Claims for Patent: 10,376,526

Summary for Patent: 10,376,526

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:	15/703,758
Patent Claims:	1. An aqueous pharmaceutical composition for nasal administration to a human in the form of a suspension comprising mometasone furoate, olopatadine hydrochloride, and a hydrocolloid in an amount sufficient for the suspension to remain in a single phase after 3 months of storage at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 2. The aqueous pharmaceutical composition of claim 1, wherein the composition has a pH of between 3.3 and 4.1. 3. The aqueous pharmaceutical composition of claim 1, wherein the composition has an osmolality of 200 mOsm/kg to 400 mOsm/kg. 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 0.025% w/w mometasone furoate, 0.665% w/w olopatadine hydrochloride, and a hydrocolloid in an amount sufficient for the suspension to remain in a single phase after 3 months of storage at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 7. The aqueous pharmaceutical composition of claim 6, wherein the pharmaceutical composition further comprising a hydrocolloid. 8. The aqueous pharmaceutical composition of claim 7, wherein the hydrocolloid comprises carboxymethylcellulose sodium. 9. The aqueous pharmaceutical composition of claim 6, wherein the pharmaceutical composition has a viscosity of 20 cps to 150 cps. 10. The aqueous pharmaceutical composition of claim 6, wherein the mometasone furoate has a mean particle size in the range of 1 .mu.m to 20 .mu.m. 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. The aqueous pharmaceutical composition of claim 6, 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. 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.degree. C. and 60%.+-.5% relative humidity. 16. The aqueous composition of claim 15, wherein the composition is substantially free of crystals of olopatadine hydrochloride after 6 months of storage at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 17. The aqueous composition of claim 15, wherein the composition contains less than 0.2% by weight of crystalline olopatadine hydrochloride, based on the 100% total weight of olopatadine hydrochloride in the composition, after 3 months of storage at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 18. The aqueous composition of claim 17, wherein the composition contains less than 0.1% by weight of crystalline olopatadine hydrochloride, based on the 100% total weight of olopatadine hydrochloride in the composition, after 3 months of storage at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 19. The aqueous composition of claim 16, wherein the composition contains less than 0.2% by weight of crystalline olopatadine hydrochloride, based on the 100% total weight of olopatadine hydrochloride in the composition, after 6 months of storage at 25.+-.2.degree. C. and 60%.+-.5% relative humidity. 20. The aqueous composition of claim 16, wherein the composition contains less than 0.1% by weight of crystalline olopatadine hydrochloride, based on the 100% total weight of olopatadine hydrochloride in the composition, after 6 months of storage at 25.+-.2.degree. C. and 60%.+-.5% RH. 21. The aqueous composition of claim 15, wherein the composition has a pH of 3.3 to 4.1. 22. The aqueous composition of claim 15, wherein the composition has a pH of 3.5 to 3.9. 23. The aqueous composition of claim 15, wherein the composition further comprises a hydrocolloid. 24. The aqueous composition of claim 23, wherein the hydrocolloid comprises carboxymethylcellulose sodium. 25. The aqueous composition of claim 15, wherein the composition has a viscosity of 20 cps to 150 cps. 26. The aqueous composition of claim 15, wherein the composition has an osmolality in the range of 250 mOsm/kg to 350 mOsm/kg. 27. The aqueous composition of claim 15, wherein the composition comprises 0.025% by weight of mometasone furoate monohydrate and 0.665% by weight of olopatadine hydrochloride. 28. The aqueous pharmaceutical composition of claim 1, wherein the composition has a pH of between 3.5 and 3.9. 29. The aqueous pharmaceutical composition of claim 1, wherein the composition further comprises a buffer. 30. The aqueous pharmaceutical composition of claim 29, wherein the buffer comprises dibasic sodium phosphate. 31. The aqueous pharmaceutical composition of claim 15, wherein the composition further comprises a buffer. 32. The aqueous pharmaceutical composition of claim 31, wherein the buffer comprises dibasic sodium phosphate.