Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from capsicum
Reexamination Certificate
2000-03-16
2004-02-10
Venkat, Jyothsna (Department: 1615)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from capsicum
C514S054000, C514S625000, C514S627000, C514S629000
Reexamination Certificate
active
06689399
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to an anti-inflammatory composition for treatment of joint and muscle pain. More specifically, the present invention provides a composition that alleviates pain associated with joint and/or muscle injuries, diseases or conditions through transdermal delivery of a casaicinoid in conjunction with a primary amine, such a glucosamine. The combination of the ingredients of the present invention, namely a capsaicinoid and a primary amine, interact in a synergistic manner to provide unexpectedly beneficial results in relief of joint and/or muscle pain associated with an inflammatory response.
BACKGROUND OF THE INVENTION
The connective tissue of mammals, such as humans, are subjected to a constant barrage of stresses and injuries throughout the life of the individual. These stresses may result from acute or chronic impacts or from the progress of various degenerative diseases, and produce painful inflammation in joint regions, such as the neck, back, arms, hips, ankles and feet. These afflictions are common, afflicting millions of Americans, and in many cases, debilitating. As a result, there is a great need for an effective and simple treatment to ease the pain associated with inflammatory connective tissue conditions.
There are a number of approaches directed to controlling the symptoms of such inflammatory connective tissue conditions. Steroids, especially corticosteroids, and non-steroidal anti-inflammatory drugs (so-called “NSAIDs”), such as aspirin (acetylsalicylic acid), ibuprofen ((2-(isobutylphenyl) propionic acid), naproxen (2-naphthaleneacetic acid, 6-methoxy-9-methyl, sodium salt), and piroxicam (4-hydroxy-2-methyl-N-2-pyridinyl-2H-1,2-benzothiazine-2-carboxamide 1,1 dioxide), are used to control the inflammation associated with connective tissue disorders. However, these drugs relieve the symptoms associated with the connective tissue disorders, but do nothing to slow the progression of the disease. Furthermore, these drugs have a number of undesirable side-effects. With respect to NSAIDS, first, NSAIDS may inhibit the body's own natural healing mechanisms, leading to further connective tissue degeneration. Second, NSAIDS also affect enzymes involved in maintaining healthy liver and kidney function, so that administration of these drugs weakens these organ systems. Finally, NSAIDS can produce gastropathy and gastric ulceration. With respect to corticosteroids, while dramatic improvements are often seen upon initial administration, corticosteroids begin to lose their effectiveness after prolonged administration. Further increases in dosage are required to overcome the loss of effectiveness, but the higher dosages themselves also eventually lose effectiveness. Furthermore, upon cessation of corticosteroid treatment, the symptoms of inflammation and swelling recur at higher levels than were experienced prior to administration. In addition, fluid retention is a serious side effect, and can lead to significant weight gain and, more importantly, dangerous levels of hypertension. Corticosteroids may also induce or contribute to osteoporosis, exacerbating what is often already a significant problem with elderly patients.
The connective tissues of mammals are capable of being regenerated by chondrocytes, cells that are responsible for the synthesis of the major components of connective tissues—collagen and proteoglycans. Collagen is a fibrous glycoprotein that is found in skin, bone, tendon, cartilage, blood vessels, and teeth. Collagen is also found in all organs, and serves as a scaffold to hold cells together. The building blocks for collagen are amino acids, and in particular the amino acids glycine, proline, hydroxyproline and hydroxylysine. Carbohydrate units are attached to collagen fibers at the hydroxylysine residues.
Proteoglycans are large, complex molecules that form the ground substance of connective tissue and determine the viscoelastic properties of joints and other structures that are subject to mechanical deformation. Proteoglycans are made up of a hyaluronic acid backbone to which are attached, at regular intervals, a core protein bearing a number of different types of modified sugars, called glycosaminoglycans. Examples of glycosaminoglycans are keratin sulfate, chondroitin sulfate, heparin, and heparin sulfate. The most important molecule in the synthesis of proteoglycans is glucosamine. Glucosamine is the precursor to the glycosaminoglycans. In addition, glucosamine forms hyaluronic acid, the backbone of proteoglycans to which the long chains of the various types of sugars are joined. Glucosamine is also a key component of synovial fluid, the liquid in joints, which provides lubrication and nutrition to cartilage.
The effects of aging and the inevitable wear and tear of daily life on structural joints mean that the structural elements of connective tissue must constantly be replaced. The rate-limiting step in the synthesis of proteoglycans is the conversion of glucose to glucosamine in the production of glycosaminoglycans. Therefore, it has been proposed to stimulate the production of proteoglycans by providing various forms of the building blocks of these complex molecules. Glucosamine administration appears to reduce the likelihood of tendon and ligament damage, as well as reducing joint inflammation, and has been shown by numerous double blind clinical trials to be both safe and effective. Administration of glucosamine appears to overcome the rate-limiting step described above by a mass action effect. U.S. Pat. No. 3,683,076, issued to Rovati et al., discloses methods for the preparation of glucosamine sulphate and glucosamine hydroiodide, useful in the treatment of degenerative joint conditions. Because these compounds oxidize readily, the compositions also preferably include a reducing agent, such as sodium hyposulfite or N-acetyl diethanolamine. U.S. Pat. No. 3,697,652, also to Rovati et al., discloses pharmaceutical preparations to treat degenerative joint conditions. Compositions contain one or more N-acyl aminocarbohydrates, preferably glucosamines and/or galactosamines. Preferably, one or more inorganic salts of alkaline earth and/or alkali metals are included (e.g., sodium sulfate, sodium iodide, etc.). U.S. Pat. No. 5,364,845, issued to Henderson, describes a therapeutic composition for the treatment and protection of connective tissue which includes glucosamine and preferably chondroitin sulfate and manganese ascorbate. U.S. Pat. No. 5,916,565, issued to Rose et al., discloses a therapeutic composition for treatment of damaged joint tissues that comprises chondroitin sulfate and glucosamine, along with multiple anti-inflammatory herbal phytochemicals, such as cayenne, which contains capsaicin.
Other components of the proteoglycans have also been provided to stimulate their production in the treatment of joint degeneration or promotion of wound healing. U.S. Pat. No. 4,801,619, issued to Lindblad, describes high molecular weight (>3×10
6
) hyaluronic acid preparations for counteracting progressive cartilage destruction. The hyaluronic acid preparations are preferably administered by intra-articular injection, and may be combined with administration of a corticosteroid or other suitable anti-inflammatory compound. U.S. Pat. No. 5,972,906, to Asculai et al., describes topically applied compositions and methods for treatment of mucous membrane disease or trauma, particularly oral mucous membrane conditions, that comprise hyaluronic acid or fragments and/or subunits thereof, along with an NSAID anti-inflammatory agent. The hyaluronic acid preparation may further include N-acetyl glucosamine or glucosamine.
Typically, glucosamine is administered by an oral route. However, oral administration of glucosamine is relatively ineffective, because the liver breaks down up to 80% of the orally administered glucosamine. Furthermore, while orally-administered glucosamine is relatively effective in reaching joint areas, many sites of pain and inflammation are poorly vascularized, and the blood-bor
Neuman, Esq. Kristin H.
Proskauer Rose LLP
Shalek, Esq. James H.
Venkat Jyothsna
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