Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Mebendazole lipid compound, preparation method and application

A technology of mebendazole lipid and mebendazole, which is applied in the field of mebendazole lipid complex and its preparation, can solve the problems of demulsification, emulsion droplet aggregation, low drug loading concentration, etc., and achieve the effect of improving fat solubility

Pending Publication Date: 2021-11-09
TIANJIN AGRICULTURE COLLEGE
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the fat solubility of mebendazole is also very low, and it is basically insoluble in commonly used oil phase solvents (such as soybean oil, medium chain oil, etc.). In the process of sterilization and storage, it is easy to cause adverse phenomena such as demulsification and milk droplet aggregation
[0005] Through the search, no patent publications related to the patent application of the present invention have been found

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
  • Mebendazole lipid compound, preparation method and application
  • Mebendazole lipid compound, preparation method and application
  • Mebendazole lipid compound, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0038] The preparation method of the above-mentioned Mbz lipoplex, the steps are as follows:

[0039] a. Weigh the mebendazole and the lipid material respectively according to the composite ratio, add the organic solvent to dissolve respectively, and mix the above two evenly;

[0040] b. After compounding at a suitable temperature for a period of time, the organic solvent is removed and vacuum-dried to obtain the mebendazole-lipid complex.

[0041] Preferably, the organic solvent is selected from one of methylene chloride, methanol, ethanol, benzyl alcohol, acetone, ethyl acetate, tetrahydrofuran, petroleum ether, tert-butanol, n-octanol, dimethylformamide or Various; preferably, one or more selected from dichloromethane, methanol, tetrahydrofuran, and acetone.

[0042] Preferably, one or more of formic acid, glacial acetic acid, sulfuric acid, trifluoroacetic acid, phosphoric acid and trinitrobenzenesulfonic acid are added to the organic solvent.

[0043] Preferably, the me...

Embodiment 1

[0054] Example 1 Preparation of mebendazole phospholipid complex containing soybean lecithin in different proportions

[0055] Weigh 0.1 g of 10 parts of mebendazole independently into conical flasks, add 100 ml of methanol solution (containing 10% formic acid, v / v), and fully dissolve. Separately weigh soybean lecithin 0.27, 0.54, 0.81, 1.08, 1.35, 1.62, 1.89, 2.16, 2.43, 2.70g into a beaker, add 20ml of dichloromethane to dissolve completely, then add it into the mebendazole solution in order, and ultrasonicate at 20°C 2 hours. Transfer to a rotary evaporator, remove the solvent by rotary evaporation at 40°C, and dry under reduced pressure at room temperature for 12 hours to obtain 10 groups of composite powders with a molar ratio of mebendazole:phospholipids of 1:1-1:10.

Embodiment 2

[0056] Example 2 Preparation of Mebendazole Lipid Complex Containing Different Proportions of Cholesterol

[0057] Weigh 0.1 g of 10 parts of mebendazole independently into conical flasks, add 100 ml of methanol (containing 1% trifluoroacetic acid, v / v), and fully dissolve. Separately weigh 0.13, 0.26, 0.39, 0.52, 0.65, 0.78, 0.91, 1.04, 1.17, and 1.30g of cholesterol into a beaker, add 20ml of tetrahydrofuran to dissolve completely, then add it to the mebendazole solution in sequence, and ultrasonicate for 1 hour at 20°C Let stand for 12 hours. Transfer to a rotary evaporator, remove the solvent by rotary evaporation at 500°C, and dry under reduced pressure at room temperature for 12 hours to obtain 10 groups of composite powders with a molar ratio of mebendazole:cholesterol of 1:1-1:10.

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 diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a mebendazole lipid compound. The compound is formed by compounding mebendazole and a lipid material through intermolecular non-covalent bonds, wherein the molar ratio of the mebendazole to the lipid material is 1: (0.1-15). The compound provided by the invention effectively improves the lipid solubility of the mebendazole, and overcomes the limitation of solubility on mebendazole liquid preparation research. The compound provided by the invention provides a good intermediate carrier for preparation research of high-efficiency delivery of the mebendazole.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a mebendazole-lipid complex and a preparation method and application thereof. Background technique [0002] Parasitic diseases are a class of diseases that seriously endanger the health of humans and animals. Parasitic diseases caused by toxoplasma gondii, cysticercosis, tapeworm, etc. are also zoonotic diseases. The treatment and prevention of parasitic infections are of great importance in medicine and public health. significance. In the World Health Organization's List of Essential Medicines, mebendazole is a broad-spectrum first-line drug against intestinal nematodes, and has been included in the Chinese Pharmacopoeia, British Pharmacopoeia, and US Pharmacopoeia as a single or mixed infection for the treatment of whipworms, worms, and hookworms . In my country, mebendazole is an over-the-counter drug. It is listed as a Class A drug in the National Essent...

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 Applications(China)
IPC IPC(8): A61K47/24A61K47/28A61K9/107A61K9/00A61K31/4184A61P33/10A61P33/02A61P33/08A61P33/00
CPCA61K47/24A61K47/28A61K9/107A61K9/00A61K31/4184A61P33/10A61P33/02A61P33/08A61P33/00
Inventor 刘黎瑶王庆奎丛方地陈成勋郭永军徐大为孙学亮戴文婕
Owner TIANJIN AGRICULTURE COLLEGE
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com