Stability additives for dry dha dosage forms

Abstract

The use of additives to stabilize DHA when compressed into tablets, or filled as a powder into capsules, for oral administration.

1 ) A nutritional supplement in the form of an orally administered tablet or powder-filled capsule comprising:
 a) dry docosahexaenoic acid (DHA) in an amount of from 100 to 300 mg; and   b) an additive selected from elemental iron, calcium ascorbate, silicon dioxide, calcium carbonate, chelated magnesium, chelated copper and combinations thereof, in an amount sufficient to stabilize said DHA from oxidative degradation.   
     
     
         2 ) The nutritional supplement of  claim 1  in the form of a tablet, further comprising one or more excipients selected from lubricants, disintegrants and binders. 
     
     
         3 ) The nutritional supplement of  claim 1  in the form of a tablet, comprising a binder selected from cyclodextrin and maltodextrin and combinations thereof. 
     
     
         4 ) The nutritional supplement of  claim 1 , comprising:
 a) from 100 to 300 mg of DHA; and   b) an additive selected from:
 i) from 10 to 40 mg of elemental iron; 
 ii) from 10 to 100 mg of ascorbic acid as calcium ascorbate; 
 iii) from 5 to 50 mg of chelated copper; 
 iv) from 10 to 300 mg of chelated magnesium; 
 v) from 50 to 300 mg of silicon dioxide; 
 vi) from 100 to 400 mg of calcium carbonate; and 
 vii) any combination thereof. 
   
     
     
         5 ) The nutritional supplement of  claim 1 , comprising, based on the weight of the supplement:
 a) from 10 to 30 wt % DHA; and   b) an additive selected from:
 i) from 2 to 8 wt % elemental iron; 
 ii) from 2 to 20 wt % of calcium as calcium ascorbate; 
 iii) from 1 to 10 wt % chelated copper; 
 iv) from 2 to 20 wt % of chelated magnesium; 
 v) from 5 to 30 wt % of silicon dioxide; 
 vi) from 20 to 70 wt % calcium carbonate; and 
 vii) any combination thereof. 
   
     
     
         6 ) The nutritional supplement of  claim 1  comprising:
 a) DHA and elemental iron in a weight ratio of from 1:12 to 1:3 (DHA:iron);   b) DHA and calcium ascorbate in a weight ratio of from 1:300 to 1:50 (DHA:ascorbic acid);   c) DHA and chelated copper in a weight ratio of from 1:200 to 5:200 (DHA:copper), wherein said copper chelate comprises from 10 to 25 wt % copper;   d) DHA and chelated magnesium in a weight ratio of from 10:200 to 100:200 (DHA:magnesium), wherein said magnesium chelate comprises from 20-30 wt % magnesium;   e) DHA and silicon dioxide in a weight ratio of from 1:1 to 4:1 (DHA:silicon dioxide);   f) DHA and calcium carbonate in a weight ratio of from 4:1 to 1:4 (DHA:calcium carbonate); or   g) a combination thereof.   
     
     
         7 ) A method of stabilizing dry docosahexaenoic acid (DHA) comprising:
 a) providing said DHA in the form of a dry particulate, wherein said particulate further comprises one or more compression binders; and   b) admixing said dry particulate with an additive selected from elemental iron, calcium ascorbate, chelated copper, chelated magnesium, silicon dioxide, calcium carbonate and combinations thereof, and one or more tablet excipients selected from lubricants, disintegrants and binders, to form an admixture.   
     
     
         8 ) The method of  claim 7 , further comprising compressing said admixture into a solid unit, or filling said admixture into a capsule shell. 
     
     
         9 ) The method of  claim 7  wherein step (a) comprises admixing from 100 to 300 mg of DHA with from 10 to 40 mg of said elemental iron, from 10 to 100 mg of ascorbic acid as calcium ascorbate; from 5 to 50 mg of chelated copper; from 10 to 300 mg of chelated magnesium; from 50 to 300 mg of silicon dioxide; from 100 to 400 mg of calcium carbonate; or a combination thereof. 
     
     
         10 ) The method of  claim 7  wherein step (a) comprises:
 a) admixing said DHA and said elemental iron in a weight ratio of from 1:12 to 1:3 (DHA:iron);   b) admixing said DHA and said calcium ascorbate in a weight ratio of from 1:300 to 1:50 (DHA:ascorbic acid);   c) admixing said DHA and said chelated copper in a weight ratio of from 1:200 to 5:200 (DHA:copper), and said copper chelate comprises from 10 to 25 wt % copper;   d) admixing said DHA and said chelated magnesium in a weight ratio of from 10:200 to 100:200 (DHA:magnesium), and said magnesium chelate comprises from 20-30 wt % magnesium;   e) admixing said DHA and said silicon dioxide in a weight ratio of from 1:1 to 4:1 (DHA:silicon dioxide);   f) admixing said DHA and said calcium carbonate in a weight ratio of from 1:4 to 4:1 (DHA:calcium carbonate); or   g) a combination thereof.   
     
     
         11 ) The method of  claim 7  wherein said compression binder in said dry particular is maltodextrin or cyclodextrin. 
     
     
         12 ) A nutritional supplement in the form of an orally administered tablet or powder filled capsule comprising:
 a) dry docosahexaenoic acid (DHA) in an amount of from 100 to 300 mg;   b) elemental iron;   c) copper as copper chelate;   d) magnesium as magnesium chelate; and   e) ascorbic acid as calcium ascorbate.   
     
     
         13 ) The nutritional supplement of  claim 12 , comprising from 150 to 250 mg of DHA. 
     
     
         14 ) The nutritional supplement of  claim 12 , comprising from 10 to 30 wt % DHA, based on the weight of the tablet. 
     
     
         15 ) The nutritional supplement of  claim 12  in the form of a tablet, further comprising one or more excipients selected from lubricants, disintegrants and binders. 
     
     
         16 ) The nutritional supplement of  claim 12  in the form of a tablet, comprising a binder selected from cyclodextrin and maltodextrin and combinations thereof. 
     
     
         17 ) The nutritional supplement of  claim 12 , comprising:
 a) elemental iron in an amount of from 10 to 40 mg;   b) 0.5-2.0 mg of copper as copper chelate;   c) 10-40 mg of magnesium as magnesium chelate; and   d) 20-80 mg. of ascorbic acid as calcium ascorbate.   
     
     
         18 ) The nutritional supplement of  claim 12 , comprising, based on the weight of the supplement:
 a) from 10 to 30 wt % DHA;   b) from 2 to 8 wt % elemental iron;   c) from 2 to 20 wt % of calcium as calcium ascorbate;   d) from 1 to 10 wt % chelated copper; and   e) from 2 to 20 wt % of chelated magnesium.   
     
     
         19 ) The nutritional supplement of  claim 12  comprising:
 a) DHA and elemental iron in a weight ratio of from 1:12 to 1:3 (DHA:iron);   b) DHA and calcium ascorbate in a weight ratio of from 1:300 to 1:50 (DHA:ascorbic acid);   c) DHA and chelated copper in a weight ratio of from 1:200 to 5:200 (DHA:copper), wherein said copper chelate comprises from 10 to 25 wt % copper; and   d) DHA and chelated magnesium in a weight ratio of from 10:200 to 100:200 (DHA:magnesium), wherein said magnesium chelate comprises from 20-30 wt % magnesium.   
     
     
         20 ) A nutritional supplement in the form of a tablet or a powder-filled capsule comprising:
 a) 50-60 mg of vitamin C as calcium ascorbate;   b) 200-1000 IU of vitamin D3 (cholecalciferol);   c) 10-20 IU of vitamin E (dl-alpha tocopheryl acetate);   d) 10-30 mg of vitamin B5 (pyridoxine hydrochloride);   e) 500-2000 mg of folic acid;   f) 5-25 mcg of vitamin B12 (cyanocobalamin);   g) 50-200 mg of calcium (as calcium carbonate);   h) 10-50 mg of iron (elemental);   i) 25-60 mg of magnesium (as magnesium chelate); and   j) 100-300 mg of DHA.