Transdermal delivery systems for active agents

Abstract

A formulation for transdermal or transmucosal administration of an active agent. The formulation includes an active agent and a delivery vehicle comprising a C 2 to C 4 alkanol, a polyalcohol, and a permeation enhancer of monoalkyl ether of diethylene glycol present in an amount sufficient to provide permeation enhancement of the active agent through dermal or mucosal surfaces. The formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters in order to avoid undesirable odor and irritation effects caused by such compounds during use of the formulation. Also, the active agent is testosterone that is present in an amount of about 1%, the alkanol is ethanol that is present in an amount of about 46.28% to about 47.5% of the formulation; the polyalcohol is propylene glycol that is present in an amount of about 6% of the formulation; and the permeation enhancer is diethylene glycol monoethyl ether that is present in an amount of about 5% of the formulation.

1 . A gel formulation for transdermal or transmucosal administration of an active agent, the formulation comprising: an active agent; a gelling agent of a carbomer present in an amount of about 1.2% of the formulation; and a delivery vehicle comprising a C 2  to C 4  alkanol, a polyalcohol, and a permeation enhancer of monoalkyl ether of diethylene glycol present in an amount sufficient to provide permeation enhancement of the active agent through dermal or mucosal surfaces; wherein the formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters in order to avoid undesirable odor and irritation effects caused by such compounds during use of the formulation, wherein the active agent is testosterone that is present in an amount of about 1%, the wherein the alkanol is ethanol present in an amount of about 46.28% to about 47.5% of the formulation; the polyalcohol is propylene glycol that is present in an amount of about 6% of the formulation; and the permeation enhancer is diethylene glycol monoethyl ether that is present in an amount of about 5% of the formulation. 
     
     
         2 . The formulation of  claim 1 , further comprising at least one excipient selected from the group consisting of antimicrobials, preservatives, antioxidants, buffers, humectants, sequestering agents, moisturizers, emollients, or film-forming agents. 
     
     
         3 . The formulation of  claim 1 , further comprising a neutralizing agent of triethanolamine present in an amount of about 0.4% of the formulation, disodium EDTA present in an amount of about 0.06%, and water. 
     
     
         4 . A method for administering testosterone to a mammal in need thereof which comprises topically or transdermally administering to the skin or the mucosa of the mammal a formulation according to  claim 1 . 
     
     
         5 . The method of  claim 4 , wherein between about 40 and about 250 mg of the formulation is administered daily upon the abdomen, shoulder, arm, or thigh of the mammal.