Oils enriched with diacylglycerols and phytosterol esters and unit dosage forms thereof for use in therapy

Abstract

Described herein are various lipid mixtures, more particularly special mixtures of fatty acids esters, which may be phytosterol esters and/or glyceride esters. Said mixtures are evaluated in the context of their ability to, upon consumption, affect the levels of circulating LDL and HDL particles, and their therapeutic effect on conditions associated with lipid metabolism, such as atherosclerosis, diabetes, metabolic disorders, etc. Compositions, dietary nutrients, food supplements and nutraceuticals comprising the herein described mixtures are also described.

1 . An edible mixture of esters of long chain polyunsaturated fatty acids (LC-PUFA), said mixture comprising esters of LC-PUFA with phytosterols and/or phytostanols and esters of LC-PUFA with glycerol, optionally also comprising free phytosterols and/or phytostanols, wherein the weight ratio of said LC-PUFA glycerol esters to their esters with phytosterol or phytostanol is from about 19:1 to about 1.5:1.  
   
   
       2 . A mixture of  claim 1 , wherein said esters of LC-PUFA with glycerol are mono-, di- and/or triglycerides.  
   
   
       3 . The mixture of  claim 1 , for use in reducing the risk of developing metabolic disorder and/or insulin resistance syndrome.  
   
   
       4 . The mixture of  claim 1 , for use in reducing circulating atherogenic small-dense LDL particles, while maintaining a high proportion of HDL/LDL ratio.  
   
   
       5 . The mixture of  claim 1 , for use in shifting HDL profile in the direction of larger and less dense particles, particularly reducing the HDL 3  subfraction while increasing the level of HDL 2  subfraction.  
   
   
       6 . The mixture of  claim 1 , for use in reducing and/or preventing the progression of the metabolic disorder and/or insulin resistance syndrome and/or atherosclerotic deleterious processes.  
   
   
       7 . The mixture of  claim 1 , for use in attenuating or counteracting any adverse effects of use of omega-3 fatty acids in the form of oils.  
   
   
       8 . The mixture of  claim 7 , wherein said adverse effect may be elevating LDL cholesterol or increasing the total/HDL cholesterol ration, related to a decrease in HDL cholesterol levels.  
   
   
       9 . An edible composition of matter comprising a mixture of esters of LC-PUFA with glycerol, enriched with a mixture of esters of LC-PUFA with phytosterols and/or phytostanols, wherein said mixture of esters LC-PUFA with glycerol is derived from any one of animal source, particularly fish oil, plant, algae and microorganisms, and wherein the weight ratio of said LC-PUFA glycerol esters to their esters with phytosterol or phytostanol is from about 1.5:1 to about 1:9.  
   
   
       10 . The composition of matter of  claim 9 , for use in reducing the risk of developing metabolic disorder and/or insulin resistance syndrome.  
   
   
       11 . The composition of matter of  claim 9 , for use in reducing circulating atherogenic small-dense LDL particles, while maintaining a high proportion of HDL/LDL ratio.  
   
   
       12 . The composition of matter of  claim 9 , for use in shifting HDL profile in the direction of larger and less dense particles, particularly reducing the HDL 3  subfraction while increasing the level of HDL 2  subfraction.  
   
   
       13 . The composition of matter of  claim 9 , for use in reducing and/or preventing the progression of the metabolic disorder and/or insulin resistance syndrome and/or atherosclerotic deleterious processes.  
   
   
       14 . The composition of matter of  claim 9 , for use in attenuating or counteracting any adverse effects of use of omega-3 fatty acids in the form of oils.  
   
   
       15 . The composition of matter of  claim 14 , wherein said adverse effect may be elevating LDL cholesterol or increasing the total/HDL cholesterol ration, related to a decrease in HDL cholesterol levels.  
   
   
       16 . An orally administrable pharmaceutical or nutraceutical unit dosage form comprising an edible mixture of esters LC-PUFA with glycerol, enriched with a mixture of esters of LC-PUFA with phytosterols and/or phytostanols, wherein said unit dosage form contains about 1.4-1.6 g of said phytosterol/phytostanol LC-PUFA esters, said dosage form being capable of providing at least 50% of the recommended daily intake (RDI) of phytosterols and the recommended daily intake of LC-PUFA.  
   
   
       17 . The pharmaceutical dosage form of  claim 16 , in the form of a capsule, preferably a soft gel capsule.  
   
   
       18 . The pharmaceutical dosage form of  claim 16 , wherein said RDI of phytosterols is from about 0.4 g to about 0.8 g and said RDI of LC-PUFA, specifically, DHA and EPA, is from about 0.3 g to about 0.65 g.  
   
   
       19 . The pharmaceutical dosage form of  claim 16 , for use in reducing the risk of developing metabolic disorder and/or insulin resistance syndrome.  
   
   
       20 . The pharmaceutical dosage form of  claim 16 , for use in reducing circulating atherogenic small-dense LDL particles, while maintaining a high proportion of HDL/LDL ratio.  
   
   
       21 . The pharmaceutical dosage form of  claim 16 , for use in shifting HDL profile in the direction of larger and less dense particles, particularly reducing the HDL 3  subfraction while increasing the level of HDL 2  subfraction.  
   
   
       22 . The pharmaceutical dosage form of  claim 16 , for use in reducing and/or preventing the progression of the metabolic disorder and/or insulin resistance syndrome and/or atherosclerotic deleterious processes.  
   
   
       23 . The pharmaceutical dosage form of  claim 16 , for use in attenuating or counteracting any adverse effects of use of omega-3 fatty acids in the form of oils.  
   
   
       24 . The pharmaceutical dosage form of  claim 23 , wherein said adverse effect may be elevating LDL cholesterol or increasing the total/HDL cholesterol ration, related to a decrease in HDL cholesterol levels.  
   
   
       25 . The pharmaceutical dosage form of  claim 16 , for twice daily administration.  
   
   
       26 . A method of treatment of metabolic syndrome and related conditions, said method comprising administering a therapeutically effective dose of an edible mixture of esters of LC-PUFA or compositions comprising thereof to a subject in need, wherein said mixture comprises esters of LC-PUFA with phytosterols and/or phytostanols and esters of LC-PUFA with glycerol, wherein the weight ratio of said LC-PUFA glycerol esters to their esters with phytosterol or phytostanol is from about 19:1 to about 1:9.  
   
   
       27 . The method of  claim 26 , wherein said effective dose is comprised in a soft gelatine capsule, said method comprising administering said capsule to said patient twice daily.  
   
   
       28 . A method of reducing circulating atherogenic small-dense LDL particles, while maintaining a high proportion of HDL/LDL ratio, said method comprising administering a therapeutically effective dose of an edible mixture of esters of LC-PUFA or compositions comprising thereof to a subject in need, wherein said mixture comprises esters of LC-PUFA with phytosterols and/or phytostanols and esters of LC-PUFA with glycerol, wherein the weight ratio of said LC-PUFA glycerol esters to their esters with phytosterol or phytostanol is from about 19:1 to about 1:9.  
   
   
       29 . The method of  claim 28 , wherein said effective dose is comprised in a soft gelatine capsule, said method comprising administering said capsule to said patient twice daily.  
   
   
       30 . A method of shifting the HDL profile in the direction of larger and less dense particles, particularly reducing the HDL 3  subfraction while increasing the level of HDL 2  subfraction, said method comprising administering a therapeutically effective dose of an edible mixture of esters of LC-PUFA or compositions comprising thereof to a subject in need, wherein said mixture comprises esters of LC-PUFA with phytosterols and/or phytostanols and esters of LC-PUFA with glycerol, wherein the weight ratio of said LC-PUFA glycerol esters to their esters with phytosterol or phytostanol is from about 19:1 to about 1:9.  
   
   
       31 . The method of  claim 30 , wherein said effective dose is comprised in a soft gelatine capsule, said method comprising administering said capsule to said patient twice daily.