Proteoglycan compositions for treatment of inflammatory diseases

Abstract

Compositions with synergistic anti-inflammatory effects in inflammatory diseases resulting from activation and consequent degranulation of mast cells and followed by secretion of inflammatory biomolecules from the activated mast cells, composed of, as active ingredients, a heavily sulfated, non-bovine proteoglycan such as shark cartilage chondroitin sulfate C and an unrefined olive kernel extract that increases absorption of these compositions in various routes of administration, plus one or more of a hexosamine sulfate such as D-glucosamine sulfate, a flavone such as quercetin, S-adenosylmethionine, a histamine-1 receptor antagonist, a histamine-3 receptor agonist, an antagonist of the actions of CRH, caffeine, and a polyamine.

I claim:  
     
         1 . A composition with synergistic anti-inflammatory properties in conditions induced by th activation of mast cells, consequent degranulation of said cells and secretion of inflammatory biomolecules, comprising a non-bovine proteoglycan sulfate and an unrefined olive kernel extract, plus one or more of a hexosamine sulfate, a flavone,, S-adenosylmethionine (“SAM”), a histamine-1 receptor antagonist, a histamine-3 agonist, an antagonist of the actions of Corticotropin Releasing Hormone (“CRH”), a hyaluronate salt, a rutin, a polyamine, and caffeine, in an appropriate excipient or vehicle.  
     
     
         2 . The composition according to  claim 1 , wherein said sulfated proteoglycan is selected from the group consisting of non-bovine chondroitin sulfate, keratan sulfate, dermatan sulfate and sodium hyaluronate.  
     
     
         3 . The composition according to  claim 2 , wherein said chondroitin sulfate is chondroitin sulfate C derived from shark cartilage.  
     
     
         4 . The composition according to  claim 1 , wherein said hexosamine sulfate is D-glucosamine sulfate.  
     
     
         5 . The composition according to  claim 1 , wherein said flavone is selected from the group consisting of quercetin, myricetin, genistein and kaempferol.  
     
     
         6 . The composition according to  claim 1 , wherein said unrefined olive kernel extract contains polyphenols and alpha-tocopherol.  
     
     
         7 . The composition according to  claim 1 , said composition being for oral use, comprising 10-3,000 mg per capsule or tablet of each of non-bovine chondroitin sulfate C, quercetin and D-glucosamine sulfate, with 900-1200 mg unrefined olive kernel extract.  
     
     
         8 . The composition according to  claim 7 , further supplemented with 3-1,000 mg of SAM per capsule or tablet.  
     
     
         9 . A composition according to  claim 1 , wherein said inflammatory diseases are selected from the group consisting of: arthritis, cancers, fibromyalgia, inflammatory bowel disease, interstitial cystitis, irritable bowel syndrome, migraines, angina, chronic prostatitis, eczema, multiple sclerosis, psoriasis, sun burn, tooth decay, periodontal disease, stressed-induced migraines, stress-induced opening of bladder mucosa, stress-induced opening of the blood-brain barrier, superficial vasodilator(flush} syndrome, and hormonally-dependent cancers.  
     
     
         10 . The composition according to  claim 9 , wherein said inflammatory disease is arthritis and said composition is for oral administration, comprising non-bovine chondroitin sulfate, quercetin, D-glucosamine sulfate, unrefined kernel olive oil, and, optionally, sodium hyaluronate.  
     
     
         11 . The composition according to  claim 9 , wherein said inflammatory disease is arthritis and said composition is for topical use, comprising D-glucosamine sulfate, non-bovine chondroitin sulfate, sodium hyaluronate, bitter willow bark extract, quercetin and unrefined olive kernel extract.  
     
     
         12 . The composition according to  claim 9  for oral or aerosol use in allergicconditions, comprising non-bovine chondroitin sulfate and a flavonoid selected from the group consisting of quercetin, myricetin and kaempferol, unrefined kernel olive oil, and, optionally, a histamine-1 receptor antagonist.  
     
     
         13 . The composition according to  claim 9 , for topical use in allergic conditions, comprising non-bovine chondroitin sulfate, myricetin, alpha-tocopherol, unrefined kernel olive oil, and, optionally, a histamine-1-receptor antagonist.  
     
     
         14 . The composition according to  claim 13 , wherein said antagonist is diphenhydramine, hydroxyzine, azatadine, azelastine or cyproheptadine  
     
     
         15 . The composition according to  claim 9  wherein said inflammatory disease is superficial vasodilator “flush” syndrome, said composition comprising a non-bovine proteoglycan, a flavonoid, bitter willow bark extract, and, optionally, cyproheptadine or azatadine.  
     
     
         16 . The composition according to  claim 9 , wherein said inflammatory disease is multiple sclerosis, said composition comprising quercetin or myricetin, hydroxyzine, and, optionally, caffeine, SAM and interferon-beta.  
     
     
         17 . The composition according to  claim 9 , wherein said inflammatory disease is migrain headaches, and said composition comprises non-bovine chondroitin sulfate, quercetin, and azatadine  
     
     
         18 . The composition according to  claim 1 , said composition being for oral use, comprising 150-300 mg per capsule or tablet of each of non-bovine chondroitin sulfate, quercetin and D-glucosamine sulfate, with 900-1200 mg of unrefined olive kernel extract, and, optionally, 100-200 mg sodium hyaluronate and/or 100 mg SAM.  
     
     
         19 . The composition according to  claim 1 , said composition consisting of an ointment or cream for topical application, comprising, in % by weight, non-bovine chondroitin sulfate, 5; D-glucosamine sulfate, 5; quercetin, 3; sodium hyaluronate 5; bitter willow bark extract 5; and unrefined kernel olive oil, 15.  
     
     
         20 . The composition according to  claim 19  supplemented by at least one of the histamine-1 receptor antagonists diphenhydramine, hydroxyzine, azelastine, azatadine r cyproheptadine, 1-5 mg %.  
     
     
         21 . The composition according to  claim 1 , said composition compromising a mouth wash composition, consisting of non-bovine chondroitin sulfate and quercetin, each 0.3-0.4 M, and, optionally, at least one of D-glucosamine sulfate, 0.4 M and SAM, 0.15 M, in a mouth wash vehicle.  
     
     
         22 . The composition according to  claim 1 , said composition consisting of a tooth paste, comprising, in mg %, non-bovine chondroitin sulfate, 5; quercetin, 3; and, optionally, D-glucosamine sulfate, 5, in a tooth paste vehicle.  
     
     
         23 . The composition according to  claim 1 , said composition consisting of a sunscreen composition, comprising, in mg %, non-bovine chondroitin sulfate, 5; quercetin 3; and at least one of D-glucosamine sulfate, 5, and titaniun dioxide, 5, in a sun screen vehicle.  
     
     
         24 . The composition according to  claim 1 , for use in treating migraine headaches, said composition comprising, in mg, non-bovine chondroitin sulfate, 50; guercetin, 100; azatadine ,4; and, optionally, a CRH antagonist.  
     
     
         25 . The composition according to  claim 1 , said composition comprising, in mg, non-bovine chondroitin sulfate, 50: quercetin, 400; hydroxyzine, 50; and, optionally, a CRH antagonist.  
     
     
         26 . The composition according to  claim 1 , said composition comprising, in mg, non-bovine chondroitin sulfate, 100; D-glucosamine sulfate, 50; quercetin, 100; and unrefined olive kernel extract, 900-1200.  
     
     
         27 . The composition according to  claim 1 , comprising, in mg %, non-bovine chondroitin sulfate, 5; D-glucosamine sulfate, 5; quercetin, 3; in 900-1200 mg of unrefined olive kernel extract.  
     
     
         28 . The composition according to  claim 1 , wherein said inflammatory disease is cancer and wherein said composition is designed for oral use, comprising 25-50 mg of genistein and 150-300 mg of quercetin, in 900-1200 mg unrefined kernel olive oil.  
     
     
         29 . The composition according to  claim 1 , wherein said inflammatory disease is atherosclerosis with or without myocardial ischemia, comprising 100-300 mg each of non-bovine chondroitin sulfate, myricetin, folic acid and SAM, in 900-1200 mg unrefined kernel olive extract, in a vehicle for oral use.  
     
     
         30 . The composition according to  claim 1 , wherein said inflammatory disease is interstitial cystitis or prostatitis, said composition comprising, in mg, 100-300 of non-bovine chondroitin sulfate, 50-300 D-glucosamine sulfate, 100-300 of sodium hyaluronate, and 100-400 quercetin, 900-1200 unrefined olive kernel extract, in a vehicle for oral use.  
     
     
         31 . The composition according to  claim 1 , wherein said inflammatory disease is multiple sclerosis, said composition comprising, in mg, 50-300 each of non-bovine chondroitin sulfate, myricetin, hydroxyzine and SAM, 900-1200 of unrefined olive kernel extract, and, optionally, interferon-beta, in a vehicle for oral use.  
     
     
         32 . The composition according to  claim 1 , said composition comprising, in mg, non-bovine chondroitin sulfate 500; myricetin 300; and diphenhydramine, 5 mg %.  
     
     
         33 . The composition according to  claim 1 , said composition comprising, in mg, non-bovine chondroitin sulfate, 50; kaempferol, 100; SAM, 50; folic acid, 50; niacin, 100; and unrefined olive kernel extract, 900-1200.  
     
     
         34 . The composition according to  claim 1 , wherein said inflammatory disease is superficial vasodilation flush syndrome, said composition comprising 50 mg non-bovine chondroitin sulfate, 150 mg quercetin, 5% by weight bitter willow bark extract, and, optionally, 4 mg cyproheptadine or azatadine.  
     
     
         35 . The composition according to  claim 1 , wherein said inflammatory disease is skin allergy, said composition comprising, in % by weight, 5 each of aloe vera, non-bovine chondroitin sulfate and alpha-tocopherol, 15 of unrefined olive kernel extract, and, optionally, azelastine.  
     
     
         36 . The composition according to  claim 1 , wherein said inflammatory disease in allergy or allergic asthma, comprising 500 mg of myricetin, 200 mg of chondroitin sulfate, and, optionally, azelastine or hydroxyzine.  
     
     
         37 . The composition according to  claim 36 , in an aerosol vehicle.  
     
     
         38 . The composition according to  claim 1 , wherein said inflammatory disease is a hormonally-dependent cancer, comprising, in mg, 150 quercetin, 50 genestein, and, optionally, 10 tamoxifen or raloxifen.  
     
     
         39 . The composition according to  claim 1 , wherein said inflammatory disease is allergic conjunctivitis, comprising quercetin 0.05%, chondroitin sulfate 2.0%, and, optionally, azelastine 0.05%.