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Method for preparing diosmetin derivative ultrafine particles

A technology of diosmin and ultrafine particles, which is applied in educts, bulk chemical production, organic chemistry, etc., can solve the problems of limited development and promotion, small compound range, etc., and achieve improved dissolution performance, uniform distribution, and particle size small effect

Active Publication Date: 2021-03-16
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, the range of compounds applicable to supercritical fluid enhanced solution dispersion technology is very small, and most compounds cannot be prepared into shaped ultrafine particles by this method, which also limits its development and promotion
[0006] Currently, there are no prior art reports on the application of supercritical fluid-enhanced solution dispersion technology for 7-O-prenyl-3'-O-methyldiosmin and 7-O-farnesenyl-3'-O- Preparation of Methylgeranin Ultrafine Particles

Method used

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  • Method for preparing diosmetin derivative ultrafine particles
  • Method for preparing diosmetin derivative ultrafine particles
  • Method for preparing diosmetin derivative ultrafine particles

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Example 1: Single factor investigation of the influence of various factors on the particle size and recovery rate of diosmin derivative ultrafine particles

[0039] Single factor experiment: Effect of solvent type on particle size of ultrafine particles of diosmin derivatives

[0040] Ethanol and ethanol-DMSO with a volume ratio of 50:1, 20:1, and 10:1 were used as solvents for the derivatives, and other parameters were crystallization pressure 11MPa, crystallization temperature 35°C, solution mass concentration 9mg / mL, solution volume Flow 1.0mL / min, CO 2 The flow rate is 3.0-3.5L / min. The diosmin derivative 1 could not obtain shaped ultrafine particles under the above solvent conditions, and the diosmin derivative 2 could obtain shaped ultrafine particles when the solvent was ethanol-DMSO at a volume ratio of 20:1.

[0041] Therefore, other parameters were optimized with the goal of diosmin derivative 2, and ethanol-DMSO with a volume ratio of 20:1 was selected as t...

Embodiment 2

[0052] Example 2: Preparation of diosmin derivative 2 ultrafine particles using optimal process conditions

[0053] The application of supercritical fluid enhanced solution dispersion technology to prepare diosmin derivative 2 ultrafine particles comprises the following steps:

[0054] Step S1, dissolving diosmin derivative 2 in an organic solvent to obtain a compound solution;

[0055] Step S2, adjust the temperature of the crystallization tank to the experimental value, and then add CO 2 Pass into the crystallization kettle, and pressurize to set experimental value;

[0056] Step S3, continue to feed CO 2 , maintaining the temperature and pressure in the crystallization tank constant, while passing the compound solution prepared in step S1 into the crystallization tank;

[0057] Step S4, after the compound solution is passed through, continue to pass through CO 2 65min, while adjusting the CO through the rotameter 2 The flow rate is maintained within a certain flow rate...

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Abstract

The invention discloses a method for preparing diosmetin derivative ultrafine particles, the diosmetin derivative is 7-O-farnesenyl-3'-O-methyl diosmetin, and the method comprises the following steps:step S1, dissolving the diosmetin derivative in an organic solvent to obtain a compound solution; S2, adjusting the temperature of the crystallization kettle to an experimental value, introducing CO2into the crystallization kettle, and pressurizing to a set experimental value; S3, continuously introducing CO2, keeping the temperature and the pressure in the crystallization kettle unchanged, andintroducing the compound solution into the crystallization kettle; and S4, after the compound solution is completely introduced, continuously introducing CO2, meanwhile, adjusting the flow rate of CO2through a rotor flow meter to be maintained within a certain flow rate range, finally, relieving the pressure to standard atmospheric pressure, taking down and opening the crystallization kettle, andcollecting ultrafine particles. According to the method, the 7-O-farnesenyl-3'-O-methyl diosmetin with smaller particle size and more uniform distribution can be obtained so that the bioavailabilityof the diosmetin is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical engineering, and in particular relates to a method for preparing ultrafine particles of diosmin derivatives. Background technique [0002] Dioxynignin and its derivatives have a wide range of biological activities. Cai Shuanglian et al designed and synthesized a variety of diosmin derivatives, including 7-O-isopentenyl-3'-O-methyldiosmin and 7-O-farnesenyl-3' with the following chemical structures -O-Methylgeranin (synthesis and biological activity of natural flavonoids and their derivatives, Organic Chemistry, 2012, 32, 560~566). Recent studies have found that these two compounds have good biological activity. However, these two compounds have poor water solubility, poor dissolution performance, and low bioavailability, which will limit their application in disease treatment and clinical practice. [0003] [0004] Supercritical Fluid Enhanced Solution Dispersion Technology (Solution Enhanced ...

Claims

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Application Information

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IPC IPC(8): C07D311/30
CPCC07D311/30Y02P20/54Y02P20/141
Inventor 王志祥王聪聪贺双杨照
Owner CHINA PHARM UNIV
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