Abstract:
The present invention relates to a method of removing or masking odor associated with chondroitin derived from marine life. The method comprises blending the chondroitin with citric acid, silicon dioxide, and optionally a flavorant to yield a substantially non-malodorous blend.

Description:
[0001]     This application claims priority from provisional application No. 60/274806. filed Mar. 9, 2001, and is a divisional application of co-pending application Ser. No. 10/094,096. 
     
    
     FIELD OF THE INVENTION  
       [0002]     The present invention relates to a method for the removal or masking of malodor from chondroitin derived from marine life. The present invention also relates to chondroitin compositions derived from marine life which lack a malodor.  
       BACKGROUND OF THE INVENTION  
       [0003]     Chondroitin and glucosamine are chondroprotective agents used for the treatment of osteoarthritis and related diseases. Chondroitin sulfate is a soluble mucopolysaccharide derived from bovine, ovine or shark cartilage. Chondroitin sulfate derived from marine life, such as cartilage isolated from sharks, provides a rich, pure, and readily absorbed source of chondroitin.  
         [0004]     Chondroitin sulfate has been reported to be effective in tissue repair and cartilage regeneration. Combinations of glucosamine and chondroitin are also effective in cartilage regeneration and joint maintenance. Chondroitin and glucosamine appear to act by increasing chondrocyte anabolic activity and suppressing degradative action of mediators on cartilage. This appears to facilitate natural tissue repair. See, e.g., H. Benedikt,  Nat. Pharm.,  1(8): 1, 22 (1997) and C. Bassleer, et al.,  Int. J. Tiss. Reac.  XIV(5): 231-241: (1992). Additionally, chondroitin and glucosamine are believed to be safer and less toxic than steroids or non-steroidal anti-inflammatory drugs commonly administered to treat arthritis and related musculo-skeletal diseases.  
         [0005]     Although shark cartilage is rich source of chondroitin, shark-derived chondroitin has a strong malodor.  
         [0006]     Therefore, there is a need for compositions containing shark-derived chondroitin without its malodor and methods of preparing the same. Removal of the malodor associated with such chondroitin would improve consumer acceptability and enhance patient compliance.  
       OBJECT OF THE INVENTION  
       [0007]     It is an object of the invention to provide a method for removing and/or reducing the malodor associated with chondroitin derived from marine life. It is further an object of the invention to provide chondroitin derived from marine life which exhibits reduced levels of malodor normally associated with such a composition.  
       SUMMARY OF THE INVENTION  
       [0008]     The invention relates to a method of removing or masking odor associated with chondroitin sulfate. The method comprises blending the chondroitin with citric acid, silicon dioxide, and, optionally a flavorant, to yield a substantially non-malodorous blend. The blend may be formed into a solid dosage form, such as a tablet.  
         [0009]     Another embodiment of the invention is a composition comprising chondroitin, citric acid, silicon dioxide, and an optional flavorant. 
     
    
     DETAILED DESCRIPTION OF THE INVENTION  
       [0010]     The present inventors have discovered that the malodor associated with chondroitin derived from marine life may be removed or masked by blending the chondroitin with citric acid and silicon dioxide. Chondroitin compositions produced through the use of the present invention exhibit reduced levels of the malodor normally associated with such chondroitin compositions derived from marine sources  
         [0011]     The chondroitin may be any chondroitin-containing composition. Commonly available are two salts, namely chondroitin sulfate or chondroitin hydrochloride. Preferably, the chondroitin is the sulfate salt and is derived from shark cartilage. Most preferably, the chondroitin is water soluble, such as Polychon 60/40 available from Vanson, Inc. (Pfanstiehl Laboratory Inc.) of Waukegan, Ill.  
         [0012]     The amount of citric acid in the composition broadly ranges from about 0.05 to about 10% percent by weight based upon 100 percent by weight of total composition. Preferably, the amount of citric acid in the composition is about 1.5 percent by weight on the same basis.  
         [0013]     The amount of silicon dioxide in the composition ranges broadly from about 0.01 to about 2.0 percent by weight based upon 100 percent by weight of total composition. Preferably, the amount of silicon dioxide in the composition is preferably about 0.2 percent by weight on the same basis.  
         [0014]     Other adjuvants as known to those in the art, such as disintegrants, antioxidants, lubricants and binders, may be included in the composition.  
         [0015]     Optionally, the composition may contain a flavorant. The flavorant may be a natural flavorant, an artificial flavorant, or a combination thereof. Preferred flavorants include, but are not limited to, natural lemon extract, artificial lemon extract,  10  natural orange extract, and any combination of any of the foregoing. The composition may contain an amount of flavorant effective in masking any degree of malodor remaining in the chondroitin-containing composition. The amount of flavorant in the composition broadly ranges from 0.0 to about 10 percent by weight based upon 100 percent by weight of total composition. Preferably, the flavorant is present in the composition in an amount of about 3.3 percent by weight on the same basis.  
         [0016]     Combinations of chondroitin and glucosamine compounds are popular. Therefore, glucosamine or a salt thereof, may also be included in the composition. Preferred salts of glucosamine indude, but are not limited to, glucosamine hydrochloride and glucosamine sulfate. The weight ratio of chondroitin sulfate to glucosamine generally ranges from about 1:100 to about 100:1. The typical mixture found in the composition which are currently commercialized have a weight ratio of about 5:4. Therefore, the preferred weight ratio of glucosamine to chondroitin is about 5:4. A preferred glucosamine is glucosamine hydrochloride, such as that produced by Wilke International of 15036 W. 106 th  Street, Lexexa, Kans. 66215.  
         [0017]     The composition may be incorporated into or formed into solid dosage forms, such as capsules or tablets.  
         [0018]     The claimed composition may be prepared by blending the chondroitin compound with citric acid, silicon dioxide, and optionally a flavorant. Preferably, citric acid, silicon dioxide, and the flavorant are mixed to form a citric acid/silicon dioxide/flavorant mixture prior to blending with the chondroitin sulfate. The citric acid/silicon dioxide/flavorant mixture is preferably prepared by mixing silicon dioxide and the flavorant and then adding citric acid.  
       EXAMPLE  
       [0019]     The following example illustrates the invention without limitations. All amounts are by weight unless otherwise specified.  
       Example 1  
       [0020]     Silicon dioxide (3.0 mg) available as Aerosil from Degussa-Huls Corporation of Ridgefield Park, N.J. was blended with 49.5 mg of natural lemon extract for about 3 minutes in a PK blender (manufactured by Patterson &amp; Keely, a divison of Harsco Corporation, East Stroudsburg, Pa. 18301). Citric acid (22.5 mg) was added to the silicon dioxide/lemon extract blend and blended for about 2 minutes.  
         [0021]     A 5:4 mixture of glucosamine sulfate and chondroitin sulfate was prepared by mixing in a mixing bowl with a PK Blender 750 grams of glucosamine hydrochloride (marketed by Pfanstiehl Laboratory Inc. of 1219 Glen Rock Avenue, Waukegan, Ill. 60085) and 600 grams of chondroitin sulfate (marketed under the tradename Polychon® 60/40 by Vanson, Inc. of Waukegan, Ill.). The mixture was placed into the feed hopper of a Fitzpatric IR-520 Chilsonator. The chilsonator converted the mixture into a compacted solid. The chilsonator was operated at a roll speed of 6 rpm, roll pressure of 1250 psig, vertical screw speed of 150 rpm, and horizontal screw speed of 15 rpm. The compacted product formed in the chilsonator was passed through a Fitzpatric M5A mill and the granulated product collected. The mill was operated at a rotor speed of 300 rpm with a 4 bar rotor and a 0.050 inch rasping screen. The relative humidity was 57% and the temperature was 75° F.  
         [0022]     The chondroitin sulfate/glucosamine hydrochloride mixture, 30.0 mg of sodium starch glycolate, and 15.0 mg of magnesium stearate were added to the silicon dioxide/lemon extract/citric acid blend and blended for about 3 minutes. The resulting powder blend was then compressed into a tablet at a suitable compression pressure using a rotary tablet press and standard tooling. The resulting tablet did not exhibit any malodor, differing substantially from that exhibited by the initial chondroitin sulfate component.  
         [0023]     Many variations of the present invention will suggest themselves to those skilled in the art in light of the above, detailed description. All such obvious variations are within the full intended scope of the appended claims.