Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts
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 for 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.
1. A method for treating an external genital or perianal wart in a patient 12 years old or older in need thereof, the method comprising topically applying up to 250 mg of a 3.75% (w/w) imiquimod cream once a day to the wart, wherein the imiquimod cream is selected from the following:
Excipients
% w/w
% w/w
% w/w
% w/w
% w/w
% w/w
Formulation
181
182
183
184
185
186
Fatty acid*
20.00
20.00
25.00
18.75
2000
21.25
Cetyl alcohol
4.00
2.20
2.20
2.20
2.20
2.20
Stearyl alcohol
2.40
3.10
3.10
3.10
3.10
3.10
White petrolatum
2.80
3.00
3.00
5.00
5.00
3.75
Polysorbate 60
3.00
3.40
3.40
3.00
3.40
3.40
Sorbitan
1.00
0.60
0.60
1.00
0.60
0.60
Monostearate
Glycerin
1.00
2.00
2.00
5.00
5.00
5.00
Xanthan gum
0.30
0.50
0.50
0.50
0.50
0.50
Purified water
64.53
59.23
54.23
55.48
54.23
54.23
Benzyl alcohol
2.00
2.00
2.00
2.00
2.00
2.00
Methylparaben
0.20
0.20
0.20
0.20
0.20
0.20
Propylparaben
0.02
0.02
0.02
0.02
0.02
0.02
Imiquimod
3.75
3.75
3.75
3.75
3.75
3.75
Total
100.00
100.00
100.00
100.00
100.00
100.00
Formulation
187
188
189
190
191
192
Fatty acid*
20.00
20.00
20.00
25.00
18.75
25.00
Cetyl alcohol
2.20
2.20
2.20
2.20
2.20
2.70
Stearyl alcohol
3.10
3.10
3.10
3.10
3.10
3.80
White petrolatum
3.00
6.00
6.00
3.00
5.00
3.00
Polysorbate 60
3.40
3.40
3.00
3.40
3.00
3.40
Sorbitan
0.60
0.60
1.00
0.50
1.00
0.60
Monostearate
Glycerin
2.00
5.00
5.00
2.00
5.00
2.00
Xanthan gum
0.50
0.50
0.50
0.50
0.50
0.50
Purified water
59.23
53.23
53.23
54.33
55.48
53.03
Benzyl alcohol
2.00
2.00
2.00
2.00
2.00
2.00
Methylparaben
0,20
0.20
0.20
0.20
0.20
0.20
Propylparaben
0.02
0.02
0.02
0.02
0.02
0.02
Imiquimod
3.75
3.75
3.75
3.75
3.75
3.75
Total
100.00
100.00
100.00
100.00
100.00
100.00
Formulation
193
194
195
196
197
198
Fatty acid*
25.00
20.00
20.00
20.00
20.00
21.00
Cetyl alcohol
2.20
4.00
2.20
2.20
2.20
2.20
Stearyl alcohol
3.10
2.40
3.10
3.10
3.10
3.10
White petrolatum
3.00
3.40
5.00
3.00
5.00
5.00
Polysorbate 60
3.40
3.80
3.40
3.40
3.40
3.40
Sorbitan
0.60
1.00
0.60
0.60
0.60
0.60
Monostearate
Glycerin
2.00
3.00
2.00
5.00
5.00
5.00
Xanthan gum
1.00
0.70
0.50
0.50
0.50
0.50
Purified water
53.73
55.73
57.23
56.23
54.23
53.23
Benzyl alcohol
2.00
2.00
2.00
2.00
2.00
2.00
Methylparaben
0.20
0.20
0.20
0.20
0.20
0.20
Propylparaben
0.02
0.02
0.02
0.02
0.02
0.02
Imiquimod
3.75
3.75
3.75
3.75
3.75
3.75
Total
100.00
100.00
100.00
100.00
100.00
100.00
wherein the fatty acid selected from the group consisting of palmitic acid, linoleic acid, stearic acid, isostearic acid, unrefined oleic acid, super refined oleic acid and mixtures thereof.
2. The method of claim 1 , wherein up to 9.375 mg of imiquimod is applied daily.
3. The method of claim 1 , wherein up to 65.625 mg of imiquimod is applied weekly.
4. The method of claim 1 , wherein up to 525 mg of imiquimod is applied in the eight week treatment period.