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A supramolecular hydrogel loaded with indomethacin and its preparation method

A technology of supramolecular hydrogel and indomethacin, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems that hinder the preparation of indomethacin injections. Achieve the effects of easy regulation, great application value, and increased load capacity

Active Publication Date: 2021-09-28
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And indomethacin is insoluble in water, seriously hinders the preparation of indomethacin injection

Method used

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  • A supramolecular hydrogel loaded with indomethacin and its preparation method
  • A supramolecular hydrogel loaded with indomethacin and its preparation method
  • A supramolecular hydrogel loaded with indomethacin and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]a. Accurately weigh β-cyclodextrin (210g, 0.19mol) and dissolve it in 1500mL of distilled water, stir it fully in an electric stirrer to make the solution into a milky white liquid, and control the temperature of the solution at about 15°C with a water bath , slowly added the prepared aqueous sodium hydroxide solution (34.4 g, 17.90 mol / 100 mL) into the liquid, and continued stirring for 1 h after observing that the cyclodextrin was completely dissolved. Accurately weigh p-toluenesulfonyl chloride (30.2g, 0.16mol) and quickly dissolve it in 90ml of acetonitrile, slowly drop the prepared p-toluenesulfonyl chloride acetonitrile solution into the cyclodextrin solution, pay attention to controlling the speed of solution dripping, constant temperature conditions Stirring was continued for 2.5 h. After static precipitation, the insoluble matter was removed by suction filtration under reduced pressure, and the pH value of the solution was slowly adjusted to 7.5 with 2M hydrochl...

Embodiment 2

[0032] Take 0.35 g of the prodrug molecule indo-2N-β-CD prepared in Example 1 and 0.5 g of F127 in a reactor, add 5 ml of deionized water, and stir at 60° C. for 4 hours. Then 0.5g α-CD was added into the reaction system, stirring was continued at 60° C. for 4 h, and the whole reaction was carried out in the dark. After the reaction, the reaction vial was slowly cooled to room temperature, and after standing for 12 hours, it was freeze-dried for 12 hours to obtain a dry hydrogel drug-loading system. The mass / volume contents of F127, indo-2N-β-CD, and α-CD were 10%, 7%, and 10%, respectively.

Embodiment 3

[0034] Take 0.15 g of the prodrug molecule indo-2N-β-CD and 0.25 g of F127 prepared in Example 1 in a reactor, add 5 ml of deionized water, and stir at 60° C. for 4 h. Then, 1 g of α-CD was added into the reaction system, and the stirring was continued at 60° C. for 4 h, and the whole reaction was carried out in the dark. After the reaction, the reaction vial was slowly cooled to room temperature, and after standing for 12 hours, it was freeze-dried for 12 hours to obtain a dry hydrogel drug-loading system. The mass / volume contents of F127, indo-2N-β-CD, and α-CD were 20%, 3%, and 5%, respectively.

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Abstract

The invention relates to a supramolecular hydrogel loaded with indomethacin and a preparation method thereof. The preparation steps are as follows: chemically modifying β-cyclodextrin to prepare novel cyclodextrin derivatives; then adding indole The prodrug molecule indo‑2N‑β‑CD is synthesized by condensation reaction between Mecine and amine-modified cyclodextrin derivatives; finally, α‑cyclodextrin, Pluronic F127, and indo‑2N‑β‑CD are used as building blocks , in aqueous solution, the pseudopolyrotaxane loaded with hydrophobic drugs is first prepared through the interaction between the cavity of the cyclodextrin and the molecular chain of F127, and then the hydrogen bond between the hydroxyl groups in the cyclodextrin molecule is used, It is further expanded into a three-dimensional new supramolecular hydrogel material; the production process of the invention is simple, and indomethacin is loaded in the hydrogel network in the form of covalent bonds, which not only improves the solubility of the drug indomethacin, but also effectively The drug loading capacity of the hydrogel was improved.

Description

[technical field] [0001] The invention belongs to the field of supramolecular hydrogel drug loading, in particular to a supramolecular hydrogel loaded with indomethacin and a preparation method thereof. [Background technique] [0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are anti-inflammatory drugs that do not contain a steroidal structure. They have anti-inflammatory, analgesic and antipyretic effects, and have been widely used as early as the last century. Indomethacin, as an indole non-steroidal anti-inflammatory drug, is widely used in the treatment of toothache, dysmenorrhea and postoperative pain. The mechanism of action of indomethacin is to reduce the synthesis of prostaglandins by inhibiting cyclooxygenase, thereby inhibiting the inflammatory response, and also inhibiting the chemotaxis of leukocytes and the release of lysosomal enzymes. Through the observation and research of clinical phenomena, the researchers found that while indomethacin exerts therap...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K47/69A61K31/405A61P29/00
CPCA61K31/405A61K47/61A61K47/6903A61P29/00
Inventor 李亮郭家豪张兴华余焓王根礼
Owner SHANGHAI INST OF TECH
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