Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
1999-04-12
2001-09-04
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C514S183000, C514S450000, C514S212010, C514S634000, C514S656000
Reexamination Certificate
active
06284797
ABSTRACT:
This invention comprises a topical preparation used to reduce pain and promote healing of the skin and tissues adjacent the skin.
BACKGROUND OF THE INVENTION
Capsaicin creams, ointments, gels or lotions are well known in the art. Capsaicin is the pungent extract of peppers or chiles and, chemically, is trans-8-methyl-N-vanillyl-6-nonenamide. Capsaicin is believed to act on a subset of primary afferent nerves mostly of the c-fiber type. It binds to a receptor site at the nerve ending and therefore interferes with the binding of substance P. There are believed to be two phases of action, first excitation and then desensitization of the nerve to nociceptive impulses. The excitation results in the shot of hot peppers or a burning/tingling sensation when applied to the skin. The desensitization results from depletion of substance P and interference with afferent transmission in a nontetrodotoxin dependent manner. Clinically, the overall effect is pain relief.
Capsaicin can be readily obtained by the ethanol extraction of the fruit of capsicum frutescens or capsicum annum. It is available commercially from a variety of suppliers and can also be prepared synthetically by published methods. In some commercially available forms of capsaicin, a slightly different composition known as pseudocapsaicin is present. This pseudocapsaicin is pharmacologically indistinguishable from natural capsaicin. The present invention encompasses the use of both forms, and where the term capsaicin is used, both forms are meant.
Disclosures of capsaicin creams, ointments and gels and their operating mechanisms are disclosed in U.S. Pat. Nos. 4,997,853; 5,063,060; 5,178,879; 5,296,225 and 5,665,378.
SUMMARY OF THE INVENTION
In this invention, a capsaicin preparation is provided which not only reduces pain but which also promotes healing of the skin and tissue adjacent the skin. This is accomplished by combining capsaicin with a norepinephrine inhibitor. Capsaicin is a known pain reliever but has no direct healing properties, i.e. any healing that occurs does so naturally without assistance by the capsaicin.
Without being bound by any particular theory, it appears that many of the successes of this invention can be explained by normalizing production and/or circulation of norepinephrine. Norepinephrine is a longer lasting version of epinephrine and assists in transmitting nerve impulses and in constricting blood vessels. Overproduction of norepinephrine causes constriction of superficial small to medium arteries and arterioles which results in trophic skin changes, demyelination of nerves and hyperesthesia. Reducing the production and/or distribution or norephinephrine results in increased superficial arterial blood flow. This increase in superficial arterial blood flow actibely assists healing those tissues adjacent the skin where the preparation is applied.
Another important component of this invention is a vasodilator. The vasodilators actively promote dilation of the blood vessels in the area where the preparation of this invention is applied. Thus, inhibition of norepinephrine in the area of treatment and the application of vasodilators both act to increase blood flow and promote healing in the treatment area.
Another important component of the preparation of this invention is a pain killer, ant-inflamminant or analgesic. Capsaicin preparations are typically irritating to the skin in the treatment area. The inclusion of a pain killer, anti-inflamminant or analgesic reduces discomfort due to the capsaicin.
A further important component of this invention is a substance that promote transcutaneous absorption. Skin has the property of preventing or reducing absorption of most materials so it is preferred in this invention to incorporate a promoter of transcutaneous absorption.
It is accordingly an object of this invention to provide an improved capsaicin preparation which reduces pain and promotes healing of tissue adjacent the skin.
Another object of this invention is to provide an improved capsaicin preparation incorporating a norepinephrine inhibitor.
A further object of this invention is to provide an improved topical preparation containing capsaicin, a norepinephrine and a vasodilator.
These and other objects and advantages of this description will become more apparent as this description proceeds, reference being made to the appended claims.
DETAILED DESCRIPTION
In this invention, a capsaicin preparation includes capsaicin,, a norepinephrine inhibitor and a therapeutically acceptable carrier. Capsaicin is employed in an effective amount, between 0.001% and 5% by weight and preferably between 0.01% and 1.0% by weight, and may be either an extract of chiles or peppers or may be synthetically manufactured.
The norepinephrine inhibitor is a psychotropic drug that interferes with release of norepinephrine, reduces the transmission or dissemination of norepinephrine or deactivates norepinephrine at the synapses. Typical norepinephrine inhibitors used in this invention are selected from a group of tricyclic antidepressants and specifically are amitriptyline, nortriptyline and doxepin. Another suitable norepinephrine inhibitor is an antipsychotic drug fluphenazine or prolixin which interferes with norepinephrine. There are a number of hypertensive medicines that reduce blood pressure by altering the effect of norepinephrine and are accordingly suitable for use in this invention. Specifically, guanidine and guanethidine alter the effects of norepinephrine and are operative in this invention.
The norepinephrine inhibitors of this invention are used in an effective amount, i.e. they are used in an amount that increases blood flow in the treatment area. In this invention, the norepinephrine inhibitors are present in 0.5-50% by weight and preferably are present on the order of about 10-20%, optimally about 15%.
The carrier may be of any suitable type and typically is selected from the group consisting of lotions, gels, ointments or creams such as are commonly used in topical preparations. A convenient manner of compounding this invention is to start with a commercially available capsaicin cream, such as CAPSAICIN TOPICAL ANALGESIC CREAM, available from Breckenridge Pharmaceutical, Inc. of Boca Raton, Fla. and add the other active ingredients. This commercial preparation has 0.025% capsaicin in a standard cream and the cream is sufficient to suspend the remaining active ingredients of this invention. The carrier is present in an effective amount, usually 1-80% by weight and also acts as a diluent.
Another important class of compounds present in preferred compositions of this invention are cardiovascular drugs that actively promote blood circulation in the treatment area by one or more mechanisms. One important group of such compounds are vasodilators that dilate small blood vessels in the treatment area. Typical vasodilators used with this invention are reserpine, nitroglycerin and hydralazine. These vasodilators are used in an effective amount, i.e. they are used in an amount that increases blood flow in the treatment area. In this invention, the vasodilators are present in 0.5-50% by weight and preferably are present on the order of about 10-20%, optimally about 15%.
Another important class of compounds present in this invention is a pain killer to offset the irritation caused by the capsaicin. The pain killer may be an anti-inflamminant and/or analgesic such as hydrocortisone cream, a non-steroidal anti-inflamminant such as ibuprofen, aspirin or other salicylates, or other pain killers such as diflunisal, fenoprofen, indomethacin, meclofenamate, naproxen, oxyphenbutazone, phenylbutazone, piroxicam, sulindac, tolmetin, zomepirac, idocaine, benzocaine, or lidocaine.
The pain killers of this invention are used in an effective amount, i.e. they are used in an amount that substantially reduces the topical irritation caused by the capsaicin. In this invention, the pain killers are present in 1-50% by weight, and preferably are present on the order of about 10-20%, optimally about 15%.
Another important class of compou
Howard S.
Moller G Turner
Page Thurman K.
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