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

a technology of diacylglyceride and phytosterol esters, which is applied in the field of lipid mixtures, can solve the problems of reducing cholesterol and triglyceride serum levels, increasing the risk of cvd, and none of the above mentioned publications describes the reduction of both cholesterol and triglyceride levels, so as to reduce the risk of metabolic disorder and/or insulin resistance syndrome, reduce the risk of circulating, and reduce the effect of hdl/l

Inactive Publication Date: 2006-10-19
ENZYMOTEC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0040] Similarly, said pharmaceutical dosage form is intended for the same uses as described above for the mixture of the invention, i.e., in reducing the risk of developing metabolic disorder and/or insulin resistance syndrome; in reducing circulating atherogenic small-dense LDL particles, while maintaining a high proportion of HDL/LDL ratio; in shifting HDL profile in the direction of larger and less dense particles, particularly reducing the HDL3 subfracti

Problems solved by technology

Similarly, it is well known that low levels of HDL cholesterol (HDL-C) are associated with an increased risk for CVD independent of LDL-C levels, and that raising HDL-C

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

example 1

Antioxidative Effect of Olive Oil, Olive Oil+Phytosterols and PSE+DAG in Olive Oil Against Macrophage Lipid Peroxidation in Eo Mice

[0257] As mentioned above, oxidative stress is involved in the pathogenesis of atherosclerosis. Atherosclerosis is associated with lipids peroxidation of plasma LDL and in arterial cells, including macrophages [Aviram M. (2000) Free. Radic. Res. 33:S85-97]. Under oxidative stress, macrophage peroxide levels become increased, and macrophages generate reactive oxygen species, leading to their increased atherogenicity [Aviram M. (2000) id ibid].

[0258] The apolipoprotein E deficient (E0) mice are widely used as an animal model for atherosclerosis as they develop severe hypercholesterolemia and atherosclerotic lesions on a chow diet. Moreover, in E0 mice, accelerated atherosclerosis is associated with increased lipid peroxidation of plasma lipoproteins and arterial cells [Keidar S. (1998) Life Sci. 63:1-11].

[0259] Angiotensin II (Ang-II), a vasoconstricto...

example 2

[0269] The effect of PSE+DAG in canola oil and PSE+DAG in fish oil on the atherogenicity of lipoproteins and macrophages, and on atherosclerosis development in the atherosclerotic apolipoprotein E deficient (Eo) mice model was investigated. Apolipoprotein E deficient (apoEo) mice at 8 weeks of age were assigned randomly to the following groups (5 mice each) as described below. The mice received regular chow diet, and in addition, they were fed (via gavage) the following, once every three days:

Group I:

1. Placebo group: did not receive any addition of oil.

2. Canola oil group (control): were fed with 60 μl of canola oil.

3. PSE+DAG in canola oil group: were fed with 60 μl of PSE+DAG in canola oil.

Group II:

1. Placebo group: did not receive any addition of oil.

2. PSE+DAG in fish oil: were fed with 60 μl of PSE+DAG in fish oil.

[0270] Each mouse consumed approximately 5 mL of water / day, and 5 g of chow / day.

Oil Preparation for Feeding

[0271] The amounts of PSE+DAG in canola ...

example 3

Human Study Comparing PSE+DAG Diet with Control

Change in Total Cholesterol Concentrations

[0282] Supplementation of mildly overweight hypercholesterolemic subjects' diet with PSE+DAG demonstrated a distinct impact on total plasma cholesterol concentrations (P-valueJ.A.M.A. 285:2486-2497], suggesting the desirable total cholesterol levels in healthy individuals to be below 200 mg / dL, the volunteers who consumed the vegetable-oil diet reduced 31% of the total cholesterol levels required to meet the target. However, following PS-E+DAG feeding the serum total cholesterol levels were markedly reduced towards these optimal level inasmuch as 71%.

Change in LDL-Cholesterol Concentrations

[0283] As shown in FIG. 11, the hypocholesterolemic effect of PS-E+DAG was more prominent, as expected, in the reduction of LDL cholesterol plasma levels (from baseline levels of 154±8 mg / dL to endpoint 135±7 mg / dL; P-value=0.0004; while control vegetable oil consumption resulted in a significant effect ...

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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.

Description

CROSS REFERENCE TO RELATED APPLICATION [0001] This application is a Continuation in Part of U.S. patent application Ser. No. 11 / 199,584 filed Aug. 8, 2005, which is a Continuation in Part of International Patent Application No. PCT / IL2004 / 000131 filed Feb. 10, 2004.FIELD OF THE INVENTION [0002] The present invention relates to various lipid mixtures, more particularly special mixtures of fatty acids esters, which may be phytosterol esters and / or glyceride esters, as well as compositions, dietary nutrients, food supplements and nutraceuticals comprising thereof, intended for the treatment and prevention of diseases and conditions associated with lipid metabolism. BACKGROUND OF THE INVENTION [0003] All publications mentioned throughout this application are fully incorporated herein by reference, including all references cited therein. [0004] Coronary Artery Disease (like atherosclerosis) is the major cause of morbidity and mortality in the Western world and its pathogenesis involves c...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K31/22A61K47/00
CPCA23D9/013A23L1/3004A23L1/3008A23V2002/00A61K31/20A61K31/22A61K31/23A61K31/56A61K31/575A61K45/06A61K2300/00A23V2250/182A23V2250/2136A23L33/11A23L33/12A61P3/00
Inventor PLATT, DORITPELLED, DORISHULMAN, AVIDORBEN-DROR, GAI
Owner ENZYMOTEC
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