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(12) Patent Application Publication (10) Pub. No.: US 2006/0194759 A1 Eidelson (43) Pub

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(12) Patent Application Publication (10) Pub. No.: US 2006/0194759 A1 Eidelson (43) Pub US 2006O194759A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0194759 A1 Eidelson (43) Pub. Date: Aug. 31, 2006 (54) TOPICAL COMPOSITIONS AND METHODS Publication Classification FOR TREATING PAN AND NFLAMMATION (51) Int. Cl. A 6LX 3L/737 (2006.01) (76) Inventor: Stewart G. Eidelson, Boca Raton, FL A6II 3L/728 (2006.01) (US) A 6LX 3/573 (2006.01) A6II 3L/045 (2006.01) A61K 3 1/7008 (2006.01) Correspondence Address: (52) U.S. Cl. ............................ 514/54: 514/171; 514/729; Raymond P. Niro 514/62 Niro, Scavone, Haller & Niro Suite 4600 (57) ABSTRACT 181 W. Madison A topical composition and method for treating pain and Chicago, IL 60602 (US) inflammation by administering an effective amount of a topical composition comprising an anti-inflammatory Ste roid such as hydrocortisone, a topical anesthetic Such as (21) Appl. No.: 11/066,863 lidocaine, menthol, and a medically acceptable carrier into which the forgoing are incorporated. A chondroprotective (22) Filed: Feb. 25, 2005 agent can also be added. US 2006/0194759 A1 Aug. 31, 2006 TOPCAL COMPOSITIONS AND METHODS FOR as lidocaine, and the steroidal anti-inflammatory drug Such TREATING PAN AND INFLAMMATION as hydrocortisone are each preferably in amounts from about 1% to about 4% of the composition by weight. The active BACKGROUND OF THE INVENTION ingredients of the invention at Such concentration ranges will relieve pain and inflammation in an enhanced and 0001) 1. Field of the Invention synergistic manner. Such benefits may diminish if the con 0002 This invention relates to the relief of pain and centrations of the individual ingredients are significantly inflammation, in particular to the control of pain and inflam below or significantly above the preferred ranges. For mation by the application of a topical composition contain instance, active ingredient concentrations significantly ing active ingredients in a suitable carrier for their transport above the preferred ranges may produce unwanted side through a patient's skin. effects Such as the thinning of the epidermis, skin rashes, Suppression of the adrenal glands, or excessive desensitiza 0003 2. Description of the Related Art tion of the skin. On the other hand, active ingredient 0004. Managing pain and inflammation remains a chal concentrations significantly below the preferred ranges may lenge today in medicine. Current treatment options include not be in sufficient amounts to produce the desired effects of the oral administration of opioid analgesics such as mor the present invention. phine, codeine and hydrocodone. The oral administration of DETAILED DESCRIPTION OF THE non-steroidal anti-inflammatory drugs (NSAID) such as INVENTION aspirin and ketoprofen provides another option in managing 0007. The present invention relates to topical composi pain and inflammation. Despite their effectiveness, the oral tions that can contain a combination of an anti-inflammatory use of the above classes of drugs is associated with various steroid Such as hydrocortisone, a topical anesthetic Such as adverse events. For instance, opioid analgesics dispose a lidocaine, menthol, and a medically acceptable carrier at patient to iatrogenic addiction, where the patient develops a appropriate concentrations to relieve pain and inflammation. dependency on the potent drug and consequently abuses it. In another embodiment, the above compositions may con The use of opioid analgesics is also associated with undes tain one or more chondroprotective agents such as chon ired symptoms Such as sedation and constipation. Likewise, droitin Sulfate and/or glucosamine at therapeutically effec pain management by the oral administration of non-steroidal anti-inflammatory drugs is associated with irritation to the tive concentrations. gastrointestinal tract, gastric bleeding, and ulcer. Other more 1. Anti-Inflammatory Steroid serious adverse events associated with the oral administra 0008 Many steroids have potent anti-inflammatory prop tion of NSAID’s include increased risks in heart attacks and erties and are used to treat a variety of conditions such as related cardiovascular diseases, as identified in AleveR) and arthritis, colitis, asthma, bronchitis, certain skin rashes, and Vioxx(R). Thus, many topical compositions containing allergic or inflammatory conditions of the nose and eyes. NSAIDs and opioid analgesics, either alone or in combi Unlike NSAID's that reduce inflammation by inhibiting the nation with other active ingredients, have been developed to biosynthesis of prostaglandins, steroidal anti-inflammatory by-pass the gastrointestinal tract and therefore mitigate the agents reduce inflammation by inducing protein synthesis adverse events associated with oral administration. Such via gene expression. A desirable anti-inflammatory steroid topical compositions also have the additional advantage of for the present invention is hydrocortisone. Hydrocortisone acting much faster in relieving pain and inflammation. is a natural corticosteroid produced by the adrenal glands. However, a challenge remains in optimizing and enhancing Other steroids suitable for the present invention include the therapeutic effects of these topical compositions. alcometasone, clocortolone, dexamethasone, hydrocortisone 21-acetate, prednisone, hydrocortisone 17-Valerate, hydro SUMMARY OF THE INVENTION cortisone 17-butyrate, betamethasone Valerate, triamcino lone acetonide, flucinonide, desonide, flucinolone acetonide, 0005 The present invention relates to the relief of pain dexamethasone 21-phosphate, prednisolone, prednisolone and inflammation by the topical application of a composition 21-phosphate, haloprednone, cortisone acetate, hydrocorti comprising a combination of remedies in a carrier compo Sone cyclopentylpropionate, cortodoxone, flucetonide, sition to enhance their transport through a patient’s skin. In fludrocortisone acetate, flurandrenolone acetonide, particular, the present invention achieves new and unex medrysone, amcinafal, amcinafide, betamethasone, pected Synergistic effects in treating pain and inflammation betamethasone benzoate, chloroprednisone acetate, clocor from the combination of an anti-inflammatory steroid Such tolone acetate, descinolone acetonide, desoximetaSone, as hydrocortisone, a topical anesthetic Such as lidocaine, and dichlorisone acetate, difluprednate, flucloronide, flumetha menthol at appropriate concentrations in a medically Sone, flumethasone pivalate, flunisolide acetate, flucor accepted carrier composition. Chondroprotective agents tolone, fluorometholone, fluperolone acetate, flupredniso Such as chondroitin Sulfate and/or glucosamine can also be lone, fluprednisolone Valerate, meprednisone, methyl added to further enhance the pain-relieving and anti-inflam prednisolone, paramethasone acetate, prednisolamate, pred matory properties of the present invention. nival, triamcinolone, triamcinolone hexacetonide, cortiva 0006. In the present invention, the appropriate concen Zol, formocortal. nivaZol or methylprednisone, beclometha tration of the medically accepted carrier may be the amount sone 17,21-dipropionate, betamethasone 17-valerate, effective to facilitate the transmission of the topical compo betamethasone 17,21-dipropionate, clobetasol 17-propi sitions of the present invention through the skin. The appro onate, clobetasone 17-butyrate, mixtures thereof, and priate concentration of menthol is preferably in an amount equivalents thereof. from about 1% to about 10% of the composition by weight. 0009. In the present invention, the steroidal anti-inflam The appropriate concentrations of the topical anesthetic Such matory compound Such as hydrocortisone is preferably US 2006/0194759 A1 Aug. 31, 2006 present in an amount from about 1% to about 4%, preferably agents have anti-inflammatory and pain relieving properties from about 1% to about 2%, and more preferably approxi in patients Suffering from osteoarthritis and other inflamma mately 1% of the composition by weight. The steroidal tory conditions. It is hypothesized that chondroprotective anti-inflammatory compound at the above concentration agents have such effects by interfering with the inflamma ranges, in combination with the other active ingredients of tory cascade, inhibiting cartilage-degrading enzymes, stimu the present invention at appropriate concentrations, lating the production of new matrix and structural proteins, enhances and synergizes the relief of pain and inflammation. improving the quality of synovial fluid to enhance cartilage Steroidal anti-inflammatory drug concentrations signifi nutrition and lubrication, stimulating the production of free cantly below 1% may be too low to produce such effects. radical Scavenging enzymes, and improving blood flow to The therapeutic effects of the present invention may also be joint tissues. Examples of chondroprotective agents Suitable affected at Steroidal concentrations significantly above 4%. for the present invention include but are not limited to Continued and prolonged usage at Such concentrations may chondroitin Sulfate, glucosamine, N-acetyl glucosamine, enhance a patient's disposition to various skin conditions polysulfated glycosaminoglycan, hyaluronic acid, pentosan Such as drying, cracking, irritation, Suppression of the adre polysulfate, and derivatives thereof. Chondroitin sulfate and nal glands, Cushing's syndrome, excessive fluid retention, glucosamine are the best studied and therefore the preferred dermatitis, allergic reactions, thinning of the skin, and chondroprotective
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