Claims for Patent: 9,750,754

Summary for Patent: 9,750,754

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. (Nashik, 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:	15/183,534
Patent Claims:	1. A method of treating allergic rhinitis comprising intranasal administration of a fixed dose aqueous pharmaceutical composition comprising (a) 0.001% w/w to 0.075% w/w mometasone or its salt in particulate form; (b) 0.5% w/w to 0.8% w/w olopatadine or its salt in dissolved form; and (c) a hydrocolloid, wherein the composition is stable for at least 24 hours when stored at about 25.degree. C. and about 60% relative humidity. 2. The method of claim 1, wherein the mometasone or its salt and the olopatadine or its salt are present in a weight ratio of 1:3 to 1:106. 3. The method of claim 1, wherein the mometasone salt is mometasone furoate and the olopatadine salt is olopatadine hydrochloride. 4. The method of claim 1, wherein the mometasone or its salt has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 5. The method of claim 1, wherein the composition has a pH of 3.3 to 4.1. 6. The method of claim 1, wherein the composition has a pH of 3.3-4.1, and an osmolality in the range of 200 mOsm/kg to 400 mOsm/kg. 7. The method of claim 1, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 8. The method of claim 1, wherein the hydrocolloid is at least 0.1% w/w of the composition. 9. A method of treating seasonal allergic rhinitis comprising intranasal administration of a fixed dose aqueous pharmaceutical composition comprising (a) 0.001% w/w to 0.075% w/w mometasone or its salt in particulate form; (b) 0.5% w/w to 0.8% w/w olopatadine or its salt in dissolved form; and (c) a hydrocolloid, wherein the composition is stable for at least 24 hours when stored at about 25.degree. C. and about 60% relative humidity. 10. The method of claim 9, wherein the mometasone or its salt and the olopatadine or its salt are present in a weight ratio of 1:3 to 1:106. 11. The method of claim 9, wherein the mometasone salt is mometasone furoate and the olopatadine salt is olopatadine hydrochloride. 12. The method of claim 9, wherein the mometasone or its salt has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 13. The method of claim 9, wherein the composition has a pH of 3.3 to 4.1. 14. The method of claim 9, wherein the composition has a pH of 3.3-4.1, and an osmolality in the range of 200 mOsm/kg to 400 mOsm/kg. 15. The method of claim 9, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 16. The method of claim 9, wherein the hydrocolloid is at least 0.1% w/w of the composition. 17. A method of treating perennial allergic rhinitis comprising intranasal administration of a fixed dose aqueous pharmaceutical composition comprising (a) 0.001% w/w to 0.075% w/w mometasone or its salt in particulate form; (b) 0.5% w/w to 0.8% w/w olopatadine or its salt in dissolved form; and (c) a hydrocolloid, wherein the composition is stable for at least 24 hours when stored at about 25.degree. C. and 60% relative humidity. 18. The method of claim 17, wherein the mometasone or its salt and the olopatadine or its salt are present in a weight ratio of 1:3 to 1:106. 19. The method of claim 17, wherein the mometasone salt is mometasone furoate and the olopatadine salt is olopatadine hydrochloride. 20. The method of claim 17, wherein the mometasone or its salt has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 21. The method of claim 17, wherein the composition has a pH of 3.3 to 4.1. 22. The method of claim 17, wherein the composition has a pH of 3.3-4.1, and an osmolality in the range of 200 mOsm/kg to 400 mOsm/kg. 23. The method of claim 17, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 24. The method of claim 17, wherein the hydrocolloid is at least 0.1% w/w of the composition. 25. A method of treating allergic rhinitis comprising intranasal administration of a stable fixed dose aqueous pharmaceutical composition comprising 0.025% or 0.05% 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; and 0.01% w/w polysorbate 80, wherein the composition has a pH of 3.3 to 4.1. 26. The method of claim 25, wherein the mometasone furoate monohydrate has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 27. The method of claim 25, wherein the composition has an osmolality in the range of 200 mOsm/kg to 400 mOsm/kg. 28. The method of claim 25, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 29. A stable fixed dose aqueous pharmaceutical composition for nasal administration to a human, the composition comprises (a) 0.001% w/w to 0.075% w/w mometasone or its salt; (b) 0.5% w/w to 0.8% w/w olopatadine or its salt; (c) one or more cellulose derivatives, and (d) one or more additional excipients. 30. The pharmaceutical composition of claim 29, wherein the one or more cellulose derivatives suppress phase separation. 31. The pharmaceutical composition of claim 29, wherein the one or more cellulose derivatives suppress phase separation for at least 24 hours when stored at about 25.degree. C. and about 60% relative humidity. 32. The pharmaceutical composition of claim 29, wherein the cellulose derivatives include carboxymethyl cellulose sodium. 33. The pharmaceutical composition of claim 29, wherein the mometasone or its salt and the olopatadine or its salt are present in a weight ratio of 1:3 to 1:106. 34. The pharmaceutical composition of claim 29, wherein the mometasone salt is mometasone furoate and the olopatadine salt is olopatadine hydrochloride. 35. The pharmaceutical composition of claim 29, wherein the mometasone or its salt has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 36. The pharmaceutical composition of claim 29, wherein the composition has a pH of 3.3 to 4.1. 37. The pharmaceutical composition of claim 29, wherein the composition has a pH of 3.3-4.1, and an osmolality in the range of 200 mOsm/kg to 400 mOsm/kg. 38. The pharmaceutical composition of claim 29, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 39. An aqueous pharmaceutical composition for nasal administration to a human, the composition comprises (a) 0.001% w/w to 0.075% w/w mometasone or its salt; (b) 0.5% w/w to 0.8% w/w olopatadine hydrochloride, wherein the composition is substantially free of crystals of olopatadine hydrochloride. 40. The pharmaceutical composition of claim 39, wherein the mometasone or its salt and the olopatadine hydrochloride are present in a weight ratio of 1:3 to 1:106. 41. The pharmaceutical composition of claim 39, wherein the mometasone salt is mometasone furoate. 42. The pharmaceutical composition of claim 39, wherein the mometasone or its salt has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 43. The pharmaceutical composition of claim 39, wherein the composition has a pH of 3.3 to 4.1. 44. The pharmaceutical composition of claim 39, wherein the composition has a pH of 3.3-4.1, and an osmolality in the range of 200 mOsm/kg to 400 mOsm/kg. 45. The pharmaceutical composition of claim 39, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 46. The pharmaceutical composition of claim 39, wherein the composition contains less than 2% of crystalline olopatadine hydrochloride, based upon 100% total weight of olopatadine hydrochloride in the composition. 47. A stable fixed dose aqueous pharmaceutical composition for nasal administration to a human, the composition comprises (a) 0.001% w/w to 0.075% w/w mometasone or its salt; (b) 0.5% w/w to 0.8% w/w olopatadine or its salt; (c) 0.1% w/w to 3% w/w of sodium carboxymethyl cellulose, and (d) one or more additional excipients, wherein the composition has a pH of 3.3 to 4.1. 48. The pharmaceutical composition of claim 47, wherein the carboxymethyl cellulose is present in the range of 0.15% w/w to 0.75% w/w. 49. The pharmaceutical composition of claim 47, wherein the composition has a viscosity in the range of 10 cps to 150 cps. 50. The pharmaceutical composition of claim 47, wherein the sodium carboxymethyl cellulose suppresses phase separation for at least 24 hours when stored at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 51. The pharmaceutical composition of claim 47, wherein the one or more additional excipients are selected from chelating agents, preservatives, buffers, surfactants, isotonicity agents, taste masking agents, antioxidants, humectants, pH adjusting agents, and mixtures thereof.