Check patentability & draft patents in minutes with Patsnap Eureka AI!

Liver targeted auxiliary material containing D-glactose and sterol and its use

A technology for excipients and galactose, applied in the field of medicine, can solve problems such as structure and molecular weight uncertainty, and achieve the effect of simple reaction process

Inactive Publication Date: 2010-04-28
沈阳药科大学科技产业集团有限公司
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this polymer has the disadvantage of uncertain structure and molecular weight.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Liver targeted auxiliary material containing D-glactose and sterol and its use
  • Liver targeted auxiliary material containing D-glactose and sterol and its use
  • Liver targeted auxiliary material containing D-glactose and sterol and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The target compound is obtained by synthesizing ethylenediamine monolactose acid acylate and reacting with cholesterol succinate.

[0031] 1. Synthesis of Ethylenediamine Monolactose Acylate (LA-ED)

[0032] Take 5 g of lactobionic acid and add 50 mL of methanol to dissolve, evaporate under reduced pressure at 50°C to remove methanol, and repeat 5 times to obtain lactobionic acid lactone. Add 7.5g of ethylenediamine (ED) into a 250mL three-necked flask, add 50mL of methanol, heat to reflux at 60°C, and magnetically stir; add the methanol solution of lactobionolactone dropwise, and the dropwise addition is completed within 60min. The stirring reaction was continued at reflux temperature for 5h. The reaction mixture was concentrated under reduced pressure, dichloromethane was added under vigorous stirring, filtered under reduced pressure, and washed with ether to obtain a white solid, namely LA-ED (5.03 g, yield 90.11%).

[0033] 2. Synthesis of Cholesterol Succinate (CHS...

Embodiment 2

[0040] The target compound is obtained by synthesizing the acylate of ethylenediamine monocholesterol succinate and reacting with lactobionolactone.

[0041] 1. (5-Cholesten-3β-ol) 4-oxo-4-(2-aminoethylamino) butyrate ((5-Cholesten-3β-yl) 4-oxo-4-(2- Synthesis of amido ethylamido) butanoate, CHS-ED)

[0042] NHS-CHS 6g was dissolved in dichloromethane, added ethylenediamine 6g, stirred under ice bath for 24h, filtered off the precipitate, removed the solvent under reduced pressure, added water and stirred, precipitate appeared, filtered to obtain the product CHS-ED (4.85g, yield 89.25%).

[0043] 2. (5-Cholesten-3β-ol) 4-oxo-4-[2-(lactosylamino) ethylamino] butyrate ((5-Cholesten-3β-yl) 4-oxo-4 -Synthesis of [2-(lactobionyl amido)ethylamido]butanoate, CHS-ED-LA)

[0044] Take 0.75 g of lactobionic acid and add 50 mL of methanol to dissolve, evaporate under reduced pressure at 50°C to remove methanol, and repeat 5 times to obtain lactobionic acid lactone. Add 1.06 g of lact...

Embodiment 3

[0046] Preparation and in vivo distribution of doxorubicin liver targeting liposome

[0047] Doxorubicin (doxorubicin) is an anthracycline antineoplastic drug commonly used in clinical practice. It has a broad antitumor spectrum and good curative effect. However, while the drug kills tumor cells, it also produces severe adverse reactions, such as cardiotoxicity, bone marrow suppression, etc. The therapeutic index is low, and its clinical application is limited. The liver-targeting liposome prepared by the material of the invention can increase the concentration of the drug in the liver, so as to improve the effect of anti-liver cancer.

[0048] Preparation of liposomes:

[0049] Prescription composition: hydrogenated soybean lecithin (HSPC) 5g, cholesterol (CH) 1.7g, targeting excipient (CHS-ED-LA) 1g, ammonium sulfate 3.3g, doxorubicin 100mg, a total of 100mL.

[0050] Add the prescribed amount of HSPC, CH, CHS-ED-LA into the configuration container, dissolve with an approp...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

A liver-targeting auxiliary containing D-galactose and sterol for preparing the medicine carrier (liposome or nanocyst) is prepared through dissolving lactobionic acid in methanol, evaporating methanol to obtain lectone lactobionate, dissolving in methanol, adding it to ethyldiamine, concentrating, adding bichloromethane, vacuum filtering, washing to obtain acrylated ethyldiamine-monolactobionate,dissolving cholesterol and succinic anhydride in dichloromethane, refluxing, removing solvent, recrystallizing to obtain cholesterol succinate, adding CHS, N-hydroxy succinimide and N,N-dicyclohexylcarbodiimide in tetrahydrofuran, reacting in ice bath while stirring, filtering to remove deposit and vacuum removing of solvent.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular it is a liver-targeted auxiliary material containing D-galactose and sterol and its application in preparation. Background technique: [0002] The liver is one of the most critical organs in the human body, participating in many processes such as digestion, excretion, detoxification and immune regulation in the body. Therefore, the liver is also one of the most vulnerable organs, such as viral hepatitis, cirrhosis and primary liver cancer. Since the 1990s, the mortality rate of liver cancer in my country has risen to the second place in cancer deaths, second only to lung cancer. In Japan, France, Italy and even the United States, especially in men, the incidence of liver cancer is on the rise. Hepatocyte carcinoma accounts for more than 90% of primary liver cancer in my country. It is now known that hepatitis B is closely related to liver cancer, followed by hepatitis C identif...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/28A61P1/16C07J9/00
Inventor 王绍宁邓意辉陈大为
Owner 沈阳药科大学科技产业集团有限公司
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com