Graphene oxide-loaded diclofenac diethylamine and preparation method thereof

A technology based on diclofenac diethylamine and graphene, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problems of difficult control of dosage, easy staining of clothes, limited duration, etc. problems, to overcome low bioavailability, less pollution, slow and stable drug release

Active Publication Date: 2019-08-16
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Transdermal administration of diclofenac diethylamine salt has a fast onset time and can avoid gastrointestinal irritation and first-pass effect, but there are problems such as difficult control of dosage, easy staining of clothes, and limited duration of administration.

Method used

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  • Graphene oxide-loaded diclofenac diethylamine and preparation method thereof
  • Graphene oxide-loaded diclofenac diethylamine and preparation method thereof
  • Graphene oxide-loaded diclofenac diethylamine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Graphene oxide supported diclofenac diethylamine

[0031] (1) Preparation method:

[0032] 1) Dissolve 9 mg of graphene oxide solid in 28 mL of distilled water, and ultrasonically dissolve the graphene oxide solution to be placed in a beaker for use; dissolve 6 mg of diclofenac diethylamine in 2 mL of water, and ultrasonically dissolve to obtain diclofenac diethylamine solution, Under the condition of stirring, the diclofenac diethylamine solution was slowly added dropwise to the graphene oxide solution, and reacted under light shielding at 20°C, and continued stirring at a speed of 30 rpm for 1 hour to obtain a reaction solution;

[0033] 2) Put the reaction solution in step 1) into a 50mL centrifuge tube, centrifuge (5000rpm, 5min) with a high-speed desktop refrigerated centrifuge at 4°C, wash, collect the supernatant, filter it with a 0.45μm organic filter membrane and transfer Put it into a high-performance liquid phase sampling bottle, seal it and store ...

Embodiment 2

[0057] Example 2 Effect of the ratio of graphene oxide and diclofenac diethylamine on the encapsulation efficiency and loading capacity of DDEA / GO

[0058] 1) Weigh 1.8mg, 4.5mg, 6mg, 9mg, and 13.5mg of diclofenac diethylamine respectively and dissolve them in 2mL of distilled water, and slowly add them dropwise to the graphene oxide aqueous solution (oxidized Graphene: 9mg, water: 28mL), light-shielding reaction, continuous stirring for 24h.

[0059] 2) The above reaction solution was centrifuged at 4°C for 10 minutes (5000r / min), the precipitate was washed with water and then centrifuged again (5000rpm, 5min). After repeated washing three times, the precipitate was freeze-dried to obtain the product DDEA / GO, and the supernatant was collected. After filtration with a 0.45 μm organic filter membrane, it was transferred into a high-performance liquid phase sampling bottle, sealed and stored in a refrigerator at 4°C until use.

[0060] 3) Determination by high performance liqui...

Embodiment 3

[0062] Example 3 Effect of reaction time between graphene oxide and diclofenac diethylamine on DDEA / GO encapsulation efficiency and loading capacity

[0063] 1) Weigh eight portions of 6mg diclofenac diethylamine and dissolve them in 2mL of distilled water respectively, and slowly add them dropwise to the graphene oxide aqueous solution (graphene oxide: 9mg, water: 28mL) under stirring (20°C, 30rpm) In the shading reaction, stir for 0min, 5min, 10min, 20min, 30min, 60min, 120min, 180min respectively.

[0064] 2) The above reaction solution was centrifuged at 4°C for 10 minutes (5000r / min), the precipitate was washed with water and then centrifuged again (5000rpm, 5min). After repeated washing three times, the precipitate was freeze-dried to obtain the product DDEA / GO, and the respective supernatants were collected , filtered with a 0.45 μm organic filter membrane, transferred to a high-performance liquid phase sampling bottle, and sealed in a refrigerator at 4°C for storage un...

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Abstract

The invention discloses the field of pharmaceutical preparations, and in particular, relates to graphene oxide-loaded diclofenac diethylamine and a preparation method thereof. The graphene oxide-loaded diclofenac diethylamine is a graphene oxide / diclofenac diethylamine complex obtained by loading diclofenac diethylamine on a graphene oxide sheet layer by non-covalent bonding. The preparation method comprises the following steps: a graphene oxide solid is dissolved in distilled water, and a graphene oxide solution is obtained by ultrasonic dissolution; diclofenac diethylamine is dissolved in water, and a diclofenac diethylamine solution is obtained by ultrasonic dissolution; under stirring conditions, the diclofenac diethylamine solution is slowly dripped into the graphene oxide solution, alight shading reaction is performed, stirring is continued, and a reaction liquid is obtained; centrifugation and washing are performed; and the target product is obtained by pre-freezing and freeze-drying. The preparation method has the advantages of simple operation and less produced pollution; and the obtained product has high drug loading amount and good stability, and has good clinical research application value.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a graphene oxide-loaded diclofenac diethylamine and a preparation method thereof. Background technique [0002] Graphene oxide (GO) is one of the important derivatives of graphene. It has the advantages of good water solubility, good stability, and low toxicity, and is widely used in drug delivery systems. The aromatic structure of graphene oxide enables the surface to provide a large number of π-π binding sites, which can be combined with molecules that also have π-π conjugated or aromatic structures; active groups such as hydroxyl and carboxyl groups on the surface of graphene oxide are easy to bind with Drug molecules form hydrogen bonds to realize drug loading. [0003] Diclofenac diethylamine (DDEA) is the diethylamine salt of diclofenac, which belongs to non-steroidal anti-inflammatory drugs. It is a prostaglandin synthesis inhibitor with anti-infla...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): A61K47/52A61K31/205A61P29/00
CPCA61K31/205A61K47/52A61P29/00
Inventor潘春娇刘宇
OwnerLIAONING UNIVERSITY