US2016193339A1PendingUtilityA1

Transdermal formulations

59
Assignee: HOFFMAN STEVENPriority: Dec 23, 2014Filed: Mar 11, 2016Published: Jul 7, 2016
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
59
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Claims

Abstract

The present disclosure is directed to transdermal and moisturizing compositions.

Claims

exact text as granted — not AI-modified
What 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.

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