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Conjugates of phytosterol or phytostanol with ascorbic acid and use thereof in treating or preventing cardiovascular disease

A technology of plant stanols and plant sterols, applied in the application field of treating and preventing cardiovascular diseases and other diseases

Inactive Publication Date: 2002-09-18
FORBES MEDI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the intent of this patent is to produce a soluble stable phytosterol delivery system, there are some problems with the long-term stability of these "fatty acid" esterified products due to the eventual oxidation of the unsaturated fatty acid moiety

Method used

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  • Conjugates of phytosterol or phytostanol with ascorbic acid and use thereof in treating or preventing cardiovascular disease
  • Conjugates of phytosterol or phytostanol with ascorbic acid and use thereof in treating or preventing cardiovascular disease
  • Conjugates of phytosterol or phytostanol with ascorbic acid and use thereof in treating or preventing cardiovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0130] Example 1 - Protection of Ascorbic Acid

[0131] Fuming sulfuric acid (24%, 8.3 g) was added dropwise to acetone (50 mL). Ascorbic acid (12 g) was added to the mixture at 0°C, and the reaction mixture was stirred at 0°C for 6 hours. The resulting crystals were filtered off with suction, the filter cake was pressed dry and washed with acetone (30 ml). The product was obtained as 5,6-isopropylidene-ascorbic acid (14 g).

Embodiment 2

[0132] Example 2 - Linkage of Phytostanols

[0133] A solution of toluene (500 ml) and pyridine (25 ml) containing phytostanol mixture (24 g) (camesteranol: 36.4%; sitostanol: 62.3%) was added dropwise to 0°C containing phosphorus oxychloride ( 9 ml) in a mixture of toluene (200 ml). The mixture was stirred at room temperature for 3 hours. Pyridine hydrochloride was removed by filtration, the mother liquor was concentrated, and toluene was recovered. The residue was dissolved in dry THF (100 mL), and a solution of the above-prepared protected ascorbic acid (14 g) in dry THF (400 mL) was added at 0°C. Stirring was maintained at room temperature for 1 hour. The solution was concentrated and the solvent was removed. Ethanol (400 mL) and 3N HCl (200 mL) were added, the mixture was heated at 50°C for 30 minutes and concentrated. Ethyl acetate (600 mL) was added and the resulting solution was washed with water (3 x 300 mL), dried over sodium sulfate and concentrated to give the...

Embodiment 3

[0134] Example 3 - Conversion to sodium salt

[0135] The above-prepared acid (17 g) was dissolved in ethanol (100 ml), and a solution of sodium methoxide (2.7 g) in ethanol (50 ml) was added with stirring at room temperature. Stirring was maintained for 30 minutes. After the addition, the obtained white filter cake was filtered out, dried and weighed to obtain 20 g of white powder (phytostanol-phosphate-sodium ascorbate).

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PUM

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Abstract

New phytosterols and / or phytostanol derivatives, including salts thereof, represented by general formulas (I), (II), (III), wherein R is a phytosterol or phytostanol part, and R2 is derived from ascorbic acid , R3 is hydrogen or any metal, alkaline earth metal or alkali metal. These derivatives are effective in the treatment and prevention of cardiovascular diseases and their underlying conditions, including atherosclerosis and hyperlipidemia.

Description

field of invention [0001] The present invention relates to the field of phytosterols and phytostanols and their application in the treatment and prevention of cardiovascular diseases and other diseases. Background of the invention [0002] Although recent scientific and technological advances have helped to improve the quality of human life and extend human lifespan, the problem of preventing atherosclerosis, the underlying cause of cardiovascular disease ("CVD"), has not been fully resolved. Atherosclerosis is a degenerative process caused by the interplay of intrinsic (genetic) and environmental factors such as diet and lifestyle. Research so far suggests that cholesterol may play a role in atherosclerosis, where it forms atherosclerotic plaques in blood vessels that eventually cut off blood supply to the heart muscle or the brain or extremities, depending on where the plaque is in the arterial network (1, 2). It has been observed that a 1% reduction in human total serum...

Claims

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Application Information

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IPC IPC(8): A23L1/30A23L33/15A61K31/375A61K31/575A61K31/58A61K31/59A61K31/6615A61P3/06A61P9/10A61P43/00C07J9/00C07J17/00C07J51/00
CPCA23V2002/00A61K31/375A61K31/575C07J17/00C07J51/00A23L33/11A23L33/15A61P3/06A61P43/00A61P9/10A61K2300/00A23V2250/708A23V2250/2136
Inventor J·P·库托尼丁岩冰陈宏明侯端杰R·K·米拉诺瓦
Owner FORBES MEDI TECH
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