Claims for Patent: 6,025,334

Summary for Patent: 6,025,334

Title:	Extracts of shark cartilage having anti-collagenolytic, anti-inflammatory, anti-angiogenic and anti-tumoral activities; process of making, methods of using and compositions thereof
Abstract:	The present invention relates to cartilage extracts and to a method of producing the same. Shark cartilage extracts having anti-angiogenic, direct anti-tumor proliferating, anti-inflammatory and anti-collagenolytic activities have been obtained by an improved process. The process comprises the steps of obtaining a homogenate of cartilage in an aqueous solution, this homogenate being centrifuged and further fractionated to obtain a total extract having molecules of a molecular weight comprised between 0 to 500 KDa. The composition of the liquid extract has then been investigated by different ways. Further fractionation of this extract led to the preliminary characterization of some of its active components. Due to the multiplicity of biological activities of the total liquid extract, it can be used for treating numerous diseases or conditions such as those having components selected from the group consisting of tumor proliferation, angiogenesis, inflammation and collagenolysis. This extract has no offensive effect on normal body functions. Therefore, this shark cartilage extract has a very promising therapeutic value. The process for the obtention of cartilage extracts is simple and efficient. The unexpectedly valuable products obtained by this process are therefore an indication of a new and non-obvious process.
Inventor(s):	Dupont; Eric (St. Nicolas, CA), Brazeau; Paul (Montreal, CA), Juneau; Christina (Ste. Foy, CA), Maes; Daniel H. (Huntington, NY), Marenus; Kenneth (Dix Hills, NY)
Assignee:	Les Laboratoires Aeterna Inc. (CA)
Application Number:	08/550,003
Patent Claims:	1. A process for obtaining a liquid extract of cartilage having a substantial portion of the biologically active components present in intact cartilage, which comprises the following steps: a) homogenizing the cartilage in an aqueous solution in conditions which are non-denaturing towards biologically active components, until the cartilage is reduced to solid particles whose size is lower than or equal to about 500 .mu.m; b) extracting said biologically active component into said aqueous solution which results in a mixture of solid particles and of a crude liquid extract having said biologically active components; c) separating said crude liquid extract from said solid particles; and d) further separating the crude liquid extract so as to obtain a final liquid extract containing cartilage molecules having a molecular weight lower than about 500 Kilodaltons (Kda); with the proviso that the cartilage is not shark cartilage. 2. A process as defined in claim 1, wherein said conditions comprise a working temperature comprised between about 0 to 10.degree. C. 3. A process as defined in claim 1, wherein said conditions comprise a working pH ranging from about 6 to about 8 for said aqueous solution. 4. A process as defined in claim 1, wherein said aqueous solution is purified water. 5. A process as defined in claim 1, wherein said cartilage and aqueous solution are in proportions of 1 Kilogram for about 1 liter or more aqueous solution volume. 6. A cartilage extract produced by the method of claim 1. 7. A process as defined in claim 1, wherein step b) is performed within 15 minutes to 24 hours. 8. A process as defined in claim 7, wherein step b) is performed within 15 minutes to 1 hour. 9. A topical formulation for treating diseases or disorders having one or more etiological components selected from the group consisting of tumor proliferation, angiogenesis, inflammation and collagenolysis, the topical formulation comprising a pharmaceutical composition comprising an effective amount of a shark cartilage extract and an antioxidant, said shark cartilage extract being prepared according to a process comprising the steps of: a) homogenizing the cartilage in an aqueous solution in conditions which are non-denaturing towards biologically active components, until the cartilage is reduced to solid particles whose size is lower than or equal to about 500.mu.; b) extracting said biologically active components into said aqueous solution which results in a mixture of solid particles and of a crude liquid extract having said biologically active components; c) separating said crude liquid extract from said solid particles; and d) further separating the crude liquid extract so as to obtain a final liquid extract containing cartilage molecules having a molecular weight lower than about 500 Kilodaltons (Kda). 10. A formulation as defined in claim 9, wherein the antioxidant is selected from the group consisting of tocopherol, tocopherol derivatives, ascorbic acid, ascorbic acid derivatives and butylated hydroxy-toluene. 11. A formulation as defined in claim 9, wherein the formulation is selected from the group consisting of solution, suspension, lotion, tincture, gel, cream, spray, emulsion, stick and ointment. 12. A formulation as defined in claim 9, wherein said formulation comprises liposomes comprising the cartilage extract. 13. A method for soothing mammalian skin which comprises the step of applying to the skin a composition as defined in claim 9. 14. A method for inhibiting collagenase activity in mammalian skin which comprises the step of applying to the skin a composition as defined in claim 9. 15. A method for reducing acne in mammalian skin which comprises the step of applying to the skin a formulation as defined in claim 9. 16. A method for reducing psoriasis in mammalian skin which comprises the step of applying to the skin a formulation as defined in claim 9. 17. A method for treating diseases or disorders having one or more etiological components selected from the group consisting of tumor proliferation, angiogenesis, inflammation and collagenolysis, the method comprising the step of administering to a patient in need of such treatment a formulation as defined in claim 9. 18. A method as defined in claim 17, wherein said diseases or disorders are selected from the group consisting of cancer, psoriasis, skin irritation and skin inflammation, arthritis and acne. 19. A formulation as defined in claim 9 additionally comprising an anti-inflammatory agent. 20. A formulation as defined in claim 19, wherein the anti-inflammatory agent is a phospholipase A2 inhibitor. 21. A formulation as defined in claim 19, wherein the anti-inflammatory agent is a botanically-derived anti-irritant. 22. A formulation as defined in claim 21, wherein the anti-inflammatory agent is selected from the group consisting of cola and green tea extract. 23. A method for reducing inflammation in mammalian skin which comprises the step of applying to the skin a formulation as defined in claim 9. 24. A method as defined in claim 23 wherein said inflammation is caused by physical abrasion. 25. A method as defined in claim 23 wherein said inflammation is caused by chemical irritant. 26. A method as defined in claim 23 wherein said inflammation is caused by exposure to ultraviolet radiation. 27. A method for treating diseases or disorders having one or more etiological components selected from the group consisting of inflammation and collagenolysis, the method comprising the step of administering to a patient in need of such treatment an effective amount of a shark cartilage extract, said shark cartilage extract being prepared according to a process which comprises the following steps: a) homogenizing the cartilage in an aqueous solution in conditions which are non-denaturing towards biologically active components, until the cartilage is reduced to solid particles whose size is lower than or equal to about 500 .mu.. b) extracting said biologically active components into said aqueous solution which results in a mixture of solid particles and of a crude liquid extract having said biologically active components; c) separating said crude liquid extract from said solid particles; and d) further separating the crude liquid extract so as to obtain a final liquid extract containing cartilage molecules having a molecular weight lower than about 500 Kilodaltons (Kda). 28. A method as defined in claim 27, wherein said diseases or disorders are selected from the group consisting of cancer, psoriasis, arthritis, acne, skin irritation and skin inflammation.

Details for Patent 6,025,334

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Smith & Nephew, Inc.	SANTYL	collagenase	Ointment	101995	06/04/1965		2014-04-28