Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2002-01-25
2003-06-03
Criares, Theodore J. (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
active
06573302
ABSTRACT:
BACKGROUND OF THE INVENTION
Arthritis is a common chronic problem, which occurs below the surface of the skin. Millions of people and animal have the condition. Various topical creams and ointments are sold for treatment of arthritis; however, most utilize an anesthetic, such as lidocane, benzocaine or other numbing agent for the skin surface.
The present invention was developed to provide a cream, which has as the three critical ingredients, capsaicin, plus an anesthetic and an analgesic. The composition overcomes other obstacles of known capsaicin creams in that the amounts used enable the warming relief of the peppers in combination with the coolness of the anesthetic, yet enable the user to still feel objects they touch due to the use of an analgesic as a critical component rather than large amounts of anesthetics.
Various capsaicin compositions have been developed over the years, in particular, the psoriatic composition of U.S. Pat. No. 4,486,450, the nasal composition of U.S. Pat. No. 5,134,166, and the composition of U.S. Pat. No. 4,997,853, the anti-inflammatory composition of U.S. Pat. No. 5,560,910, the composition of U.S. Pat. No. 5,962,532, the composition for animals of U.S. Pat. No. 5,916,565, the stomach treatments of U.S. Pat. No. 5,889,041, the composition of U.S. Pat. No. 5,827,886, the patch with medication of U.S. Pat. No. 5,741,510, all of which are incorporated by reference herein.
After many years of research and testing on subject, the present invention has been developed which does not rely on topical anesthetics, such as lidocaine (Entry 5310, p. 786 Merck Index, Tenth Edition 1983) and benzocaine (ethyl aminobenzoate, Entry 3710, p. 546 Merck Index, Tenth Edition, 1983) into formulations containing capsaicin, and then applying such formulations for the initial period of treatment to eliminate the painful burning from the application of capsaicin, allowing the patient to continue therapy while being able to feel through the skin onto which the cream is applied.
SUMMARY OF THE INVENTION
The present invention relates to a method of treating arthritis using a cream composition therefore in which capsaicin is used as the principle therapeutic agent along with an analgesic and an anesthetic in a cream.
An object of the present invention is to provide a cream, which is easily applied, easy to absorb into the skin, and provides ability to feel objects.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT
Capsaicin is trans-8-methyl-N-vanillyl-5 nonenamide, a naturally occurring alkyl vanillylamide and a type of capsaicinoid. It is found in high concentration in fruit of plants of the Capsicum genus. The chili pepper, red pepper and paprika are all species of Capsicum. All hot papers contain capsaicinoids. Capsaicinoids are natural materials, which produce a burning sensation in the mouth. Capsicum has recently been officially defined in the USP 23 where it is defined as the dried ripe fruit of
Capsicum frutescens
Linne or
Capsicum annum
Linne.
There are two main capsaicinoids, capsaicin and dihydrocapsaicin and three minor capsaicinoids, nordihydrocapsaicin, homocapsaicin and homodihydrocapsaicin. All capsaicinoids are considered usable within the scope of this invention.
Capsicum is the dry powder obtained by grinding up the fruits of these plants. Capsicum oleoresin (or capsaicin oleoresin) is the liquid concentrate extracted from the dry powder. Capsaicin, a white crystalline material, is obtained from the liquid concentrate.
The composition of the invention comprises capsaicin as a first active ingredient and at least one second active ingredient acting as an analgesic to reduce the sensation of capsaicin induced skin irritation. The ingredients are contained in a carrier fluid. The genus capsicum is a member of a large tropical family solanaceae. There are numerous species, of which
Capsicum annum, Capsicum chinense
and
Capsicum frutescens
are closely related.
Capsicum frutescens
is also known as Cayenne Pepper, Chili Pepper, Pimento Tabasco Pepper and Tabasco-sauce pepper.
Capsaicin (N-Vanillyl-8-methyl-6-(E)-noneamide) is the most pungent of the capsaicinoids. It is very soluble in fats, oils and alcohols. Capsicum also contains a red coloring matter, oleic acid, palmitic acid and stearic acid.
Capsicum frutescens
extract can be obtained from Bio-Botanica, Inc. of Hauppauge, N.Y. and appears as a viscous fluid, having a sallow yellow color, a caustic and pungent aroma, and is soluble in ethanol.
Capsicum is a powerful local stimulant. It is strongly rubifacient acting without vesication.
In the present invention, capsaicin is mixed with a carrier fluid. Preferably, the carrier fluid is water-based and forms an aqueous solution containing the ingredients. However, the carrier may be a fluid such as an oil based carrier, a fat based carrier, a fatty alcohol based carrier and combination of these.
Additional irritant is added to the capsaicin and carrier. Histidines, such as histamine dihydrochloride, are considered usable in the scope of the present invention to create vasodilatation, and act as a second irritant. Adding the second irritant produces an analgesic effect and does not numb the site, like an anesthetic or depress coetaneous sensory receptors. It is possible to add more than one histidine to achieve the analgesic reaction. Instead, it has a topical counterirritant effect by stimulating coetaneous sensory receptors, see, Federal Register, Vol. 48, No. 27, Tuesday Feb. 8, 1983, pages 5367 et. seq. Local anesthetics, such as benzocaine and lidocaine, act differently as anesthetics not producing an analgesic effect which is achieved by adding an additional irritant, such as a histamine hydrochloride or most preferably a histamine dihydrochloride. If a histamine dihydrochloride is used, it is preferred to use a starting composition of 98% histamine, although compositions in the range of 96-99% histamine will be usable as well.
Generally speaking, the cream will contain in the range of 0.00125% to 1% by weight of capsaicin. Compositions containing more than 1% by weight of capsaicin will provide a therapeutic effect, with up to 62% by weight capsaicin, except that the burning side effect will increase in proportion to the increase percentage of capsaicin. Compositions containing 0.025% to 20% by weight of capsaicin could be used. Compositions of 0.025 to 2% by weight are considered usable as well. Compositions containing in the range of 0.025% to 0.25% by weight of capsaicin are preferred because they are narrowly encompassed within current FDA guidelines regarding capsaicin use. However, the FDA guidelines were developed at a time when there was not an effective method for relieving the discomfort generated by capsaicin. The present invention provides a method to increase the amount of capsaicin that can be administered comfortably.
In the present invention, capsaicin is mixed with a carrier fluid to formulation. Preferably, the carrier is water-based and forms a cream containing ingredients that quickly soak into the skin, providing fast transdermal absorption. However, the carrier may be a fluid such as an oil-based carrier, a fat based carrier, a fatty alcohol based carrier or combination of these, or an omega-6 fatty acid.
The novel cream uses an encapsulation agent, colloidal oatmeal, or hydrogenated lecithin, dipotassium glycyrrhizinate or a similar encapsulation agent, or even combinations of these agents, to be effective. The colloidal oatmeal has intrinsic SFP, natural sunscreen capability. In addition, the colloidal oatmeal encapsulates the capsaicin to reduce the inflammation effect the capsaicin has on the skin, while still enabling the capsaicin to work effectively. Typically, up to 3-wt. % colloidal oatmeal is used in this invention, although any amount of about between 2 wt. % and up to about 10-wt. % can be used. The colloidal oatmeal works within the scope of this invention because it contains hydrophilic colloids. These colloids help to provide a protective barrier on the skin to control inflammation. In addition, histid
Barr Teresa Leigh
Holt Stephen D.
Buskop Wendy
Buskop Law Group P.C.
Criares Theodore J.
Kim Jennifer
Medical Merchandising Inc.
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