayer delivers a spray at 6 cm having a major axis of 52 to 63 mm, a minor axis of 47 to 53 mm, and an ellipticity of 1.1 to 1.2. 14. The sprayer of claim 13, wherein the pharmaceutical composition is a single phase suspension comprising mometasone furoate in particulate form and olopatadine hydrochloride in dissolved form. 15. The sprayer of claim 13, wherein the pharmaceutical composition further comprising a hydrocolloid. 16. The sprayer of claim 15, wherein the hydrocolloid comprises carboxymethylcellulose sodium. 17. The sprayer of claim 13, wherein the pharmaceutical composition has a viscosity of 20 cps to 150 cps. 18. The sprayer of claim 15, wherein the hydrocolloid is in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25.+-.2.degree. C. and 60.+-.5% relative humidity. 19. The sprayer of claim 14, wherein the mometasone furoate has a mean particle size in the range of 1 .mu.m to about 20 .mu.m. 20. The sprayer of claim 14, wherein the composition has a pH of 3.3 to 4.1. 21. The sprayer of claim 14, wherein the composition has a pH of 3.5 to 3.9. 22. The sprayer of claim 14, wherein the composition has an osmolality in the range of 250 mOsm/kg to 350 mOsm/kg. 23. The sprayer of claim 14, wherein the composition is a single phase aqueous suspension comprising: 0.025% w/w mometasone furoate monohydrate; 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. 24. A method of treating rhinitis in a human in need thereof comprising administering a pharmaceutical composition comprising mometasone furoate and olopatadine hydrochloride by spraying the sprayer of claim 2 into the nose of the human to provide an effective amount of the pharmaceutical composition. 25. A method of treating rhinitis in a human in need thereof comprising administering a pharmaceutical composition comprising mometasone furoate and olopatadine hydrochloride by spraying the sprayer of claim 13 into the nose of the human to provide an effective amount of the pharmaceutical composition. 26. A sprayer containing an aqueous pharmaceutical composition in the form of a single phase suspension comprising 25 mcg mometasone furoate in particulate form and 665 mcg olopatadine hydrochloride, wherein the sprayer delivers a spray at 6 cm having a D.sub.50 droplet size of 34.68 to 39.28 .mu.m. 27. The sprayer of claim 2, wherein the mometasone furoate is in particulate form and the olopatadine hydrochloride is in dissolved form. 28. The sprayer of claim 2, wherein the sprayer comprises (i) a container containing the pharmaceutical composition, (ii) a pump communicating with the pharmaceutical composition of the container, and (iii) an actuator communicating with a top portion of the pump to deliver the spray of the pharmaceutical composition. 29. The sprayer of claim 13, wherein the sprayer comprises (i) a container containing the pharmaceutical composition, (ii) a pump communicating with the pharmaceutical composition of the container, and (iii) an actuator communicating with a top portion of the pump to deliver the spray of the pharmaceutical composition. 30. The sprayer of claim 13, wherein, after storage at 25.+-..degree. C. and 60.+-.5% relative humidity for 3 to 6 months, the sprayer delivers a spray at 6 cm having a major axis of 61 to 63 mm, a minor axis of 51 to 53 mm, and an ellipticity of 1.2. 31. The sprayer of claim 23, wherein, after storage at 25.+-..degree. C. and 60.+-.5% relative humidity for 3 to 6 months, the sprayer delivers a spray at 6 cm having a major axis of 61 to 63 mm, a minor axis of 51 to 53 mm, and an ellipticity of 1.2. 32. The sprayer of claim 13, wherein, after storage at 40.+-..degree. C. and 75.+-.5% relative humidity for 3 months, the sprayer delivers a spray at 6 cm having a major axis of 58 mm, a minor axis of 49 mm, and an ellipticity of 1.2. 33. The sprayer of claim 23, wherein, after storage at 40.+-..degree. C. and 75.+-.5% relative humidity for 3 months, the sprayer delivers a spray at 6 cm having a major axis of 58 mm, a minor axis of 49 mm, and an ellipticity of 1.2.