Dietary supplement derived from natural products by hot melt extrusion (hme) processing

Abstract

The invention provides a composition rich in flavonoids based on natural extracts, comprising a flavonoid extract dispersed by melt mixing or extrusion and encapsulated in a polymer matrix. The invention is also a novel dietary supplement with the naturally occurring ingredient (−)-epicatechin, cacao extracted, that could potentially prevent or reduce the risk of Atherosclerotic pathology. The use of (−)-epicatechin is promising as a therapeutic agent due to its potential antioxidant activity and its diverse biological properties. (−)-Epicatechins are chemically unstable and extensively degraded in fluids of near neutral or greater pH, such as intestinal juice and bile. Current technologies used for taste masking and modified release as spray drying, liposome entrapment, co-crystallization, freeze drying, among others, suffer from numerous shortcomings, including poor repeatability and limitations on target delivery.

What is claimed is: 
     
         1 . A composition rich in flavonoids based on natural extracts, comprising a flavonoid extract dispersed by melt mixing or extrusion and encapsulated in a polymer matrix. 
     
     
         2 . The composition of  claim 1 , wherein said extract is at least one from the group consisting of cocoa extract, cacao extract, tea extract,  Vitis vinifera  seeds and skin extract,  Persea americana  leaves, peel and seed extract,  Allium cepa  extract,  Allium sativum  extract,  Vaccinium oxycoccos  and  Vaccinium macrocarpon  extract,  Nasturtium officinale  extract,  Petroselinum crispum  extract,  Vitis vinifera  fruit and red wine extract,  Citrus reticulate, Citrus sinensis, Citrus limon  and  Citrus paradise, Olea europaea  leaves and fruits extract,  Garnicia mangostana  extract,  Garcinia  species extract selected from the group consisting of  G. cambogia, G. kola, G. madruno , and mixtures thereof. 
     
     
         3 . The composition of  claim 1 , wherein said polymer matrix is selected from the group consisting of poly (acrylic acid), poly (ethylene oxide), poly (ethylene glycol), poly (vinyl pyrrolidone), poly (vinyl alcohol), polyacrylamide, poly (isopropyl acrylamide), poly (cyclopropyl methacrylamide), ethyl cellulose, carboxymethyl cellulose, hydroxyethyl cellulose, propyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, cellulose acetate phthalate, alginic acid, carrageenan, chitosan, hyaluronic acid, pectinic acid, (lactide-co-glycolide) polymers, starch, sodium starch glycolate, polyurethane, silicones, polycarbonate, polychloroprene, polyisobutylene, polycyanoacrylate, poly (vinyl acetate), polystyrene, polypropylene, poly (vinyl chloride), polyethylene, poly (methyl methacrylate), poly (hydroxyethyl methacrylate), acrylic acid, butyl acrylate copolymer, 2-ethylhexyl acrylate and butyl acrylate copolymer, vinyl acetate and methyl acrylate copolymer, ethylene vinyl acetate and polyethylene terephthalate, ethylene/vinyl acetate copolymer and polyethylene, polyethylene terephthalate, cellulose, methyl cellulose, hypromellose acetate succinate nf, hypromellose acetate succinate jp, hypromellose acetate succinate, hypromellose phthalate nf, hypromellose phthalate, low-substituted hydroxypropyl cellulose nf, low-substituted hydroxypropyl cellulose jp, low-substituted hydroxypropyl cellulose nf—low-substituted hydroxypropyl cellulose jp copolymer, hypromellose usp, hypromellose ep, hypromellose jp, hypromellose phthalate jp, hypromellose phthalate ep, hypromellose, hypromellose phthalate nf, hypromellose phthalate, low-substituted hydroxypropyl cellulose, methacrylates, cellulose acetate butyrate, polylactide-polyglycolide copolymers, polycaprolactone, polylactide, polyglycolide, polyvinylpyrrolidone-co-vinyl acetate, polyrethanes, polyvinyl caprolactam—polyvinyl acetate—polyethylene glicol graft copolymer, polyvinyl caprolactam, polyvinyl acetate, vinylpyrrolidone—vinyl acetate copolymer, vinyl-pyrrolidone polymer, polyvinylacetate, polyoxyethylene—polyoxypropylene copolymer, polyoxy-ethylene, polyoxypropylene, polyoxirane, povidone, polyethylene oxide, cellulose acetate, copovidone, povidone K12, povidone K17, povidone K25, povidone K30, povidone K90, hypromellose E5, hypromellose E4m, hypromellose K3, hypromellose K100, hypromellose K4m, hypromellose K100m, hypromellose phthalate HP-55, hypromellose phthalate HP-50, hypromellose acetate succinate 1 grade, hypromellose acetate succinate m grade, hypromellose acetate succinate h grade, cellulose acetate phthalate, cationic methacrylate, methacrylic acid copolymer type A, methacrylic acid copolymer type B, methacrylic acid copolymer type C, polymethylacrylates, polyvinyl alcohol, hydroxypropylmethylcellulose acetate succinate, ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate, ethyl acrylate-methyl methacrylate copolymer, butyl/methyl methacrylate-dimethylaminoethyl methacrylate copolymer, butyl/methyl methacrylate, dimethylaminoethyl methacrylate, methacrylic acid-ethyl acrylate copolymer, methacrylic acid, methacrylic acid-methyl methacrylate copolymer, methyl acrylate-methyl methacrylate-methacrylic acid copolymer, methyl acrylate, methyl methacrylate and diethylaminoethyl methacrylate copolymer, methyl methacrylate, diethylaminoethyl methacrylate, succinate, d-α-tocopheryl polyethylene glicol 100 succinate, d-α-tocopheryl polyethylene glicol, ethylene oxide, polypropylene oxide, polyvinyl alcohol-polyethylene glycol graft copolymer, methacrylic acid-ethyl acrylate copolymer, poloxamer, micronized poloxamer, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, ethylene glycol-vinyl alcohol graft copolymer, polydextrose nf, hydrogenated polydextrose nf, methacrylic acid copolymer, methacrylic acid and methyl methacrylate copolymer, methacrylic acid and ethyl acrylate copolymer, carbomer homopolymer, carbomer copolymer, carbomer interpolymer and mixtures thereof. 
     
     
         4 . The composition of  claim 1 , which exhibits taste masking characteristics up to 120 seconds in saliva in the absence of flavoring or sweeteners or related agents. 
     
     
         5 . The composition of  claim 1 , which exhibits taste masking characteristics and successive modified release of minimum 80% up to 240 minutes, wherein the first 120 minutes occurs in a medium of pH=1.2, and the rest 120 minutes in a medium of pH=6.8. 
     
     
         6 . The composition of  claim 1 , having modified release characteristics and having a particle-size distribution between 250 μm and 425 μm. 
     
     
         7 . The composition of  claim 1 , having modified release characteristics and having a particle-size distribution between 180 μm and 250 μm. 
     
     
         8 . The composition of  claim 1 , having modified release characteristics and having a particle-size distribution between 125 μm and 180 μm 
     
     
         9 . The composition of  claim 1 , having modified release characteristics and having a particle-size distribution up to 125 μm 
     
     
         10 . The composition of  claim 1 , having modified release characteristics in the absence of coatings, crosslinking or chemical reactions affecting said composition. 
     
     
         11 . A method for manufacturing the composition of  claim 1 , comprising the steps of:
 (a) melt mixing or extruding the extract under operating conditions and screw configuration to protect the characteristics of said natural extract or mixtures thereof; and   (b) milling the resulting composition to a powder under operating conditions suitable to protect the characteristics of the natural extract or mixtures thereof.   
     
     
         12 . The method of  claim 11 , further including the step of adding the resulting milled powder to a food or a matrix. 
     
     
         13 . A composition manufactured according to  claim 11 , wherein said composition is used in a dietary supplement, food, functional food, nutraceuticals and pharmaceuticals. 
     
     
         14 . A composition manufactured according to  claim 11 , wherein said composition has thermal stability, light and moisture resistance. 
     
     
         15 . A taste masking composition rich in flavonoids based on natural extracts, comprising a flavonoid extract dispersed by melt mixing or extrusion and encapsulated in a polymer matrix. 
     
     
         16 . The composition of  claim 15 , wherein said extract is at least one from the group consisting of cocoa extract, cacao extract, tea extract,  Vitis vinifera  seeds and skin extract,  Persea americana  leaves, peel and seed extract,  Allium cepa  extract,  Allium sativum  extract,  Vaccinium oxycoccos  and  Vaccinium macrocarpon  extract,  Nasturtium Officinale  extract,  Petroselinum crispum  extract,  Vitis vinifera  fruit and red wine extract,  Citrus reticulate, Citrus sinensis, Citrus limon  and  Citrus paradise, Olea europaea  leaves and fruits extract,  Garnicia mangostana  extract,  Garcinia  species extract selected from the group consisting of  G. cambogia, G. kola, G. madruno , and mixtures thereof. 
     
     
         17 . The composition of  claim 15 , wherein said polymer matrix is selected from the group consisting of poly (acrylic acid), poly (ethylene oxide), poly (ethylene glycol), poly (vinyl pyrrolidone), poly (vinyl alcohol), polyacrylamide, poly (isopropyl acrylamide), poly (cyclopropyl methacrylamide), ethyl cellulose, carboxymethyl cellulose, hydroxyethyl cellulose, propyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, cellulose acetate phthalate, alginic acid, carrageenan, chitosan, hyaluronic acid, pectinic acid, (lactide-co-glycolide) polymers, starch, sodium starch glycolate, polyurethane, silicones, polycarbonate, polychloroprene, polyisobutylene, polycyanoacrylate, poly (vinyl acetate), polystyrene, polypropylene, poly (vinyl chloride), polyethylene, poly (methyl methacrylate), poly (hydroxyethyl methacrylate), acrylic acid, butyl acrylate copolymer, 2-ethylhexyl acrylate and butyl acrylate copolymer, vinyl acetate and methyl acrylate copolymer, ethylene vinyl acetate and polyethylene terephthalate, ethylene/vinyl acetate copolymer and polyethylene, polyethylene terephthalate, cellulose, methyl cellulose, hypromellose acetate succinate nf, hypromellose acetate succinate jp, hypromellose acetate succinate, hypromellose phthalate nf, hypromellose phthalate, low-substituted hydroxypropyl cellulose nf, low-substituted hydroxypropyl cellulose jp, low-substituted hydroxypropyl cellulose nf—low-substituted hydroxypropyl cellulose jp copolymer, hypromellose usp, hypromellose ep, hypromellose jp, hypromellose phthalate jp, hypromellose phthalate ep, hypromellose, hypromellose phthalate nf, hypromellose phthalate, low-substituted hydroxypropyl cellulose, methacrylates, cellulose acetate butyrate, polylactide-polyglycolide copolymers, polycaprolactone, polylactide, polyglycolide, polyvinylpyrrolidone-co-vinyl acetate, polyrethanes, polyvinyl caprolactam—polyvinyl acetate—polyethylene glicol graft copolymer, polyvinyl caprolactam, polyvinyl acetate, vinylpyrrolidone—vinyl acetate copolymer, vinyl-pyrrolidone polymer, polyvinylacetate, polyoxyethylene—polyoxypropylene copolymer, polyoxy-ethylene, polyoxypropylene, polyoxirane, povidone, polyethylene oxide, cellulose acetate, copovidone, povidone K12, povidone K17, povidone K25, povidone K30, povidone K90, hypromellose E5, hypromellose E4m, hypromellose K3, hypromellose K100, hypromellose K4m, hypromellose K100m, hypromellose phthalate HP-55, hypromellose phthalate HP-50, hypromellose acetate succinate 1 grade, hypromellose acetate succinate m grade, hypromellose acetate succinate h grade, cellulose acetate phthalate, cationic methacrylate, methacrylic acid copolymer type A, methacrylic acid copolymer type B, methacrylic acid copolymer type C, polymethylacrylates, polyvinyl alcohol, hydroxypropylmethylcellulose acetate succinate, ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate, ethyl acrylate-methyl methacrylate copolymer, butyl/methyl methacrylate-dimethylaminoethyl methacrylate copolymer, butyl/methyl methacrylate, dimethylaminoethyl methacrylate, methacrylic acid-ethyl acrylate copolymer, methacrylic acid, methacrylic acid-methyl methacrylate copolymer, methyl acrylate-methyl methacrylate-methacrylic acid copolymer, methyl acrylate, methyl methacrylate and diethylaminoethyl methacrylate copolymer, methyl methacrylate, diethylaminoethyl methacrylate, succinate, d-α-tocopheryl polyethylene glicol 100 succinate, d-α-tocopheryl polyethylene glicol, ethylene oxide, polypropylene oxide, polyvinyl alcohol-polyethylene glycol graft copolymer, methacrylic acid-ethyl acrylate copolymer, poloxamer, micronized poloxamer, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, ethylene glycol-vinyl alcohol graft copolymer, polydextrose nf, hydrogenated polydextrose nf, methacrylic acid copolymer, methacrylic acid and methyl methacrylate copolymer, methacrylic acid and ethyl acrylate copolymer, carbomer homopolymer, carbomer copolymer, carbomer interpolymer and mixtures thereof. 
     
     
         18 . The composition of  claim 15 , having modified release characteristics and having a particle-size distribution between 250 μm and 425 μm. 
     
     
         19 . The composition of  claim 15 , having modified release characteristics and having a particle-size distribution between 180 μm and 250 μm. 
     
     
         20 . The composition of  claim 15 , having modified release characteristics and having a particle-size distribution between 125 μm and 180 μm. 
     
     
         21 . The composition of  claim 15 , having modified release characteristics and having a particle-size distribution up to 125 μm