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A supramolecular hydrogel and its preparation method, and a slow-release preparation for killing schistosome cercariae and its preparation method

A technology of supramolecular hydrogel and sustained-release preparations, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems such as poor water solubility, difficulty in extraction, and short duration of drug action and other problems, to achieve the effects of good mechanical properties, strong hydrogen bonding, good drug loading and sustained release performance

Inactive Publication Date: 2020-09-08
GANNAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the commonly used cercariasis drugs include niclosamide, praziquantel and plant cercariasis drugs, etc., but all of them have obvious deficiencies, such as poor water solubility and difficult extraction.
At present, it is reported that the drug molecule of the cercaricide niclosamide is covalently bonded to the hydrophilic group polyethylene glycol to enhance the water solubility and water floating ability of the drug, but there is a problem of short drug effect time in practical application

Method used

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  • A supramolecular hydrogel and its preparation method, and a slow-release preparation for killing schistosome cercariae and its preparation method
  • A supramolecular hydrogel and its preparation method, and a slow-release preparation for killing schistosome cercariae and its preparation method
  • A supramolecular hydrogel and its preparation method, and a slow-release preparation for killing schistosome cercariae and its preparation method

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preparation example Construction

[0037] The present invention provides a preparation method of the supramolecular hydrogel described in the above technical scheme, comprising the following steps:

[0038] The supramolecular hydrogel is obtained by mixing N,N'-diaspartic acid-perylenetetracarboxylic acid diimide, water and tetrahydrofuran, and then performing ultrasonic treatment.

[0039] In the present invention, the power of the ultrasonic treatment is preferably 300-600W, more preferably 400-500W; the time is preferably 2.5-3.5h, more preferably 3h. In an embodiment of the present invention, specifically, N,N'-diaspartic acid-perylenetetracarboxylic acid diimide, water and tetrahydrofuran are mixed and then ultrasonicated until the resulting system is gelled to obtain a supramolecular hydrogel.

[0040] In the present invention, NAAPD is an amphiphilic molecule with a hydrophobic structure in the middle and hydrophilic groups at both ends. Ultrasound provides energy for the NAAPD molecule, so that the NAAP...

Embodiment 1

[0048] Mix 0.01mmol of N,N'-diaspartic acid-perylenetetracarboxylic acid diimide with 1mL of water and 1mL of tetrahydrofuran, and ultrasonically treat it for 3h under the condition of 400W, until the obtained system is gelled, and a deep red N,N '-Diaspartic acid-perylenetetracarboxylic acid diimide (NAAPD) gel.

[0049] Characterize the morphology and structure of the NAAPD gel, and test its mechanical properties, specifically as follows:

[0050] (1) The NAAPD gel is mixed with water to prepare 10 -4 mol / L hydrogel solution, the hydrogel solution was dropped on the surface of the silicon wafer stuck on the conductive adhesive, and dried naturally, and the morphology of the obtained xerogel was characterized by using a FEIQUANTA450 scanning electron microscope, and the accelerated voltage 15.0kV. figure 1 It is the SEM image of the NAAPD gel, wherein (a) is the SEM image of the NAAPD gel in a large range, and (b) is the SEM image of the NAAPD gel in a small range. Depend ...

Embodiment 2

[0053] Mix 0.01mmol of N,N'-diaspartic acid-perylenetetracarboxylic acid diimide with 0.5mL of water, 0.5mL of tetrahydrofuran and polyether benzamide, and ultrasonically treat it at 400W for 3h until the resulting system gels , to obtain NAAPD gel loaded with polyether benzamide (drug-loaded NAAPD gel).

[0054] By changing the amount of polyether benzamide added, the drug-loading ability of NAAPD gel was tested by the classic test tube inversion method. The experimental results show that under the condition that a stable gel state can be formed (such as Figure 5 Shown in a), the maximum drug loading capacity of NAAPD gel is 500mg / mL.

[0055] According to the method in Example 1, the morphology of the drug-loaded NAAPD gel (drug loading is 100mg / mL) is characterized, and its mechanical properties are tested, as follows:

[0056] (1) if Figure 5 As shown in b and 5c, (b) is the SEM image of the drug-loaded NAAPD gel in a large range, and (c) is the SEM image of the drug-...

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Abstract

The invention provides supramolecular hydrogel. The supramolecular hydrogel is obtained and prepared from N,N'-diaspartic acid-perylene-3,4,9,10-tetracarboxylic acid imidodicarbonic diamide, water andtetrahydrofuran, wherein the ratio of amount of substance of N,N'-diaspartic acid-perylene-3,4,9,10-tetracarboxylic acid imidodicarbonic diamide to volume of water to volume of tetrahydrofuran is 0.01mmol:(0.5-1.5)mL:(0.5-1.5)mL. In the invention, the N,N'-diaspartic acid-perylene-3,4,9,10-tetracarboxylic acid imidodicarbonic diamide (NAAPD) is taken as a gelator, has good molecular planarity andcan produce Pi-Pi accumulation, and four carboxylic groups are contained at the two ends of a molecule, so that intermolecular hydrogen bonding interaction is stronger. The supramolecular hydrogel provided by the invention has excellent mechanical strength; and the supramolecular hydrogel is taken as a carrier for a schistosome cercaria killing active substance, has good medicine carrying and slow release properties on the schistosome cercaria killing active substance and also has the characteristics of high mechanical strength and good biocompatibility.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, in particular to a supramolecular hydrogel and a preparation method thereof, a slow-release preparation for killing schistosome cercariae and a preparation method thereof. Background technique [0002] Schistosomiasis is an endemic disease caused by schistosomiasis adults parasitizing the human body, and is a major infectious disease that seriously endangers people's health. Nearly 200 million people around the world have been infected, covering 76 countries and regions, and the number of people living in endemic areas threatened by infection has reached 779 million. It is listed by the World Health Organization as an extremely recurring infectious disease. There are three species of Schistosoma japonicum, Schistosoma haematobium and Schistosoma mansoni that parasitize the human body. Among them, the life cycle of Schistosoma japonicum can be divided into seven main stages: eggs, mir...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08J3/075C08G83/00A61K9/06A61K47/34A61K31/167A61P33/12
CPCA61K9/06A61K31/167A61K47/34A61P33/12C08G83/008C08J3/075C08J2387/00Y02A50/30
Inventor 李亿保朱磊朱志强何英杰
Owner GANNAN NORMAL UNIV