Solid dispersion of 24-methylene cycloartanol ferulic acid eater and preparation thereof

A pineapple alcohol ferulate and solid dispersion technology, applied in the field of medicine, can solve the problems of unpredictability, poor water solubility, and no solution for 24-methylene pineapple alcohol ferulate solubilization, etc. Good dissolution effect and improved solubility

Active Publication Date: 2011-05-18
BEIJING CENTURY BIOCOM PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the above-mentioned disclosed technical solutions have made some progress in solving the water solubility of oryzanol, the effect is not satisfactory
At the same time, the feasibility of these solutions for the less water soluble 24-methylene cycloartenol ferulate is unpredictable
In terms of the prior art, there is no solubilization scheme for 24-methylene cycloartenyl ferulic acid ester, and the solid dispersion of the present invention has made significant progress on this problem

Method used

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  • Solid dispersion of 24-methylene cycloartanol ferulic acid eater and preparation thereof
  • Solid dispersion of 24-methylene cycloartanol ferulic acid eater and preparation thereof
  • Solid dispersion of 24-methylene cycloartanol ferulic acid eater and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Mix and grind 4g of 24-methylene cycloartenol ferulate and 15g of povidone K30 for 20 minutes, add the obtained ground powder into 80ml of ethanol and stir for 10 minutes, pour the obtained solution into a rotary evaporator, and concentrate it to 10ml Take it out and dry it in an oven, and crush the obtained solid through an 80-mesh sieve to obtain the 24-methylene cycloartenyl ferulic acid ester solid dispersion composition 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 1g of 24-methylenecycloartenyl 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 and passed through 80 mesh Sieve to obtain the solid dispersion of 24-methylene cycloartenol ferulate of the present invention.

Embodiment 3

[0046] Measure 50ml of ethanol, add 20g of povidone K30, 1g of propylene glycol, 1g of 24-methylenecycloartenol ferulate, and 0.2g of egg yolk phospholipid into it, and heat it in a water bath at 50°C to fully stir to dissolve. 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 24-methylenecycloartenyl ferulic acid ester solid dispersion of the present invention.

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Abstract

The invention discloses a solid dispersion of 24-methylene cycloartanol ferulic acid eater, comprising the 24-methylene cycloartanol ferulic acid eater and povidone as a carrier material. The invention further discloses a pharmaceutical preparation and a preparation method of the solid dispersion. Proved by experiments, the solid dispersion makes an obvious technical progress on technical indexes such as dissolution rate, stability, water-solubility, bioavailability and the like.

Description

technical field [0001] The invention discloses a solid dispersion of 24-methylene cycloartenol ferulate, which comprises 24-methylcycloartenyl ferulate and povidone as a carrier, and belongs to the field of medicine. Background technique [0002] Oryzanol is a natural mixture composed of cycloartenol ferulic acid esters and sterol ferulic acid esters. The main two components are cycloartenol ferulic acid esters and 24 - Methyl cycloartenol ferulate, the content of the two in unpurified oryzanol is about 70%, and it is the main active ingredient in oryzanol. Long-term studies have found that oryzanol has a variety of pharmacological activities, such as lowering blood lipids, lowering cholesterol absorption, preventing lipid oxidation, preventing cardiovascular diseases, alleviating various physical obstacles and autonomic nervous disorders in women after menopause, and improving diencephalon function out of tune. [0003] Because oryzanol has a wide range of medicinal effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/48A61K9/20A61K9/16A61K9/14A61K31/575A61K47/32A61P3/06A61P15/12A61P25/00
Inventor 郝守祝王雷波
Owner BEIJING CENTURY BIOCOM PHARMA TECH
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