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Claims for Patent: 5,238,944

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Claims for Patent: 5,238,944

Title: Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
Abstract:Pharmaceutical formulations and adhesive-coated sheet materials for the topical and/or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, including creams, ointments and pressure-sensitive adhesive compositions. Pharmacological methods of using the formulations and the adhesive-coated sheet materials of the invention in the treatment of viral infections.
Inventor(s): Wick; Steven M. (Mahtomedi, MN), Schultz; Helen J. (Falcon Heights, MN), Nelson; Gregory R. (Hudson, WI), Mitra; Amit K. (Woodbury, MN), Berge; Stephen M. (Shoreview, MN)
Assignee: Riker Laboratories, Inc. (St. Paul, MN)
Application Number:07/845,323
Patent Claims: 1. A substantially non-irritating pharmaceutical formulation for topical and/or transdermal administration of the agent 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, which formulation comprises:

(a) a therapeutically effective amount of 1-isobutyl-1-H-imidazo[4,5-q]quinolin-4-amine; and

(b) a pharmaceutically acceptable vehicle for said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, which vehicle comprises isostearic acid in an amount of about 3 percent to about 45 percent by weight based on the total weight of said formulation, said formulation being further characterized in that, when tested according to the hairless mouse skin model the formulation provides a penetration of the agent of at least about 10 percent of the total amount of the agent contained in the formulation in 24 hours.

2. A formulation according to claim 1 wherein said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine is present in an amount of about 0.5 percent to about 9 percent by weight based on the total weight of said formulation.

3. A formulation according to claim 1 in the form of a cream, comprising an oil phase and a water phase in admixture, said oil phase comprising:

(a) said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine;

(b) said isostearic acid;

(c) one or more emollients present in a total amount of about 5 percent to about 30 percent by weight based on the total weight of said formulation; and

(d) one or more emulsifiers selected from the group consisting of a nonionic surface active agent and a trivalent cationic emulsifier and present in a total amount of about 2 percent to about 14 percent by weight based on the total weight of said formulation;

said water phase comprising water in an amount of about 45 percent to about 85 percent by weight based on the total weight of said formulation.

4. A formulation according to claim 3 wherein said isostearic acid is present in an amount of about 5 percent to about 25 percent by weight based on the total weight of said formulation.

5. A formulation according to claim 1 in the form of an ointment comprising:

(a) said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine;

(b) said isostearic acid in ana mount of about 3 percent to about 25 percent by weight based on the total weight of said formulation; and

(c) a pharmaceutically acceptable ointment base in an amount of about 60 percent to about 95 percent by weight based on the total weight of said formulation.

6. A formulation according to claim 3 wherein said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine is present in an amount of about 1 percent to about 5 percent by weight based on the total weight of said formulation.

7. A formulation according to claim 4, comprising about 1 percent of said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, about 10 percent of said isostearic acid, about 2 percent benzyl alcohol, about 2.2 percent cetyl alcohol, about 3.1 percent stearyl alcohol, about 2.55 percent polysorbate 60, about 0.45 percent sorbitan monostearate, about 2 percent glycerin, about 0.2 percent methylparaben, about 0.02 percent propylparaben and about 76.48 percent purified water, all percentages being based on the total weight of said formulation.

8. A formulation according to claim 4, comprising about 1 percent of said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, about 10 percent of said isostearic acid, about 6 percent cetearyl alcohol, about 2.55 percent polysorbate 60, about 0.45 percent sorbitan monostearate, about 2 percent glycerin, about 0.2 percent methylparaben, about 0.02 percent propylparaben and about 77.78 percent purified water, all percentages being based on the total weight of said formulation.

9. A formulation according to claim 4, comprising about 1 percent of said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, about 10 percent of said isostearic acid about 2 percent benzyl alcohol, about 1.7 percent cetyl alcohol, about 2.3 percent stearyl alcohol, about 2.55 percent polysorbate 60, about 0.45 percent sorbitan monostearate, about 2 percent glycerin, about 0.2 percent methylparaben, about 0.02 percent propylparaben and about 77.78 percent purified water, all percentages being based on the total weight of said formulation.

10. A formulation according to claim 4, comprising about 5 percent of said 1-isobutyl-1H-imidazo-[4,5-c]quinolin-4-amine, about 25 percent of said isostearic acid, about 2 percent benzyl alcohol, about 2.2 percent cetyl alcohol, about 3.1 percent stearyl alcohol, about 3 percent petrolatum, about 3.4 percent polysorbate 60, about 0.6 percent sorbitan monostearate, about 2 percent glycerin, about 0.2 percent methylparaben, about 0.02 percent propylparaben and about 53.48 percent purified water, all percentages being based on the total weight of said formulation.

11. A formulation according to claim 4, comprising about 1 percent of said 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, about 5 percent of said isostearic acid, about 15 percent petrolatum, about 12.8 percent light mineral oil, about 8 percent aluminum stearate, about 4 percent cetyl alcohol, about 3 percent polyglyceryl-4 oleate, about 1 percent acetylated lanolin, about 0.063 percent propylparaben, about 1 percent Veegum K, about 0.12 percent methylparaben and about 49.02 percent purified water, all percentages being based on the total weight of said formulation.

12. A method of topical and/or transdermal administration of 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine for treating a viral disease in a mammal, which method comprises

(1) placing a formulation according to claim 1 on the skin of a mammal; and

(2) allowing said formulation to remain in contact with the skin for a sufficient time to permit an effective amount of the 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine to penetrate the skin to achieve the antiviral effect.

13. A method of topical and/or transdermal administration of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine to induce interferon biosynthesis in a mammal, which method comprises

(1) placing a formulation according to claim 1 on the skin of a mammal; and

(2) allowing said formulation to remain in contact with the skin for a sufficient time to permit an effective amount of 1-isobutyl 1H-imidazo[4,5-c]-quinolin-4-amine to penetrate the skin to induce interferon biosynthesis.
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