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Polymer-coated oleanolic acid liposome and preparation method thereof

A technology of oleanolic acid and polymers, applied in the field of medicine, can solve the problems of poor solubility and dissolution rate, limited dissolution and absorption, poor oral absorption of OA, etc., to improve stability, promote transmembrane absorption, and facilitate packaging Effect

Inactive Publication Date: 2013-11-06
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

OA is mainly absorbed by passive diffusion, but its solubility and dissolution rate in water are extremely poor, and the apparent permeability coefficient of intestinal cells (Caco-2 monolayer cells) is only 1.1×10 -6 -1.3×10 -6 cm / s, thus limiting its dissolution and absorption in the gastrointestinal tract, resulting in poor oral absorption of OA, and the absolute bioavailability in rats is only 0.7%

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 A polymer-coated oleanolic acid liposome and a preparation method thereof, which comprises the following steps:

[0020] Using the ethanol injection method, take 0.1g of oleanolic acid, 2g of soybean lecithin, 0.5mg of cholesterol, and 800.1g of Tween dissolved in ethanol as the oil phase, so that the drug and lipid are completely dissolved, and quickly drop into the liquid under constant temperature stirring. In 50ml of mannitol phosphate buffer solution (5%, w / v, pH 6.8), keep stirring at constant temperature (50±2°C) until ethanol evaporates completely. Ultrasonic treatment (ultrasonic power 80%, ultrasonic time 4min) under the condition of ice-water bath, obtains oleanolic acid liposome suspension. Slowly drop the prepared suspension into 50ml of trimethyl chitosan phosphate buffer (1%, w / v) with a quaternary ammonium degree of 65%, and stir and mix for 60 minutes at 10°C to obtain trimethyl chitosan Glycan-coated oleanolic acid liposome suspension was sp...

Embodiment 2

[0021] Example 2 A polymer-coated oleanolic acid liposome and a preparation method thereof, comprising the following steps:

[0022] Using the film dispersion method, take 0.3g of oleanolic acid, 4.1g of soybean lecithin, 2g of cholesterol, 800.06g of Tween, and 1880.07g of poloxamer dissolved in ethanol as the oil phase, and evaporate to dryness at 35°C using a rotary evaporator. Remove the ethanol from the membrane, stop the rotation and keep the vacuum for 2 hours, then stop, add 50ml of dextran phosphate buffer solution (5%, w / v, pH6.8), shake vigorously for 40min, wash the membrane at 4°C Homogenize with a high pressure homogenizer (homogenization pressure 80Mpa, cycle times 5 times) to obtain oleanolic acid liposome suspension. Slowly drop the prepared suspension into 50ml of carboxymethyl chitosan phosphate buffer (1%, w / v), stir and mix at 10°C for 60min to obtain carboxymethyl chitosan-coated oleoresin Fruit acid liposome suspension, prepared by spray drying (inlet a...

Embodiment 3

[0023] Example 3 A polymer-coated oleanolic acid liposome and a preparation method thereof, comprising the following steps:

[0024] Using the reverse phase evaporation method, take 3.5g of egg yolk lecithin and 0.9g of cholesterol dissolved in ether as the oil phase, add 3.1ml of lactose and mannitol (1:1, w / w) mixed phosphate buffer solution, and ultrasonicate for 5min to obtain For the emulsion, use a rotary evaporator at 25°C to remove ether to a colloidal state, add 7ml of ethanol solution containing 0.2g oleanolic acid, and evaporate to dryness at 35°C, stop the rotation and keep vacuuming for 2 hours, then stop, add lactose, Mix mannitol (1:1, w / w) in 50ml of phosphate buffer (5%, w / v, pH 6.8), shake vigorously for 40min, wash the membrane and sonicate it in an ice-water bath (ultrasonic power 80%, ultrasonic time 4min), that is, oleanolic acid liposome suspension. Slowly drop the prepared suspension into 50ml of cyclodextrin-containing phosphate buffer (7%, w / v), stir...

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Abstract

The invention belongs to the technical field of medicine and relates to a polymer-coated oleanolic acid liposome and a preparation method thereof. The preparation method comprises the following steps of preparing an oleanolic acid liposome suspension, adding a polymer into the oleanolic acid liposome suspension, carrying out coating to obtain a polymer-coated oleanolic acid liposome suspension, and carrying out spray drying or freeze drying to obtain polymer-coated oleanolic acid liposome powder, wherein before use, hydration reconstruction is carried out according to requirements. The polymer-coated oleanolic acid liposome utilizes long-circulating characteristics, biological adhesion and penetration promotion of the coating material, improves drug encapsulation efficiency and liposome stability, prolongs in-vivo residence and cycle time of particulates, promotes intercellular transmembrane transport of the particulates, improves oral bioavailability of oleanolic acid, is processed into solid powder, and is convenient for package, storage, transport and use.

Description

technical field [0001] [0002] The invention belongs to the technical field of medicine, and relates to a polymer-coated oleanolic acid liposome and a preparation method thereof. Background technique [0003] Oleanolic acid (OA) is widely distributed in nature and is a pentacyclic triterpenoid compound. It is an effective active monomer extracted from natural plants and exists in free form or in the form of glycosides. OA can improve the structure and function of liver cells, inhibit the formation of lipid peroxidation in the mitochondria of liver cells, and has been clinically used as an OTC drug for adjuvant treatment of liver diseases for acute chemical liver injury, chronic liver cirrhosis and liver fibrosis, and also has two-way immune regulation and anti-cancer pharmacological effects. OA is mainly absorbed by passive diffusion, but its solubility and dissolution rate in water are extremely poor, and the apparent permeability coefficient of intestinal cells (Caco-2 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/56A61P1/16A61P37/02A61P35/00
Inventor 张婧廖正根李翔罗云
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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