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Claims for Patent: 6,143,329

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Claims for Patent: 6,143,329

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, trimcindone acetonide, and an odorless form of the composition.
Inventor(s): Kim; Soo-Il (Maple Glen, PA)
Assignee: Rorer Pharmaceutical Products Inc. (Greenville, DE)
Application Number:09/315,454
Patent 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 triamcinolone acetonide; (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 a compound that has anti-microbial properties.

2. A composition according to claim 1 further comprising about 0.004 to 0.02 wt. % of a quaternary ammonium compound that has antimicrobial properties and about 0.01 to about 0.5 wt. % of a chelating agent.

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. An article of manufacture comprising

(A) an aqueous pharmaceutical composition which comprises: a pharmaceutically effective amount of solid particles of triamcinolone acetonide which is effective in treating an abnormal bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity and 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 composition in unsheared form is relatively high, with the composition being a gel having said particles suspended therein; (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;

(B) a vessel which contains said composition; and

(C) a precompression pump which is associated with the vessel and which is capable of spraying a full dose of the composition into the nostril of an individual.

7. The article of manufacture of claim 6 wherein said composition further comprises an antimicrobial compound.

8. The article of manufacture of claim 6 wherein said composition further comprises a chelating agent.

9. The article of manufacture of claim 6 wherein said vessel contains greater than two full doses of said composition.

10. The article of manufacture of claim 6 wherein said vessel contains a least about 120 full doses of said composition.

11. The article of manufacture of claim 9 wherein said precompression pump is capable of spraying at least one full dose of about 100 mg of said composition into the nostril of an individual.

12. The article of manufacture of claim 9 wherein said precompression pump is capable of spraying at least one full dose of composition containing about 55 mcg of triamcinolone acetonide into the nostril of an individual.

13. An article of manufacture comprising:

(A) a thixotropic 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 7.5, and which comprises (a) triamcinolone acetonide; (b) a mixture of microcrystalline cellulose and carboxymethylcellulose sodium; (c) Polysorbate 80; (d) disodium ethylenediamine tetraacetate; (e) benzalkonium chloride; (f) dextrose; and (g) purified water;

(B) a vessel which contains said composition; and

(C) a precompression pump associated with the vessel and which is capable of spraying a full dose of the composition into the nostril of an individual.

14. A method for treating allergic rhinitis in an individual comprising the administration to said individual of an aqueous thixotropic pharmaceutical composition comprising:

(A) a pharmaceutically effective amount of solid particles of triamcinolone acetonide which is effective in treating allergic rhinitis by virtue of its being present on the mucosal surfaces of the nasal cavity of the individual; and

(B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition thixotropic properties; by spraying a full dose of the composition in the form of a readily flowable atomized mist into one of the nostrils of the individual for deposit on the mucosal surfaces of the nasal cavity in the form of a viscous composition which resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity.

15. The method of claim 14 wherein said administration of said composition is performed once daily.

16. The method of claim 15 wherein said once-a-day administration includes spraying multiple full doses of said composition.

17. The method of claim 14 wherein said composition resists being cleared from the mucosal surfaces for at least one hour.

18. The method of claim 14 wherein at least about 23% of said triamcinolone acetonide remains deposited in the inferior concha region of said nasal cavity of said individual two hours after administration.

19. The method of claim 14 wherein at least about 6% of said triamcinolone acetonide remains deposited in the superior concha region of said nasal cavity of said individual two hours after administration.

20. The method of claim 14 wherein at least about 47% of said triamcinolone acetonide remains deposited in the frontal cavity of said nasal cavity of said individual two hours after administration.

21. The method of claim 14 comprising spraying a total of about 200 to about 450 mcg of said triamcinolone acetonide into said nostril of said individual daily.

22. The method of claim 14 comprising spraying a total of about 100 to about 130 mcg of said triamcinolone acetonide into said nostril of said individual daily.

23. The method of claim 14 comprising spraying a full dose of about 55 mcg of said triamcinolone acetonide into said nostril of said individual.

24. The method of claim 23 including spraying two of said full doses into said nostril once-a-day.

25. A method for delivering an aqueous thixotropic pharmaceutical composition comprising triamcinolone acetonide to 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 comprising spraying a full dose of the composition in the form of a readily flowable atomized mist into each nostril of the individual and allowing said sprayed composition to deposit on said surfaces in the form of a viscous composition which resists being cleared from the mucosal surfaces by the inherent mucocilliary forces which are present in the nasal cavity.

26. The method of claim 25 wherein said composition comprises 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.

27. The method of claim 26 wherein at least about 47% of said triamcinolone acetonide remains deposited in the frontal cavity of the individual two hours after administration.

28. The method of claim 26 wherein at least about 23% of the triamcinolone acetonide remains deposited in the inferior concha region of the individual two hours after administration.

29. The method of claim 26 wherein at least about 6% of the triamcinolone acetonide remains deposited in the superior concha region of the individual two hours after administration.
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