LONG-ACTING TOPICAL FORMULATION AND METHOD OF USE THEREOF
Provided herein are long-acting, non-aqueous pharmaceutically acceptable compositions of active ingredients for topical administration.
1 . A topical pharmaceutically acceptable composition, comprising:
a) a pharmaceutically active agent;
b) benzyl alcohol; and
c) propylene carbonate.
2 . The composition of claim 1 , wherein the benzyl alcohol is present at about 50.0 to 90.0% w/w.
3 . The composition of claim 1 , wherein the propylene carbonate is present at about 5.0 to 30.0% w/w.
4 . A topical pharmaceutically acceptable composition, comprising:
a) a pharmaceutically active agent;
b) N-methyl-2-pyrrolidone (NMP);
c) 2-pyrrolidone; and
d) a triglyceride carrier.
5 . The composition of claim 4 , wherein the combination of NMP and 2-pyrrolidone are present at about 30.0 to 70.0% w/w.
6 . The composition of claim 5 , wherein the NMP is present at about 15.0 to 25.0% w/w.
7 . The composition of claim 5 , wherein the 2-pyrrolidone is present at about 25.0 to 35.0% w/w.
8 . The composition of claim 4 , wherein the triglyceride carrier is present at about 25.0 to 60.0% w/w.
9 . The composition of claim 1 , wherein the composition further comprises an antioxidant.
10 . The composition of claim 1 , wherein the butylated hydroxy toluene (BHT).
11 . The composition of claim 1 , wherein the pharmaceutically active agent is a macrolide parasiticide.
12 . The composition of claim 1 , wherein the macrolide parasiticide is moxidectin, selamectin, milbemycin, ivermectin, doramectin, emamectin, eprinomectin, doximectin, abimectin, roxithromycin, clarithromycin, tulathromycin, gamithromycin, dirithromycin, fidaxomicin, megalomicin, erythromycin, azithromycin, or combination thereof.
13 . The composition of claim 1 , wherein the macrolide parasiticide is moxidectin.
14 . The composition of claim 1 , wherein the pharmaceutically active agent is an isoxazoline compound.
15 . The composition of claim 1 , wherein the isoxazoline compound is afoxolaner, fluralaner, sarolaner, lotilaner, or a combination thereof.
16 . The composition of claim 1 , wherein the composition comprises moxidectin and fluralaner.
17 . The composition of claim 1 , wherein the pharmaceutically active agent is present in an amount of about 1.0 to 25.0% w/w.
18 . The composition of claim 1 , wherein at least about 5-15 ng/ml of the pharmaceutically active agent is present in the blood stream of the subject for at least about 50 or 60 days or greater upon administration to a mammal.
19 . The composition of claim 1 , wherein at least about 2-10 ng/ml of the pharmaceutically active agent is present in the blood stream of the subject for at least about 90 days or greater upon administration to a mammal.
20 . A method of treating a disease or disorder in a subject, comprising topically administering to the subject an effective amount of a composition of claim 1 .
21 . The method of claim 20 , wherein the subject is a mammal.
22 . The method of claim 20 , wherein the subject is a canine.
23 . The method of claim 20 , wherein the subject is a feline.
24 . The method of claim 20 , wherein the disease or disorder is an infection.
25 . The method of claim 20 , wherein the disease or disorder is a parasitic or microbial infection.
26 . The method of claim 20 , wherein the disease or disorder is ectoparasitic infestation.
27 . The method of claim 20 , wherein the ectoparasite is body lice, crab lice, scabies, fleas or ticks.
28 . The method of claim 20 , wherein the parasitic infection is heartworm.
29 . The method of claim 20 , wherein at least about 5-15 ng/ml of the pharmaceutically active agent is present in the blood stream of the subject for at least about 50 or 60 days or greater upon administration to a mammal.
30 . The method of claim 20 , wherein at least about 2-10 ng/ml of the pharmaceutically active agent is present in the blood stream of the subject for at least about 90 days or greater upon administration to a mammal.
31 . The method of claim 20 , wherein the composition is administered once every 2, 3, 4, 5 or 6 months.
32 . The method of claim 20 , wherein the composition is administered at most once every 2, 3, 4, 5 or 6 months, and wherein the subject remains substantially infection free for at least 2, 3, 4, 5, 6 months or more after each administration.
33 . A method of preventing or treating heartworm in a subject, comprising topically administering to the subject an effective amount of a composition of claim 1 .
34 . The method of claim 33 , wherein the subject is a canine or feline.
35 . The method of claim 33 , wherein the composition is administered at most once every 2, 3, 4, 5 or 6 months, and wherein the subject remains substantially heartworm free for at least 2, 3, 4, 5, 6 months or more after each administration.
36 . A method of killing ectoparasites on a subject, comprising topically administering to the subject an effective amount of a composition of claim 1 .
37 . The method of claim 36 , wherein the subject is a canine or feline.
38 . The method of claim 36 , wherein the ectoparasite is body lice, crab lice, scabies, fleas or ticks.
39 . The method of claim 36 , wherein the composition is administered at most once every 2, 3, 4, 5 or 6 months, and wherein the subject remains substantially free of living ectoparasites for at least 2, 3, 4, 5, 6 months or more after each administration.
40 . A method of killing ectoparasites on a subject and preventing or treating heartworm in the subject, comprising topically administering to the subject an effective amount of a composition of claim 1 .
41 . The method of claim 40 , wherein the subject is a canine or feline.
42 . The method of claim 40 , wherein the ectoparasite is body lice, crab lice, scabies, fleas or ticks.
43 . The method of claim 40 , wherein the composition is administered at most once every 2, 3, 4, 5 or 6 months, and wherein the subject remains substantially heartworm free and free of living ectoparasites for at least 2, 3, 4, 5, 6 months or more after each administration.