Novel stable beadlets of lipophilic nutrients

Abstract

The invention disclosed in this application relates to novel stable beadlets of lipophilic nutrients comprising an inert core having a coating of stabilizing antioxidants, lipophilic nutrients, or mixtures thereof. The beadlets may be coated with one or more coatings to protect the lipophilic ingredients from the atmosphere, specifically the coatings can be used to protect against moisture and/or oxygen. The invention also relates to a process for the preparation of the stable beadlets. The beadlets can be used in medicines and dietary supplements intended to facilitate the reduced risk of macular degeneration, cataract, and several forms of cancer.

1 - 18 . (canceled) 
   
   
       19 . A process for the preparation of beadlets of lipophilic nutrients comprising:
 (i) forming a colloidal suspension of lipophilic nutrient by dissolving the lipophilic nutrient in a non-polar solvent and diluting the resulting solution with a polar solvent;   (ii) spraying the resulting colloidal suspension onto an inert core in a fluid-bed system provided with a bottom-spray mechanism at a temperature in the range of ambient temperature to 45 degree C., at an atomisation pressure in the range of about 0.1 kg/cm 2  to about 3 kg/cm 2  and a spray rate in the range of about 10 g/hour to about 600 g/hour; and   (iii) drying the resulting beadlets in the fluid-bed system at an atomisation pressure of about 0.8 kg/cm 2  to about 1.2 kg/cm 2 .   
   
   
       20 . The process of  claim 19  wherein the lipophilic nutrient comprises a compound selected from the group consisting of carotenoid, lipophilic vitamin, lipid, and mixtures thereof. 
   
   
       21 . A process as claimed in  claim 20  wherein the lipophilic nutrient comprises a carotenoid selected from the group consisting of lutein, zeaxanthin, lutein esters, alpha-carotene, beta-carotene, zeaxanthin esters, astaxanthin, lycopene, and mixtures thereof. 
   
   
       22 . A process as claimed in  claim 20  wherein the lipophilic nutrient comprises a lipophilic vitamin selected from the group consisting of Vitamin A, Vitamin D, Vitamin E as tocopherols or tocotrienols, Vitamin K, and mixtures thereof. 
   
   
       23 . A process as claimed in  claim 20  wherein the lipophilic nutrient comprises a lipophilic nutrient selected from the group consisting of lecithin, mixed tocopherols or tocotrienols, plant sterols, plant stanols, omega 3 fatty acids, polyunsaturated fatty acids, and mixtures thereof. 
   
   
       24 . A process as claimed in  claim 19  wherein the beadlets comprise about 1 wt. % to about 50 wt. % lipophilic nutrient. 
   
   
       25 . A process as claimed in  claim 19  wherein the lipophilic nutrient is mixed with a stabilising antioxidant. 
   
   
       26 . A process as claimed in  claim 25  wherein the stabilising antioxidant comprises a substance selected from the group consisting of vitamin E acetate, natural tocopherols, ascorbyl palmitate, ascorbic acid, sodium ascorbate, citric acid, rosemary extract, rosemary oil, curcuminoids, green tea extract, ginger extract, carnosic acid, butylated hydroxy anisole, butylated hydroxy toluene, and mixtures thereof. 
   
   
       27 . A process as claimed in  claim 19  wherein the inert core comprises a carbohydrate that does not react with the lipophilic nutrient and said carbohydrate is selected from the group consisting of sugar, mannitol, starch, sago, microcrystalline cellulose, and mixtures thereof. 
   
   
       28 . A process as claimed in  claim 19  wherein the inert core is in the form of a sphere, and has a diameter of about 200 microns to about 3 mm. 
   
   
       29 . A process as claimed in  claim 19  wherein the non-polar solvent comprises a solvent selected from the group consisting of methylene chloride, chloroform, petroleum ether (low boiling), petroleum ether (high boiling), and mixtures thereof; and the polar solvent comprises a solvent selected from the group consisting of isopropyl alcohol, acetone, methanol, ethanol, and acetonitrile, and mixtures thereof. 
   
   
       30 . A process as claimed in  claim 19  wherein the non-polar solvent comprises methylene chloride and the polar solvent comprises isopropyl alcohol and the ratio of methylene chloride to isopropyl alcohol is between about 1:1 and about 0.1:1. 
   
   
       31 . The process of  claim 30  wherein the ratio of methylene chloride to isopropyl alcohol ranges from about 0.2:1 to about 2:1. 
   
   
       32 . A process as claimed in  claim 19  wherein the beadlets are provided with an oxygen barrier coating comprising oxygen barrier polymer, said oxygen barrier polymer comprising a polymer selected from the group consisting of hydroxy propyl cellulose, hydroxy propyl methyl cellulose, methacrylate copolymers, polyvinyl pyrrolidone, ethyl cellulose, carboxymethyl cellulose, polyvinyl alcohol, and mixtures thereof. 
   
   
       33 . A process as claimed in  claim 32  wherein the beadlets comprise about 1 wt. % to about 40 wt. % oxygen barrier coating. 
   
   
       34 . A process as claimed in  claim 19  wherein the beadlets are provided with a moisture barrier coating comprising a moisture barrier polymer selected from the group consisting of carboxy methyl cellulose sodium, hydroxy propyl cellulose, hydroxy propyl methyl cellulose, methacrylate copolymers, polyvinyl alcohol, and mixtures thereof. 
   
   
       35 . A process as claimed in  claim 34  wherein the beadlets comprise about 1 wt. % to about 40 wt. % moisture barrier coating. 
   
   
       36 . A process as claimed in  claim 34  wherein the moisture barrier coating also acts as an oxygen barrier. 
   
   
       37 . A process as claimed in  claim 19  wherein the beadlets are in the form of spheres having a diameter of about 250 microns to about 3.5 mm. 
   
   
       38 . A process as claimed in  claim 19  wherein a stabiliser and/or a disintegrating agent are added to the lipophilic nutrient. 
   
   
       39 . A process as claimed in  claim 38  wherein the beadlet comprises stabiliser, said stabiliser comprising a compound selected from the group consisting of sorbic acid, sodium benzoate, sodium salicylate, EDTA, and mixtures thereof. 
   
   
       40 . A process as claimed in  claim 38  wherein the beadlet comprises disintegrating agent, said disintegrating agent comprising a compound selected from the group consisting of starch, cross-linked polyvinyl pyrrolidone, cross-carmellose, sodium starch glycolate, and mixtures thereof. 
   
   
       41 . A process as claimed in  claim 38  wherein the beadlets comprise about 0.1 wt. % to about 5 wt. % disintegrating agent. 
   
   
       42 . A process as claimed in  claim 38 , wherein the beadlets comprise about 0.1 wt. % to about 20 wt. % stabilizer and/or disintegrating agent. 
   
   
       43 . A process as claimed in  claim 19  wherein a binding agent is mixed with the colloidal suspension before it is used for spraying in the fluidised system, said binding agent comprising a compound selected from the group consisting of gum acacia, gum tragacanth, gum xanthan, polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxypropyl methyl cellulose (5 cps), hydroxypropyl methyl cellulose (15 cps), and mixtures thereof. 
   
   
       44 . A process as claimed in  claim 43  wherein the binding agent is hydroxypropyl methyl cellulose and the beadlets comprises about 0.1 wt. % to about 10 wt. % binding agent. 
   
   
       45 . A process as claimed in  claim 43  wherein a stabilizer and/or a disintegrating agent is used along with the binding agent. 
   
   
       46 . A process as claimed in  claim 19  wherein the colloidal suspension is sprayed at a bed temperature ranging from about 25 degree C. to about 40 degree C. 
   
   
       47 . A process as claimed in  claim 26  wherein the atomization pressure during spraying is in the range of about 0.5 kg/cm 2  to about 3 kg/cm 2 .