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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 oligosaccharides generally have a higher positive charge in water. Its structure in water is similar to cationic surfactants and is more toxic.

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

technical field [0001] The invention relates to the field of medicinal materials, in particular to the synthesis of a dextran / indomethacin and the preparation thereof into a solution drug delivery system loaded with poorly soluble drug polymer nanoparticles. Background technique [0002] Malignant tumors are a major killer that endangers human health and destroys the quality of human life. It is also one of the main causes of death. About 7 million people die from tumors every year (accounting for 13% of the total number of deaths); in recent years, The morbidity and mortality of malignant tumors in my country are also increasing year by year, with more than 2.6 million cases and 1.8 million deaths each year. The current clinical methods for treating tumors include surgical resection, chemotherapy, and radiotherapy, among which the application of drugs to chemotherapy is one of the auxiliary means of surgical resection, and it is also the main systemic treatment. However, du...

Claims

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Application Information

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IPC IPC(8): C08B37/02A61K47/69A61K47/61A61K9/19A61K31/405A61P35/00A61K31/704A61K38/13A61K31/337A61K31/366A61K31/55
CPCA61K9/19A61K31/337A61K31/366A61K31/405A61K31/55A61K31/704A61K38/13C08B37/0009A61K2300/00
Inventor 魏晓红
Owner HANGZHOU NORMAL UNIVERSITY
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