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Cycloartenyl ferulate solid dispersion and preparation thereof

A technology of pineapplenyl ferulic acid ester and solid dispersion, which is applied in the field of medicine and can solve the problems of poor bioavailability and low solubility of cycloartenyl ferulic acid ester monomer

Active Publication Date: 2012-08-22
BEIJING CENTURY BIOCOM PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with oryzanol raw materials, cycloartenol ferulate monomer has lower solubility and poorer bioavailability
No studies in the prior art have addressed the issue of improving the dissolution and bioavailability of cycloartenol ferulate

Method used

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  • Cycloartenyl ferulate solid dispersion and preparation thereof
  • Cycloartenyl ferulate solid dispersion and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Mix and grind 4g cycloartenol ferulate and 15g povidone K30 for 20min, add the obtained ground powder into 80ml ethanol and stir for 10min, pour the obtained solution into a rotary evaporator, concentrate it to 10ml, and take it out in an oven After drying, the obtained solid is pulverized and passed through an 80-mesh sieve to obtain the solid dispersion of cycloartenol ferulate of the present invention.

Embodiment 2

[0044] Measure 150ml of ethyl acetate, add 7g of povidone K90 into it and shake to dissolve fully. Then add 1 g of cycloartenol ferulic acid ester, heat and stir at 70°C for about 15 minutes, pour the resulting solution into a rotary evaporator, and when concentrated to 20ml, take it out and dry it in an oven. The obtained solid is crushed through a 80-mesh sieve to obtain The cycloartenol ferulic acid ester solid dispersion of the present invention.

Embodiment 3

[0046] Measure 50ml of ethanol, add 20g of povidone K30, 1g of propylene glycol, 1g of cycloartenyl ferulic acid ester, and 0.2g of egg yolk phospholipid into it, and heat it in a water bath at 50°C and fully stir to dissolve it. The obtained solution was poured into a rotary evaporator, and when concentrated to 15 ml, it was taken out and dried in an oven, and the obtained solid was pulverized and passed through an 80-mesh sieve to obtain the cycloartenol ferulic acid ester solid dispersion of the present invention.

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Abstract

The invention discloses cycloartenyl ferulate solid dispersion, which comprises cycloartenyl ferulate and povidone serving as a carrier material. The invention further discloses a medicinal preparation and a preparation method of the solid dispersion. Experiments prove that the solid dispersion makes obvious technical progress in technical indexes such as dissolution rate, stability, water solubility, bioavailability and the like.

Description

technical field [0001] The invention discloses a solid dispersion of cycloartenol ferulate, which comprises cycloartenol ferulate and povidone as a carrier, and belongs to the field of medicine. Background technique [0002] Oryzanol is a natural mixture composed of cycloartenol-based ferulic acid esters and sterol-based ferulic acid esters, and its appearance is white or light yellow crystalline powder. In rice bran oil oryzanol, the content of cycloartenol ferulate is about 70-80%. Long-term studies have found that oryzanol has a variety of pharmacological activities, including: lowering blood lipids, lowering cholesterol absorption, preventing lipid oxidation, and preventing cardiovascular diseases. In addition, recent studies have also found that oryzanol can alleviate various physical disorders and autonomic nervous disorders in women after menopause, and improve diencephalic dysfunction. [0003] Oryzanol is easily soluble in organic solvents such as chloroform and a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/48A61K47/32A61K31/575A61P3/06A61P9/00A61P15/12
Inventor 郝守祝王雷波
Owner BEIJING CENTURY BIOCOM PHARMA TECH
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