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Dexamethasone small-molecular hydrogel drug delivery system and preparation method thereof

A technology of dexamethasone and small molecular water, which is applied in the directions of drug combination, pharmaceutical formula, medical preparation containing active ingredients, etc., can solve the problems of poor biocompatibility, complex degradation products, difficult synthesis, etc. mild conditions

Inactive Publication Date: 2013-01-02
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are many drug delivery systems, such as liposomes, block polymers, polymer assemblies, dendrimers, albumin, polymer hydrogels, etc., due to the inherent defects of these carriers: complex degradation products, economical Poor efficiency, difficult synthesis, poor biocompatibility in vivo, etc.

Method used

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  • Dexamethasone small-molecular hydrogel drug delivery system and preparation method thereof
  • Dexamethasone small-molecular hydrogel drug delivery system and preparation method thereof
  • Dexamethasone small-molecular hydrogel drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0009] 1. Synthesis of Dexamethasone Derivatives

[0010] Put 1mmol of dexamethasone into a round bottom flask, add 4 equivalents of 1,4-succinic anhydride (glutaric anhydride), dissolve it with 12 milliliters of piperidine, stir at room temperature for 24 hours; then spin the piperidine to dryness ; Then add an appropriate amount of water, place it on ice to precipitate the product, then centrifuge (10000r / min) for 5-10min, discard the supernatant, wash with water for two changes; finally freeze-dry.

[0011] A: Dex-SA (dexamethasone succinate) NMR analysis

[0012] 1 HNMR (300MHz, DMSO-d 6 )δ7.27 (d, J=10.11, 1H), 6.19-6.24 (q, 1H), 5.99 (m, 1H), 5.42 (d, 1H), 5.17 (s, 1H), 4.99-5.06 (m, 1H), 4.75-4.82(m, 1H), 4.10-4.15(m, 1H), 2.82-2.91(m, 1H), 2.58-2.61(m, 3H), 2.26-2.40(m, 3H), 2.09- 2.18(m, 2H), 1.53-1.79(m, 6H), 1.05-1.096(m, 1H).MS: calc.M+=492.2, obsvd.(M+1) + =493.1.

[0013] B: Dex-GA (dexamethasone glutarate) NMR analysis

[0014] 1 HNMR (300MHz, DMSO-d 6 ...

example 1

[0016] Example 1 (preparation of 2 wt% hydrogel at pH 7.0 and temperature 20°):

[0017] Take 4 mg of succinylated dexamethasone derivatives in a 1.5 ml glass bottle, add 150 microliters of PBS (PH=7.0) solution, adjust the pH value to 7.0 with sodium carbonate solution, and set the volume to 200 microliters with PBS solution, Stand still (20 degrees Celsius) to make it self-hydrolyzed, and form a gel after about 70 hours.

example 2

[0018] Example 2 (preparation of 2 wt% hydrogel at pH 7.0 and temperature 30°):

[0019] Take 4 mg of succinylated dexamethasone derivatives in a 1.5 ml glass bottle, add 150 microliters of PBS (PH=7.0) solution, adjust the pH value to 7.0 with sodium carbonate solution, and set the volume to 200 microliters with PBS solution, Stand still (30 degrees Celsius) to make it self-hydrolyzed, and form a gel after about 50 hours.

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Abstract

The invention relates to a dexamethasone small-molecular hydrogel drug delivery system and a preparation method thereof. According to the invention, dexamethasone is subjected to derivatization by using 1,4-succinic anhydride or glutaric anhydride, such that a dexamethasone prodrug is formed. Through pH value regulation, the prodrug is subjected to auto-hydrolysis, such that dexamethasone drug molecules are released; the molecules are subjected to self-assembly spontaneously, such that the small-molecular hydrogel is formed. Specifically, dexamethasone 21 hydroxyl site derivatization is achieved by using 1,4-succinic anhydride (glutaric anhydride), such that gel-forming precursor molecules are obtained. The precursor molecules have good solubility, high drug load, and simple components. Through auto-hydrolysis, dexamethasone drug molecules can be released, and can be spontaneously self-assembled into the hydrogel. The process does not need to be driven by any chemical reagent. According to the system, drug molecules and derivatized drug are adopted as carriers, such that other carriers are not needed. Therefore, the dexamethasone novel delivery system provided by the invention assists in improving solubility and drug load of dexamethasone in water, and is potential to be developed into a novel preparation form of dexamethasone.

Description

technical field [0001] The technical scheme of the invention relates to a preparation method of dexamethasone small molecule hydrogel and its application as a novel dexamethasone drug delivery system. Specifically, it is a new drug delivery system of dexamethasone and the preparation of nanofibers of dexamethasone and its derivatives. Background technique [0002] Dexamethasone is a class of adrenal corticosteroids. In 1958, Arth and Oliveto synthesized dexamethasone respectively. In 1960, Merck & Co. produced dexamethasone sodium phosphate. Up to now, more than 12 kinds of dexamethasone derivatives have been listed. It has anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects, and is mainly used for the treatment of bacterial infections, allergic diseases, and tumor treatment. Its water solubility is poor at room temperature, about 0.1mg / mL, so it is often derivatized or dissolved with some other solvents in clinical use, and intramuscular inject...

Claims

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Application Information

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IPC IPC(8): C07J5/00A61K9/06A61K31/573A61P29/00A61P37/08A61P37/06A61P31/04A61P35/00
Inventor 杨志谋王玲杨成彪
Owner NANKAI UNIV