Niclosamide ethanolamine salt-hydroxypropyl-beta-cyclodextrin inclusion compound and preparation thereof

A technology for niclosamide ethanolamine salt and ethanolamine salt hydroxypropyl, which is applied in the field of niclosamide ethanolamine salt-hydroxypropyl-β-cyclodextrin and its preparation, can solve the problems of less research on injection preparations and the like , to achieve the effect of strong solubilization, small local irritation and low hemolysis

Pending Publication Date: 2020-02-25
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to improve the dissolubility of niclosamide, research on its formulation mainly lies in how to improve the field of molluscicide of niclosamide, such as paste, wettable powder, slow-release agent, controlled-release agent, etc.; but niclosamide There are few studies on oral preparations and injection preparations for clinical application

Method used

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  • Niclosamide ethanolamine salt-hydroxypropyl-beta-cyclodextrin inclusion compound and preparation thereof
  • Niclosamide ethanolamine salt-hydroxypropyl-beta-cyclodextrin inclusion compound and preparation thereof
  • Niclosamide ethanolamine salt-hydroxypropyl-beta-cyclodextrin inclusion compound and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0021] One, the preparation method of clathrate

[0022] The invention provides a preparation method of niclosamide ethanolamine salt-hydroxypropyl-β-cyclodextrin inclusion compound, which comprises the following steps, and all the steps of the invention are completed under light-proof conditions.

experiment example 1

[0023] Experimental Example 1 Quality Evaluation of NHC Inclusion Compounds Prepared by Different Preparation Methods

[0024] Grinding method (Kneading method)

[0025] Weigh about 0.25g of NES powder and 10g of HP-β-CD, mix them in a mortar, add appropriate amount of distilled water and grind until thick slurry (about 2h). Dry at 40°C, pulverize, and pass through a 80-mesh sieve to obtain a yellow powder product.

[0026] Freeze-drying (Co-lyophilized)

[0027] Weigh 0.25 g of NES powder, and measure 25 mL of HP-β-CD solution with a mass concentration of about 400 g / L. Heat the water temperature to 60°C under magnetic stirring and slowly put NES into the aqueous solution of HP-β-CD, keep stirring at a constant temperature for 2 hours to obtain a clear solution, pre-freeze in a -80°C refrigerator for 18 hours, and freeze-dry in a vacuum freeze dryer for 24 hours , the dry matter was pulverized and passed through a 80-mesh sieve to obtain a yellow powder product.

[0028] ...

experiment example 2

[0034] Experimental Example 2 Quality Evaluation of NHC Inclusion Compounds Prepared by Different Concentrations of HP-β-CD Solutions

[0035] Prepare 10mL of cyclodextrin solutions with concentrations of 200g / L, 250g / L, 300g / L, 350g / L, 400g / L, and 500g / L, respectively, and put them into NES according to the ratio of substances of 11:1. Under the condition of water bath at 45°C, NES was slowly added into the HP-β-CD aqueous solution while stirring, and the constant temperature stirring was continued for 2 hours to obtain a clear solution. The inclusion ratios were calculated respectively, and the results are shown in Table 2.

[0036] Table 2 Quality evaluation of NHC clathrates prepared by different concentrations of HP-β-CD solutions

[0037]

[0038] Experimental results: The NHC clathrate prepared by using the concentration of HP-β-CD (300g / L) of the present invention has a high clathrate rate and good clathrate effect. The results show that only the NHC clathrate prep...

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Abstract

The invention provides niclosamide ethanolamine salt-hydroxypropyl-beta-cyclodextrin inclusion and a preparation method thereof; the inclusion is prepared from niclosamide ethanolamine salt and hydroxypropyl-beta-cyclodextrin as a raw material and belongs to the field of pharmacy. In the invention, a molar ratio of hydroxypropyl-beta-cyclodextrin to niclosamide ethanolamine salt is 7:(1-16):1, theinclusion is prepared by: adding niclosamide ethanolamine salt to a hydroxypropyl-beta-cyclodextrin solution prepared, stirring in the dark to obtain a clear solution, and lyophilizing to obtain theniclosamide ethanolamine salt-hydroxypropyl-beta-cyclodextrin inclusion; after the inclusion is formed, the water solubility of the niclosamide ethanolamine salt is obviously improved. The inclusion has high inclusion rate, the preparation method is simple, the efficiency is high, the application range is wide, and the inclusion is suitable for large-scale production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a niclosamide ethanolamine salt-hydroxypropyl-β-cyclodextrin and a preparation method thereof. The inclusion compound obtained by the method has a relatively high inclusion rate, and the niclosamide The dissolution and bioavailability of amine ethanolamine salts will also be improved. Background technique [0002] Niclosamide (niclosamide, NHC), the chemical name is N-(2'-chloro-4'-nitrophenyl)-5-chlorosalicylamide, light yellow powder, insoluble in water, soluble in hot alcohol and chloroform , Ether, due to its high efficacy and low toxicity, has been used as a drug for the treatment of human intestinal parasites for more than 50 years. In recent years, during the research and development of anti-tumor drugs, a large number of drug screening experiments have found that niclosamide also has potential anti-tumor effects. Compared with newly synthesized anti-tum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/167A61P35/00A61P33/00
CPCA61K47/6951A61K31/167A61P35/00A61P33/00
Inventor 王淼陈羽刘瑞雪
Owner SHENYANG PHARMA UNIVERSITY
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