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Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts

a technology of genital and perianal warts and formulations, which is applied in the field of pharmaceutical formulations, can solve the problems of inconvenient regimens, high recurrence rate, pain or burning associated with therapy, and unknown clinical relevance of findings, and achieve the effect of simplified dosing regimens and low dosage strength imiquimod

Inactive Publication Date: 2011-08-25
MEDICIS PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0019]The present invention addresses the above-mentioned limitations associated with the treatment of EGWs with FDA-approved Aldara® 5% imiquimod cream through the discovery of novel and improved imiquimod treatment regimens of short duration, lower dosage strength imiquimod pharmaceutical formulations, and simplified dosing regimens to treat EGWs.

Problems solved by technology

However, the clinical relevance of these findings is unknown.
Each of these therapies has disadvantages such as inconvenient regimens, pain or burning associated with the therapy, scarring, itching, or high recurrence rates.
Notwithstanding FDA approval, Aldara® 5% imiquimod cream treatment for EGWs is not without limitation, including an unsimplified and lengthy dosing regimen (administration three times per week until total clearance of EGWs is achieved, or up to 16 weeks).
The eccentric dosing schedule is not easy to remember, which could lead to reduced compliance with resulting reduced efficacy.
If applied too thickly or generously, Aldara® 5% imiquimod cream can cause site or local skin reactions, such as erosions or ulcerations, causing pain or dysfunction (e.g., of the foreskin or urethra).
In addition, efficacy of treatment with Aldara® 5% imiquimod cream may be limited, especially in men, in patients with longstanding or recurrent disease, or for treatment of keratinized areas (e.g., inguinal).

Method used

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  • Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts
  • Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts
  • Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0211]A cream according to the present invention is prepared from the following ingredients:

% by WeightAmountOil Phase1-isobutyl-1H-imidazo[4.5-c]-quinolin-4-amine1.040.0 gIsostearic acid10.0400.0 gBenzyl alcohol2.080.0 gCetyl alcohol2.288.0 gStearyl alcohol3.1124.0 gPolysorbate 602.55102.0 gSorbitan monostearate0.4518.0 gAqueous Phase Glycerin2.080.0 gMethylparaben0.28.0 gPropylparaben0.020.8 gPurified water76.483059.2 g

[0212]The materials listed above were combined according to the following procedure: The glycerin, methylparaben, propylparaben and water were weighed into a 4 liter glass beaker then heated on a hot plate with stirring until the parabens isostearic acid and 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine were weighed into an 8 liter stainless steel beaker and heated on a hot plate until the amine was in solution (the temperature reached 69° C.). The benzyl alcohol, cetyl alcohol, stearyl alcohol, polysorbate 60 and sorbitan monostearate were added to the isostearic a...

examples 2-9

[0213]Using the general method of Example 1, the cream formulations shown in Tables 1 and 2 are prepared.

TABLE 1% by WeightExample Example Example Example 2345Oil Phase1-isobutyl-1H-imidazo[4,5-1.01.01.01.0c]quinolin-4-amineIsostearic acid10.010.05.05.0Benzyl alcohol2.0Cetyl alcohol1.7Stearyl alcohol2.3Cetearyl alcohol6.06.06.0Polysorbate 602.552.552.552.55Sorbitan monostearate0.450.450.450.45Brij ™ 30a10.0Aqueous PhaseGlycerin2.02.02.02.0Methylparaben0.20.20.20.2Propylparaben0.020.020.020.02Purified water77.7877.7882.7872.78aBrij ™ 30 (polyoxyethylene(4) lauryl ether) is available from ICI Americas, Inc.

TABLE 2% by WeightExample Example Example Example 67 89Oil Phase1-isobutyl-1H-imidazo-[4,5-1.01.01.01.0c]quinolin-4-amineIsostearic acid10.025.010.06.0Benzyl alcohol2.02.0Cetyl alcohol2.21.7Stearyl alcohol3.12.3Cetearyl alcohol6.06.0Polysorbate 602.553.42.552.55Sorbitan monostearate0.450.60.450.45Brij ™ 30a10.0Aqueous PhaseGlycerin2.02.02.02.0Methylparaben0.20.20.20.2Propylparaben0....

example 10

[0214]A cream according to the present invention is prepared from the following ingredients in the following Table 3:

TABLE 3% by WeightAmountOil Phase1-isobutyl-1H-imidazo[4,5-1.03.00gc]quinolin-4-amineIsostearic acid5.015.0gWhite petrolatum15.045.0gLight mineral oil12.838.4gAluminum stearate8.024.0gCetyl alcohol4.012.0gWitconol ™ 14a3.09.00gAcetylated lanolin1.03.0gPropylparaben0.0630.19gAqueous PhaseVeegum ™ Kb1.03.0gMethylparaben0.120.36gPurified water49.017147.05gaWitconol ™ 14 (polyglyceryl4 oleate) is available from Witco Chemical Corp. Organics DivisionbVeegum ™ K (colloidal magnesium aluminum silicate) is available from R. T. Vanderbilt Company Inc.

[0215]The materials listed above were combined according to the following procedure: The 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine and the isostearic acid were weighed into a glass jar and heated with occasional stirring until the amine was dissolved (the temperature reached 68° C.). To this solution was added, the petrolatum, ...

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Abstract

Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital / perianal warts with shorter durations of therapy than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital / perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital / perianal warts are also disclosed and described.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is entitled to and claims priority benefit to U.S. Utility patent application Ser. No. 12 / 771,076 filed Apr. 30, 2010; and priority benefit under 35 U.S.C. §119(e) to U.S. Provisional Application No. 61 / 341,721 filed Apr. 1, 2010; U.S. Provisional Application No. 61 / 341,476 filed Mar. 30, 2010; and U.S. Provisional Patent Application No. 61 / 225,202, filed Jul. 13, 2009; entitled “LOWER DOSAGE STRENGTH IMIQUIMOD FORMULATIONS AND SHORT DOSING REGIMENS FOR TREATING GENITAL AND PERIANAL WARTS”, the contents of which are incorporated herein by reference in their entireties.FIELD OF THE INVENTION[0002]The present invention relates to pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c-quinolin-4-amine, also known as (a.k.a.) 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, a.k.a. imiquimod, to treat genital and perianal warts with shorter durations of therapy, than...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4745A61P17/12
CPCA61K31/44A61K31/4745A61K9/0014A61K47/10A61K47/12A61K9/06A61P15/00A61P17/12A61P31/12A61P31/22
Inventor NORDSIEK, MICHAEL T.LEVY, SHARON F.LEE, JAMES H.KULP, JAMES H.BALAJI, KODUMUDI S.MENG, TZE-CHIANGWU, JASON J.BAHM, VALYN S.BABILON, ROBERT
Owner MEDICIS PHARMA CORP
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