US2016193339A1PendingUtilityA1
Transdermal formulations
Est. expiryDec 23, 2034(~8.5 yrs left)· nominal 20-yr term from priority
Inventors:Steven Hoffman
A61K 47/22A61K 38/28A61K 47/12A61P 3/10A61P 17/16A61K 47/10A61K 8/361A61K 8/4913A61K 8/34A61Q 19/007A61K 8/39A61K 9/0014A61K 45/06
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Claims
Abstract
The present disclosure is directed to transdermal and moisturizing compositions.
Claims
exact text as granted — not AI-modifiedWhat is claimed:
1 . A composition comprising
a first component comprising:
a compound of formula I
R—(OCH 2 CH 2 ) y —OH (I)
wherein R is C 1-20 alkyl, C 2-20 alkenyl; or C 2-20 alkynyl; and y is 1 to 25;
a tetrafunctional block copolymer surfactant terminating in primary hydroxyl groups;
a sorbitan derivative;
a C 8-10 alkyl ammonium salt;
a compound of formula II
HO—(CH 2 CH 2 O) m —C(CH 3 )(C 4 H 9 )—C≡C—C(CH 3 )(C 4 H 9 )—(OCH 2 CH 2 ) n —OH (II)
wherein m and n are each independently 1 to 25;
or a combination thereof;
a second component comprising:
an amide of the formula III
R 2 —N(R 1 )—C(O)—R 3 (III)
wherein
each R 1 is independently H or C 1-3 alkyl; and
R 2 and R 3 are independently C 1-7 alkyl or together with the atoms to which they are attached, form a lactam having 3 to 10 carbon atoms;
a sulfoxide;
a urea;
ethyl acetate;
or a combination thereof;
a C 2-10 alkyl alcohol; an organic acid having 1 to 25 carbon atoms; and optionally, water.
2 . The composition of claim 1 , wherein the first component is the compound of formula I.
3 . The composition of claim 2 , wherein R is C 1-20 alkyl.
4 . The composition of claim 2 , wherein y is 5 to 15.
5 . The composition of claim 3 , wherein the compound of formula I is cetomacrogol 1000;
octadecan-1-ol, ethoxylated; polyoxyethylene(12)tridecyl ether; polyoxyethylene(10)tridecyl ether; fatty alcohol polyoxyethylene ether, polyoxyethylene branched nonylcyclohexyl ether, nonaethylene glycol monododecyl ether, 23-{[4-(2,4,4-trimethyl-2-pentanyocyclohexyl]oxy}-3,6,9,12,15,18,21 -heptaoxatricosan-1-ol, or a combination thereof.
6 . The composition of claim 2 , wherein R is C 2-20 alkenyl.
7 . The composition of claim 6 , wherein the compound of formula I is polyoxyl(10)oleyl ether, polyethylene glycol tert-octylphenyl ether, or a combination thereof.
8 . The composition of claim 2 , wherein R is C 2-20 alkynyl.
9 . The composition claim 1 , wherein the first component is a tetrafunctional block copolymer surfactant terminating in primary hydroxyl groups.
10 . The composition of claim 9 , wherein the tetrafunctional block copolymer surfactant terminating in primary hydroxyl groups is ethylenediaminetetrakis(ethoxylate-Block-propoxylate).
11 . The composition of claim 1 , wherein the first component is a sorbitan derivative.
12 . The composition of claim 11 , wherein the sorbitan derivative is polyoxyethylene sorbitan tetraoleate, 1,4-anhydro-6-O-palmitoyl-D-glucitol (sorbitan, monohexadecanoate), a polyethylene glycol sorbitan monolaurate, or a combination thereof.
13 . The composition of claim 1 , wherein the first component is a C 8-10 alkyl ammonium salt.
14 . The composition of claim 13 , wherein the C 8-10 alkyl ammonium salt is methyltrialkyl(C 8 -C 10 )ammonium chloride (ADOGEN 464).
15 . The composition of claim 1 , wherein the first component is the compound of formula II.
16 . The composition of claim 1 , wherein the second component is the compound of formula III.
17 . The composition of claim 16 , wherein R 1 is methyl, ethyl, or propyl.
18 . The composition of claim 16 , wherein R 2 and R 3 , together with the atoms to which they are attached, form a lactam having 3 to 10 carbon atoms.
19 . The composition of claim 18 , wherein the lactam is a pyrrolidone.
20 . The composition of claim 1 , wherein the second component is a sulfoxide.
21 . The composition of claim 1 , wherein the second component is a urea.
22 . The composition of claim 1 , wherein the second component is ethyl acetate.
23 . The composition of claim 1 , wherein the C 2-10 alkyl alcohol is glycerol, propylene glycol, ethanol, isopropanol, 1-propanol, butanol, t-butanol, pentanol, 1-octanol, or a combination thereof.
24 . The composition of claim 1 , wherein the organic acid is a fatty acid or a C 1-6 alkyl acid.
25 . The composition of claim 1 comprising
about 36 vol. % of the first component;
about 4 vol. % of the second component;
about 48 vol. % of the C 2-10 alkyl alcohol; and
about 12 vol. % of the organic acid.
26 . The composition of claim 1 comprising
about 5 vol. % of the first component;
about 0.5 vol. % of the second component;
about 7 vol. % of the C 2-10 alkyl alcohol;
about 2 vol. % of the organic acid; and
about 85 vol. % of the water.
27 . The composition of claim 1 in the form of a gel, transdermal patch, lotion, cream, spray, emulsion, or dispersion.
28 . The composition of claim 1 , further comprising a therapeutic agent.
29 . A method comprising applying a composition of claim 28 to the skin of a mammal for a time sufficient to achieve permeation of at least a portion of the therapeutic agent through the skin.
30 . A method comprising administering a composition of claim 1 to the skin of a mammal for a time and under conditions effective to achieve passage of at least a portion of said composition through said skin.Cited by (0)
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