Transdermal silicone gel (silogel) compositions and methods of preparation

Abstract

A silicone gel (“silogel”) composition used to deliver pharmaceutical products transdermally as well as a method for producing the silogel composition, which may contain up to 80% additive ingredients. Preferred embodiments of the invention may include silogel compositions which provide high viscosity/no separation due to API. They are not temperature-sensitive, have no shear stress from the ointment mill/EMP, have no gumming up/stickiness, and no hardening.

What is claimed: 
     
         1 . A silicone gel composition comprising:
 a hydrophilic silicone copolyol, wherein the hydrophilic silicone copolyol comprises phenyl trimethicone;   a lipophilic silicone copolyol, wherein the lipophilic silicone copolyol comprises C30-45 dimethicone;   a non-ionic oil-in-water (O/W) emulsifier agent, wherein the non-ionic oil-in-water (O/W) emulsifier agent comprises a blend of cetearyl alcohol and ceteareth-20;   a non-ionic water-in-oil (W/O) emulsifier agent, wherein the non-ionic water-in-oil (W/O) emulsifier agent comprises a copolymer of hydroxyethyl acrylate and sodium acryloyldimethyl taurate;   an inorganic hydrocolloid, wherein the inorganic hydrocolloid comprises magnesium aluminum silicate;   an organic hydrocolloid, wherein the organic hydrocolloid comprises hydroxypropyl starch phosphate; and   a biocompatible surfactant with phosphatidylcholine, wherein the biocompatible surfactant comprises lecithin.   
     
     
         2 . The silicone gel composition of  claim 1 , wherein the hydrophilic silicone copolyol further comprises polyoxyethylene (EO) groups, partial or complete substitution of EO with polyoxypropylene (PO), varying degree of modification of grafted polymers, or a mixture thereof. 
     
     
         3 . The silicone gel composition of  claim 1 , wherein said hydrophilic silicone copolyol is present in a concentration range from about 0.1 to about 4.0 weight percent. 
     
     
         4 . The silicone gel composition of  claim 1 , wherein the lipophilic silicone copolyol further comprises alkyl chains compatible with hydrocarbon oils, or a mixture thereof. 
     
     
         5 . The silicone gel composition of  claim 1 , wherein said lipophilic silicone copolyol is present in a concentration range from about 0.1 to about 4.0 weight percent. 
     
     
         6 . The silicone gel composition of  claim 1 , wherein the non-ionic oil-in-water (O/W) emulsifier agent further comprises a polyethoxylated emulsifier, a polypropoxylated emulsifier, or a mixture thereof. 
     
     
         7 . The silicone gel composition of  claim 1 , wherein said non-ionic oil-in-water (O/W) emulsifier agent is present in a concentration range from about 1.0 to about 20.0 weight percent. 
     
     
         8 . The silicone gel composition of  claim 1 , wherein the non-ionic water-in-oil (W/O) emulsifier agent further comprises an ester of an alkanecarboxylic acid emulsifier, or a mixture thereof. 
     
     
         9 . The silicone gel composition of  claim 1 , wherein said non-ionic water-in-oil (W/O) emulsifier agent is present in a concentration range from about 1.0 to about 20.0 weight percent. 
     
     
         10 . The silicone gel composition of  claim 1 , wherein the inorganic hydrocolloid further comprises a bentonite, a hectorite, a hydrotalcite, or a mixture thereof. 
     
     
         11 . The silicone gel composition of  claim 1 , wherein said inorganic hydrocolloid is present in a concentration range from about 0.1 to about 4.0 weight percent. 
     
     
         12 . The silicone gel composition of  claim 1 , wherein the organic hydrocolloid further comprises a gum, a polymer, a starch, or a mixture thereof. 
     
     
         13 . The silicone gel composition of  claim 1 , wherein said organic hydrocolloid is present in a concentration range from about 0.1 to about 4.0 weight percent. 
     
     
         14 . The silicone gel composition of  claim 1 , wherein the biocompatible surfactant with phosphatidylcholine comprises a naturally occurring unsaturated lecithin. 
     
     
         15 . The silicone gel composition of  claim 1 , wherein said biocompatible surfactant with phosphatidylcholine is present in a concentration range from about 0.1 to about 5.0 weight percent. 
     
     
         16 . A method for producing a transdermal delivery system for therapeutic agents comprising:
 dissolving active therapeutic agents in the silicone gel composition of  claim 1 .   
     
     
         17 . A method of dissolving an active drug into the silicone gel composition of  claim 1  comprising:
 using an electronic pestle and mortar to mix the active drug into the silicone gel composition. 
 
     
     
         18 . A silicone gel composition prepared by the method comprising:
 mixing a non-ionic oil-in-water (O/W) emulsifier agent comprising a blend of cetearyl alcohol and ceteareth-20 with a non-polar solvent to produce an oil phase;   mixing an inorganic hydrocolloid comprising magnesium aluminum silicate with water to produce an inorganic hydrocolloid phase;   mixing an organic hydrocolloid comprising hydroxypropyl starch phosphate with a poloxamer emulsifier and with a non-ionic water-in-oil (W/O) emulsifier comprising a copolymer of hydroxyethyl acrylate and sodium acryloyldimethyl taurate and with water to produce an organic hydrocolloid phase;   mixing one or more lipophilic silicone copolyols comprising phenyl trimethicone and C30-45 dimethicone to produce a silicone emulsifier phase;   mixing the inorganic hydrocolloid phase with the organic hydrocolloid phase to produce a hydrocolloid phase;   mixing the hydrocolloid phase with the oil phase to produce a hydrocolloid oil phase;   mixing the silicone emulsifier phase with the hydrocolloid oil phase to produce an emulsified phase;   adding a biocompatible surfactant comprising lecithin to the emulsified phase and mixing to produce a surfactant emulsified phase; and   adding one or more antimicrobial agents, one or more moisturizers, and silicone to the surfactant emulsified phase and mixing to produce the silicone gel composition.