United States Patent:  6,083,190

Assignee:  ALZA Corporation (Mountain View, CA)

Filed:  December 14, 1998

An electrotransport composition comprises at least one C₂ -C₄ lower alcohol, unsaturated derivatives thereof, or mixtures thereof, and at least one C₈ -C₄ higher alcohol, unsaturated derivatives thereof, or mixtures thereof. An electrotransport device and a method of increasing transdermal electrotransport flux utilize the composition of the invention for delivering pharmaceutically-acceptable agents across a body surface such as skin.

DISCLOSURE OF THE INVENTION

This invention arose from a desire to improve on prior art technology in the field of transdermal electrotransport delivery. This invention provides a composition that enhances the electrotransport flux of a drug or prodrug through a body surface such as skin. The permeation enhancing composition comprises in combination (1) at least one lower alcohol and (2) at least one higher alcohol, both of which may be linear branched, aromatic, and/or cyclic The lower alcohol is preferably a C₂ -C₄ alkanol or unsaturated derivatives thereof, and more preferably ethanol. The higher alcohol is preferably a C₈ -C₁₄ alkanol or unsaturated derivatives thereof, more preferably a C₁₀ -C₁₂ alkanol or unsaturated derivatives thereof. Of these higher alcohols, dodecanol and 1-dodecanol are most preferred.

The composition of the invention reduces the electrical resistance of body surfaces, such as the skin, mucosa, and nails, during electrotransport agent delivery, and permits a reduction in the size of the delivery device and/or the power (ie, voltage) required to maintain a particular level of electrotransport current and rate of electrotransport agent delivery.

The present composition is suitable for use in reducing the electrical resistance of the body surface (eg, skin) site adjacent the donor electrode of an electrotransport delivery device, the skin site adjacent the counter electrode of the device, or both body surface sites. The permeation enhancer composition may be applied to the body surface prior to or during agent delivery, but the composition is preferably placed in the donor and/or counter reservoir of an electrotransport delivery device and is delivered to the body surface simultaneously with the agent.

Also provided herein is an electrotransport delivery device comprising donor and counter electrodes, at least one of the electrodes having a reservoir comprising the lower/higher alcohol composition, an electrical power source which is electrically connected to the donor and counter electrodes, and optionally electronic control circuitry.

The composition of the present invention may be used with different electrotransport devices for the delivery of a variety of pharmaceutically acceptable agents, including those specifically disclosed herein. One particular application for which the composition is most suitable is the electrotransport delivery of amine and amino acid containing agents.

Claim 1 of 7 Claims

1. An electrotransport delivery device comprising donor and counter electrodes electrically connected to a power source; at least one of the electrodes having a reservoir containing a composition comprising:

an agent in a form suitable for electrotransport delivery;

about 0.01 to 100 mM of at least one C₈ -C₁₄ linear branched, cyclic, or aromatic alcohol or unsaturated derivatives thereof or mixtures thereof; and

about 0.5 to 30% (v/v) of at least one C₂ -C₄ alcohol or unsaturated derivatives thereof, or mixtures thereof.

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