Topical dermal anaesthetic

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice

Reexamination Certificate

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Details

C424S078020

Reexamination Certificate

active

06416772

ABSTRACT:

BACKGROUND
1. The Field of the Invention
The present invention relates to analgesics. Specifically, the present invention relates to an anagesic solution or liquid composition which is applied topically to the surface of the skin, or transdermally, for treatment of pain and irritation.
2. The Relevant Technology
The use of aspirin and other analgesic, anti-inflammatory agents is well known and has proven to be very valuable in the medical and scientific community. Aspirin has shown to have a variety of benefits in the treatment of aches and pains such as muscular aches, strains and cramps, arthritis, joint pain, lower back discomfort, bursitis, rheumatism, bums, insect bites and sports injuries.
However, certain side effects of aspirin, such as stomach irritation, may cause individuals to discontinue the use of this useful pain killer and anti-inflammatory. The ability to apply aspirin to an area of discomfort without ingesting the aspirin is a need which has been long felt within the medical community.
In addition, the ability to apply non-aspirin analgesics in an effective transdermal manner is a long-felt need. Applying an analgesic transdermally allows one to focus the analgesic in a certain painful area without diluting it by routing it through the blood stream.
A variety of difficulties, however, are associated with the goal of achieving a safe and stable form of transdermal analgesic. First, it is vital that the analgesic permeate the necessary layers of skin in order to anesthetize pain without adversely affecting vital internal organs. Thus, it is critical to provide a solution which dissolves aspirin or other analgesic agents and transports it topically to the area of pain where it can then permeate the skin to provide effective relief. While some topical analgesics have been introduced, they are largely limited in their ability to efficiently and effectively permeate the necessary layers of skin to provide for fast relief of the experienced pain.
Second, topical analgesics have been known to take effect long after they have been applied. Once the solution is applied to the skin, it usually takes quite some time for the analgesic to react and begin working. This may be caused by several reasons, such as the fact that the analgesic may not permeate the skin very well, the analgesic may need time itself to begin providing its pain relieving effects, etc.
Third, while certain solutions effectively cause the analgesic agents to permeate the skin, it is critical that the analgesic agent be stable within the solution such that it has a marketable shelf life. Aspirin is sparingly soluble in water. Permeating solutions may degrade aspirin and other analgesics by a variety of scientific processes including hydrolysis, glycolysis, and transesterification, for example. Until the present invention, teachings in the art indicated that aspirin was not stable in topical solutions involving the lower aliphatic alcohols because it too readily hydrolyzed to acidic and salicylic acids.
It would therefore be a significant advance in the art to discover and employ a composition having the ability to safely permeate skin at a more rapid rate. It would also be a significant advantage to provide a topical analgesic that is able to facilitate and speed up the pain relieving effects of the analgesic agent. Finally, it would also be a significant advantage to provide a topical analgesic that maintains a shelf stable state.
SUMMARY AND OBJECTS OF THE INVENTION
It is an object of the present invention to provide a topical analgesic having a composition that potentiates the analgesic, thus having a catalytic effect on the analgesic to speed and enhance pain relieving characteristics of composition.
It is another object of the present invention to provide a topical analgesic that relieves pain and does not dry the skin.
It is another object of the present invention to provide a composition which exists in a liquid state and is applied transdermally for relief of pain which contains an analgesic, anti-inflammatory agent which is shelf stable.
It is still another object of the invention to provide a composition containing absorption enhancing elements which allow the composition to permeate the necessary layers of the skin in order to address the aches and pains to be relieved, but does not enter the blood stream thus adversely affecting the internal organs.
It is a further object of the invention to provide such a solution which can be applied directly in the area of pain on the body.
It is still further an object of the invention to provide such a solution in a form which does not need to be shaken or stirred before use.
To achieve the foregoing objects, and in accordance with the invention as embodied and broadly described herein, the present invention features a liquid composition applied transdermally for relief of pain comprising: alcohol in an amount by weight of about 57 to about 91 percent; glycerin in an amount by weight of about 1 to about 12 percent; an analgesic agent in an amount by weight of about 2 to about 28 percent, the analgesic agent comprising a derivative of salicylic acid; methylsulfonylmethane in an amount by weight of about 0.02 to 5 percent; and emu oil in an amount by weight of about 0.01 to 3 percent, the liquid composition permeating skin to relieve pain. The liquid composition further comprises, as an option, aloe vera in an amount by weight of at least about 0.05 percent and being present in an amount by weight of about 0.05 to 4 percent, and in a preferred embodiment being present in an amount by weight of 0.125 percent.
In addition, and also as an optional element, allantoin may be used. Allantoin is a great potentiator and a good analgesic in its own right. The range of allantoin should be 0.04 to 2.00 percent by weight.
In a preferred embodiment, the analgesic agent consists of acetylsalicylic acid, triethanolamine, triethanolamine salicylate, acetaminiphen, (4-isobutylphenyl) propionic acid, naprosyn, and/or a salicylate. These may be used separately, or in conjunction with one another depending on the type of pain and desired relief. Also in a preferred embodiment, the alcohol consists of either isopropyl alcohol or ethyl alcohol.
In a preferred embodiment using triethanolamine or triethanolamine salicylate as the analgesic agent, the specific composition of the liquid formula is: alcohol present in an amount by weight of 81.7 percent; glycerin present in an amount by weight of about 3.12 percent; an analgesic agent present in an amount by weight of about 15 percent; aloe vera present in an amount by weight of 0.125 percent; methylsulfonylmethane present in an amount by weight of 0.04 percent; and emu oil present in an amount by weight of 0.015 percent. The use of aloe vera is optional, but preferred. If desired it may be removed, thereby increasing the percent by weight of one of the other elements in the composition.
In another preferred embodiment using acetylsalicylic acid, acetaminiphen, naprosyn, (4-isobutylphenyl) propionic acid, or a salicylate such as methyl salicylate as the analgesic agent, alcohol is present in an amount by weight of 88.78 percent; glycerin is present in an amount by weight of about 4.87 percent; analgesic agent is present in an amount by weight of about 6 percent; aloe vera is present in an amount by weight of 0.2 percent; methylsulfonylmethane (MSM) is present in an amount by weight of 0.08 percent; and emu oil is present in an amount by weight of 0.07 percent. Again, the use of aloe is optional, but preferred and may be removed if desired.
The present invention further features a liquid composition applied transdermally for relief of pain comprising alcohol, glycerin, an analgesic agent, and either or both of methylsulfonylmethane and emu oil, each being present in a percent by weight.
Finally, the present invention features a method for relieving pain, the method comprising: applying a liquid composition to the skin surrounding an area of said pain wherein the liquid composition comprises alcohol in an amount by weight of about

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