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
CN112500385AActive Publication Date: 2021-03-16CHINA PHARM UNIV

Patent Information

Authority / Receiving Office
CN Β· China
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2021-03-16

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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.
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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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