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Details for Patent: 6,375,984

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Details for Patent: 6,375,984

Title: Aqueous-based pharmaceutical composition
Abstract:An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (iii) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity, a method of use of the composition and a method for preparation of the composition, including in preferred form the use of anti-inflammatory steroid, for example, triamcinolone acetonide, and an odorless form of the composition.
Inventor(s): Kim; Soo-Il (Maple Glen, PA)
Assignee: Rorer Pharmaceuticals Products Inc. (Greenville, DE)
Filing Date:Apr 28, 2000
Application Number:09/561,371
Claims:1. An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual, which is propellant-free, and has a pH of about 4.5 to about 7.5, and which comprises: (A) at least about 85 wt. % of water; (B) about 0.001 to about 2 wt. % of solid particles of a medicament selected from the group consisting of dexamethasone and prednesolone; (C) about 1 to about 5 wt. % of a suspending agent comprising a mixture of about 85 to 95 wt. % of microcrystalline cellulose and about 5 to about 15 wt. % of carboxymethyl cellulose based on the weight of the mixture, the amount of suspending agent being effective to maintain said solid particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the composition in unsheared form is about 400 to about 800 centipoise; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition is about 50 to about 200 centipoise and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (iii) in deposited form on the mucosal surfaces, the viscosity of the composition is about 400 to about 800 centipoise and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity; and (D) about 0.004 to about 0.02 wt. % of a quaternary ammonium compound that has anti-microbial properties; and (E) about 0.01 to about 0.5 wt. % of a chelating agent.

2. A composition according to claim 1 wherein said quaternary ammonium compound is benzalkonium chloride and said chelating agent is disodium ethylenediamine tetraacetate.

3. A composition according to claim 1 having about 0.001 to about 0.01 wt. % of dispersing agent which is effective in wetting the particles of medicament.

4. A composition according to claim 3 wherein said dispersing agent is Polysorbate 80.TM..

5. A composition according to claim 1 including dextrose.

6. A method for treating allergic rhinitis in an individual comprising applying to the mucosal surfaces of the nasal cavities of an individual a composition according to claim 21 by spraying a dose of the composition into each of the nasal cavities of the individual, said dose containing a pharmaceutically effective amount of said medicament and depositing pharmaceutically effective amounts of the medicament on each of the mucosal surfaces of the anterior regions of the nose, the frontal sinus and the maxillary sinuses and on each of the mucosal surfaces which overlie the turbinates covering the conchas and such that pharmaceutically effective amounts of the medicament are retained on each of said mucosal surfaces for at least about an hour.

7. A method according to claim 6 wherein said quaternary ammonium compound is benzalkonium chloride, and said chelating agent is disodium ethylenediamine tetraacetate.

8. A method according to claim 6 wherein the composition which is applied to said surfaces includes about 0.001 to about 0.01 wt. % of dispersing agent which is effective in wetting the particles of medicament.

9. A method according to claim 8 wherein said dispersing agent is Polysorbate 80.TM..

10. A method according to claim 6 wherein the dose of composition applied to each of the nasal cavities comprises about 200 to about 450 mcg of medicament.

11. A method for preparing an aqueous pharmaceutical composition comprising a medicament in the form of solid particles of a medicament selected from the group consisting of dexamethasone and prednisolone, a dispersing agent for wetting said particles, and a suspending agent for maintaining said particles substantially uniformly dispersed in the composition and for imparting to the composition thixotropic properties, said method comprising: (A) providing an aqueous suspension of said particles and said dispersing agent; (B) providing a thixotropic aqueous suspension comprising said suspending agent; and (C) combining each of the suspensions by introducing one of the suspensions into the bottom of the other suspension.

12. The method of claim 11 wherein said dispersing agent is Polysorbate 80.TM..

13. The method of claim 11 wherein said suspending agent is a mixture of microcrystalline cellulose and carboxymethyl-cellulose sodium.

14. A method according to claim 11 wherein the suspension of particles is introduced into the bottom of the thixotropic suspension.

15. A method according to claim 11 wherein said dispersing agent is Polysorbate 80.TM. and wherein said suspension of (A) further comprises a quaternary ammonium anti-microbial agent and wherein the suspension of (B) further comprises a chelating agent and an anti-osmotic agent.

16. A method according to claim 15 wherein the anti-microbial agent consists essentially of benzalkonium chloride,the chelating agent consists essentially of EDTA and the anti-osmotic agent consists essentially of dextrose.

17. A method according to claim 6 wherein said composition is applied once daily to each of the nasal cavities of the individual in an amount which includes about 100 to about 130 mcg of said medicament.

18. A method according to claim 17 wherein said composition is applied by use of a precompression pump.
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