Application of lipid-modified substance of chlorogenic acid and derivative thereof

Abstract

The invention provides a lipid-modified substance of chlorogenic acid and a derivative thereof, and a preparation and purification method of the lipid-modified substance, wherein the lipid-modified substance includes the chlorogenic acid or the derivative thereof and phosphoglyceride. A preparation process includes steps of performing constant-temperature magnetic stirring reflux for a certain time to the chlorogenic acid or the derivative thereof and the phosphoglyceride with an aprotic solvent and drying an obtained reaction liquid to obtain a crude product. A purification process includes the steps of re-dissolving the crude product with filtration to obtain a filtrate and then drying the filtrate. The lipid-modified substance of the chlorogenic acid and the derivative thereof is high in composition rate and can significantly improve the fat-solubility of the chlorogenic acid and the derivative thereof, so that a subsequent preparation is convenient to process and shape. The lipid-modified substance can be used as an intermediate for preparing a lipidosome, nano particles, polymer micelles or a dendritic polymer and the like nano drug-delivery systems and micro emulsion, self-micro emulsion and the like micron drug-delivery systems, thereby enhancing in-vivo absorption of the chlorogenic acid and the derivative thereof and further increasing the bioavailability of the medicines in a preparation.

Description

technical field [0001] The invention relates to a lipid modification of chlorogenic acid and its derivatives and a preparation and purification method thereof, belonging to the technical field of medicine. Background technique [0002] Chlorogenic acid (ChA), also known as coffee tannin, is an ester formed by condensation of caffeic acid (CA) and quinic acid (quinic acid, QA), and belongs to polyphenols compounds with a wide range of biological activities. Its sources are mainly the dried flower buds or flowers with early blooming of honeysuckle, honeysuckle, red gland honeysuckle, mountain silver flower or hair style honeysuckle, leaves of Eucommia ulmoides, fruit of Rosaceae hawthorn, and the fruit of Rosaceae Hawthorn. Cauliflower plant, Sapinaceae plant willow, Eurasian water keel root, Verbenaceae plant Pseudomonas root, Brassicaceae plant cabbage stems and leaves, Polygonaceae plant flat-planted whole plant and Rubiaceae plant Pompeo Vegetables and other herbs. [0...

AI Technical Summary

Problems solved by technology

[0008] The present invention aims at chlorogenic acid and its derivatives due to their good polarity, poor membrane permeability, low bioavailability during administration, and being easily decomposed by various digestive enzymes in the gastrointestinal tract, which limits the development of oral preparations, etc. To solve the problem, prepare a lipid modification of chlorogenic acid and its derivatives, namely phospholipid complex, to improve the lipophilicity of the drug, enhance its affinity with cells in the body, increase the bioavailability of the drug when it acts, and provide The processing and shaping of subsequent formulations provides easier to handle intermediates

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