US2013096203A1PendingUtilityA1

Low toxicity topical active agent delivery system

Assignee: YOUNG PHARMACEUTICALS INCPriority: Dec 15, 2009Filed: Nov 26, 2012Published: Apr 18, 2013
Est. expiryDec 15, 2029(~3.4 yrs left)· nominal 20-yr term from priority
Inventors:John E. Kulesza
A61P 37/02A61P 29/00A61P 31/00A61P 35/00A61P 17/06A61P 17/16A61P 17/00A61K 8/69A61K 31/07A61K 8/671A61Q 19/007A61K 47/50A61K 31/194A61K 31/60A61K 8/368A61Q 15/00A61K 8/585A61K 47/30A61K 8/38A61K 47/24A61K 31/203A61K 9/0014A61Q 19/08A61Q 19/00A61K 9/28A61K 47/08A61K 47/06A61K 31/327A61K 31/232
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Claims

Abstract

An active agent delivery composition is provided that allows topical delivery of active agents including vitamin A and its derivatives. A polyhalogenic vehicle such as methoxyonafluorobutane or ethoxyonafluorobutane serves as a coupler for an active agent and a silicone carrier so as to allow solubilization of active agents not normally miscible in silicones and providing a moisture maintaining composition.

Claims

exact text as granted — not AI-modified
1 - 21 . (canceled) 
     
     
         22 . An active agent topical delivery composition comprising:
 an active agent selected from the group consisting of vitamin A or its derivatives, hydroxy acids, and benzoyl peroxide;   a volatile linear organopolysiloxane carrier;   an organic polyhalogenic vehicle, said vehicle present at from 5 percent to 40 percent by weight; and   organic hydrocarbon solvent at less than 5% by weight;   said composition substantially free of water and ethanol, and said active agent fully solubilized in said composition.   
     
     
         23 . The composition of  claim 22  wherein said organic solvent is ethoxydiglycol. 
     
     
         24 . (canceled) 
     
     
         25 . The composition of  claim 22  wherein said active agent is a vitamin A derivative that is: retinal; retinoic acid; retinyl ester; retinol; tretinoin; isotretinoin; adapalene; tazarotene; or combinations thereof. 
     
     
         26 . The composition of  claim 22  wherein said active agent is vitamin A or its derivatives wherein said vitamin A or its derivatives are present at between 0.001 to 2 weight percent. 
     
     
         27 . The composition of  claim 22  wherein said hydroxy acid is salicylic acid, acetylsalicylic acid, or combinations thereof. 
     
     
         28 . The composition of  claim 22  wherein said agent is benzoyl peroxide, said benzyol peroxide present from 1 to 10 weight percent. 
     
     
         29 . The composition of  claim 22  wherein said volatile linear organopolysiloxane carrier is ethyl trisiloxane. 
     
     
         30 . The composition of  claim 29  wherein said ethyl trisiloxane is present at about  70  percent by weight. 
     
     
         31 . The composition of  claim 22  wherein said vehicle is methoxynonafluorobutane or ethoxynonafluorobutane. 
     
     
         32 . The composition of  claim 22  wherein said vehicle is present at 15 percent to 25 percent by weight. 
     
     
         33 . The composition of  claim 22  wherein said active agent is a retinoid. 
     
     
         34 . A skin care composition comprising:
 an active agent at a therapeutically effective concentration;   a volatile linear organopolysiloxane carrier of 2 to 6 silicon atoms;   an organic polyhalogenic vehicle having a boiling point less than 78 degrees Celsius; and   organic hydrocarbon solvent at 0-5 percent by weight;   said active agent insoluble in said carrier alone and said vehicle alone at said concentration;   said composition substantially free of water.   
     
     
         35 . The composition of  claim 34  wherein said active agent selected from the group consisting of vitamin A or its derivatives, hydroxy acids, and benzoyl peroxide. 
     
     
         36 . The composition of  claim 34  wherein said active agent is vitamin A or its derivatives wherein said vitamin A or its derivatives are present at between 0.001 to 2 weight percent. 
     
     
         37 . The composition of  claim 34  wherein said volatile linear organopolysiloxane carrier is ethyl trisiloxane, or a combination of ethyl trisiloxane and disiloxane. 
     
     
         38 . The composition of  claim 37  wherein said ethyl trisiloxane is present at about 70 percent by weight. 
     
     
         39 . The composition of  claim 34  wherein said vehicle is present at 5 percent to 25 percent by weight.

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