Transdermal compositions

Abstract

The present invention is directed to transdermal compositions and the uses thereof. These compositions include at least one of the following components: a C1-C6 dialkyl, C12-C30 dialkyl quaternary ammonium salt, a C12-C30 fatty acid, a nitrogenous organic base, C12-30 fatty alcohol, monoglyceride or the reaction products thereof.

Description

[0001] The present application claims priority of provisional application U.S. Serial No. 60 / 412,437, filed on Sep. 20, 2002.BACKGROUND OF THE DISCLOSURE[0002] 1. Field of the Invention[0003] The present invention is directed to compositions useful as a carrier for transdermal compositions. These compositions are also useful, in combination with active agents, in the treatment of skin diseases, skin injuries, chronic skin conditions and the like. The transdermal compositions of the present invention are directed to products formed by the reaction of combinations of a quaternary ammonium salt, a fatty acid, a fatty alcohol, a nitrogenous base and a monoglyceride.[0004] 2. Background of the Prior Art[0005] The design of a composition which, when applied in combination with an active agent, to treat various skin diseases, skin injuries, chronic skin conditions and the like is complex due to the necessity of insuring delivery of the active agent to the proper place on or below skin, pro...

AI Technical Summary

Problems solved by technology

The design of a composition which, when applied in combination with an active agent, to treat various skin diseases, skin injuries, chronic skin conditions and the like is complex due to the necessity of insuring delivery of the active agent to the proper place on or below skin, providing proper permeation into the skin and providing the desired physical separation, if any, of the composition from the skin surface.

The above remarks establish the difficulty of designing compositions for transdermal use which meet all of the above requirements of an efficient transdermal composition.

However, the problem is multiplied when it is appreciated that the cost of preparing a wide range of effective compositions which meet all of these requirements for all skin conditions is quite imposing.

Thus, a composition which meets all of the requirements mentioned above in the case of a burnt skin may not be effective to meet all of the requirements when a skin irritation is to be treated.

Thus, the costs of providing a wide range of compositions suitable for transdermal compositions is imposing.

Insect bites cause itching, inflammation and irritation of the skin.

The problems associated with antiseptic compositions of the prior art are that they include aggressive detergents and microphobes which are so irritating to the skin that they can make affected portions of the rough skin chapped and / or irritated.

Without wishing to be bound, it believed that chronic wounds are typically nutrient poor and circulatory poor sites.

Excessive stimulation causes pain as blood rushes back into little used capillaries.

However, pain may be felt from this enhanced stimulation.

It is to be noted that the amide hydrate forms an emulsion as it cools and may even form a gel, a cracked crust which is unappealing to view.

These degreasing surfactants are irritating and sticky on the skin.

The wax film has an unpleasant hand feel because the coefficient of friction is so high.

Premixes of unsaturated fats are somewhat different than premixes of saturated fats because the unsaturated fats are liquid at room temperature and are harder to make phase stable.

If the gel is too strong, this iterative process is interrupted and conversion to the tertiary amide is low.

Absolute Concentration--If the concentration of the reactants is too high, there is not enough free water to circulate the mix without shear.

Low levels of TEA tend to thin the mixture and break the gel.

Such bruising is common in humans of advanced age who are often bruised over much of their bodies, especially their outer extremities.

That is, infants, as well as the elderly, are subject to the skin problem defined as diaper rash.

Although diapers absorb much of the moisture and bodily discharge, still skin in areas protected by diapers are chronically wet resulting in the formation of rashes and, serious skin infections.

This pressure manifests itself in the development of sores which grow progressively more serious as manifested by increasing red color culminating in their more serious manifestation of the breaking open of the skin.

Obviously, this is counterproductive in cuts which may open and bleed, in skin ulcers which may cause pain as capillaries suddenly are expanded by increased blood supply and burns in which nutrients are transported past the damaged burn surface site.

The combination of the first reaction product and the monoglyceride tend to heal wounds and do not enhance transmission of nutrients from the skin surface.

These antimicrobial compounds are beneficial on the surface of the skin, but may be detrimental if in the blood stream.

Such a combination would tend to slow the rate of absorption.

Benzethonium chloride is a reactive material that is unstable in an acid environment; it reacts with fatty acids and soaps and thus is unstable.

Thus, if added to the transdermal compositions of the present invention which is then processed into a microsphere, it would be expected that the compositions would be unstable.

On the other hand, it is not stable if added at temperatures below the Freezing Zone and above ambient temperature at a pH of about 7.5 to about 8.

However, when the quaternary ammonium salt, e.g., DDAC, is not substantially converted to the first reaction product, some of the patients, approximately 25% thereof, feel pain.

Maintaining skin health is always complex, particularly with hands that are exposed to harsh chemicals.

Treatment with antiseptic products tends to cause cracking and chaffing of hands (contact dermatitis).

It is difficult to kill these hidden microorganisms because the antiseptic fluids cannot get into the cracks and crevices during the sanitizing process.

These hands are often cracked and chapped.

The antiseptic nature of the hands is typically not critical, but cracked and chapped hands hurt.

It is difficult to make a skin care product that is simultaneously absorbing and not absorbing.

This solution can make the hands feel better, but the secondary treatment of either sanitizing or providing a barrier is compromised because the moisturizing ingredients in the first application remain on the surface of the skin.

The surface oils cover and protect the microorganisms, such that the expected sanitizing is compromised.

Images