Synthetic method and application of glucan/indometacin graft

A technology of indomethacin grafts and synthesis methods, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, etc., can solve problems such as high toxicity, and achieve high drug loading, tumor Increased cell inhibition rate and simple preparation

Active Publication Date: 2017-10-31
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the presence of a large number of free amino groups on chitosan oligosaccharides, the nanoparticles made of chitosan oligo

Method used

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  • Synthetic method and application of glucan/indometacin graft
  • Synthetic method and application of glucan/indometacin graft
  • Synthetic method and application of glucan/indometacin graft

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Weighed indomethacin (3.086mmol, 1103mg), EDC (9.258mmol, 1774mg) and DMAP (0.9258mmol, 113.0mg), dissolved in 10mL of DMSO, stirred to dissolve completely, kept at constant temperature at 60°C for 30min, slowly Add dextran (3.086mmol, 500mg) (Mw=10000), stir and react at 25°C for 24h, then transfer the reaction solution to a dialysis bag (MWCO=7000), dialyze with double distilled water as the medium, and continue to replace the medium for 48h , after the dialysis, collect the milky liquid in the dialysis bag, at 4 DEG C, centrifuge 10min at 4000rpm, remove the insoluble matter, get the supernatant and freeze-dry to obtain the dextran / indomethacin graft (hereinafter abbreviated as Dex / Indo) freeze-dried product 1.

[0056] The obtained dextran / indomethacin graft lyophilized product 1 was Dex10000 / Indo20%.

Embodiment 2

[0058] Separately weigh indomethacin (1.543mmol, 551.5mg), EDC (4.629mmol, 886.9mg) and DMAP (0.4629mmol, 56.0mg), dissolve in 10mL DMSO, stir to dissolve completely, and keep at constant temperature 70°C for 20min , slowly added dextran (3.086mmol, 500mg) (Mw=10000), stirred and reacted at 70°C for 12h, then transferred the reaction solution to a dialysis bag (MWCO=5000), dialyzed with double distilled water as the medium, and continuously replaced Medium 48h, after dialysis finishes, collect the milky liquid in the dialysis bag, at 10 ℃, 2000rpm centrifugal 50min, remove insoluble matter, get the supernatant and freeze-dry to obtain dextran / indomethacin graft (hereinafter abbreviated as Dex / Indo) freeze-dried product 2.

[0059] The obtained dextran / indomethacin graft lyophilized product 2 was Dex10000 / Indo50%.

Embodiment 3

[0061] Separately weigh indomethacin (0.617mmol, 220.6mg), EDC (1.851mmol, 354.7mg) and DMAP (0.1851mmol, 23.0mg), dissolve in 10mL DMSO, stir to dissolve completely, keep at constant temperature 20°C for 12h , slowly added dextran (3.086mmol, 500mg) (Mw=10000), stirred and reacted at 20°C for 48h, then transferred the reaction solution to a dialysis bag (MWCO=6000), dialyzed with double distilled water as the medium, and continuously replaced Medium 48h, after dialysis finishes, collect the milky liquid in the dialysis bag, at 2 ℃, 8000rpm centrifugal 20min, remove insoluble matter, get the supernatant liquid freeze-drying and promptly obtain dextran / indomethacin graft (hereinafter abbreviated as Dex / Indo) freeze-dried product3.

[0062] The obtained dextran / indomethacin graft lyophilized product 3 was Dex10000 / Indo100%.

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Abstract

The invention relates to the field of medicinal materials and discloses a synthetic method and application of a glucan/indometacin graft. According to the synthetic method and the application, the problem that certain drugs have serious toxic and side effects is solved. 4-dimethylaminopyridine (DMAP) is taken as a catalyst, carbodiimide (EDC) is taken as a dehydrating agent, glucan and indometacin are respectively taken as a hydrophilic skeleton and a hydrophobic chain segment, and hydroxide radicals in a chemical structure of glucan (Dex) generate esterification reaction with carboxyl in a chemical structure of indometacin (Indo) to generate an amphipathic compound, namely the glucan/indometacin graft. A drug delivery system which is prepared from the glucan/indometacin graft and loaded with an indissolvable drug polymer nanoparticle solution has relatively high drug loading capacity and encapsulation efficiency, presents hypotoxicity and can be used as a drug carrier.

Description

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Claims

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Application Information

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Owner HANGZHOU NORMAL UNIVERSITY
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