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Selenium or tellurium containing polymer as well as preparation method and application of selenium or tellurium containing polymer

A technology of polymers and copolymers, which is applied in medical preparations of non-active ingredients, drug combinations, drug delivery, etc., can solve the problems of decreased drug efficacy, limited application, and poor solubility, so as to improve the therapeutic effect and reduce drug administration. Frequency, the effect of reducing side effects

Active Publication Date: 2016-03-09
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, paclitaxel and camptothecin have poor solubility, which greatly limits their application.
The traditional way of administering anticancer drugs clinically, such as intravenous administration, has a short half-life, which not only reduces the utilization rate of the drug in the body, reduces the efficacy, but also causes some serious side effects, including nausea and vomiting and other gastrointestinal reactions, nephrotoxicity, Ototoxicity, neurotoxicity, myelosuppression, etc.

Method used

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  • Selenium or tellurium containing polymer as well as preparation method and application of selenium or tellurium containing polymer
  • Selenium or tellurium containing polymer as well as preparation method and application of selenium or tellurium containing polymer
  • Selenium or tellurium containing polymer as well as preparation method and application of selenium or tellurium containing polymer

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Experimental program
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Embodiment 1

[0044]Add 4.74g of selenium powder into a 100mL branched round bottom flask, add 20mL of deoxygenated deionized water, and stir evenly. Under an ice bath and an argon atmosphere, a sodium borohydride solution containing 4.54 g was added dropwise to the system until the system was colorless. Sodium selenium hydride solution is obtained, denoted as NaHSe. Dissolve 13.0 g of trichloropropionic acid in 30 mL of deoxygenated deionized water, and add Na 2 CO 3 Adjust the pH to 8.0. The trichloropropionic acid solution was added to the sodium selenium hydride solution, reacted at room temperature for 12 hours under an argon atmosphere, and then filtered. Add 1mol / L HCl to the filtrate to acidify to pH 3~4, producing a large amount of dark red precipitate. Extract with ethyl acetate three times, add anhydrous magnesium sulfate to the extract and dry for 3-4h, remove the solvent and recrystallize. Selenium-containing small molecules with modified carboxyl groups at both ends were ...

Embodiment 2

[0046] Add 2.37g of selenium powder into a 100mL branched round bottom flask, add 15mL of deoxygenated deionized water, and stir evenly. Under an ice bath and an argon atmosphere, a solution containing 2.27 g of sodium borohydride was added dropwise to the system until the system was colorless. Continue to add 2.37g of selenium powder, raise the temperature to 105°C and react for 20min to obtain a sodium diselenide solution, denoted as Na 2 Se 2 . Take 6.5g trichloropropionic acid and dissolve it in 15mL anaerobic water, add Na 2 CO 3 Adjust the pH to 8.0. The trichloropropionic acid solution was added to the sodium diselenide solution, reacted at room temperature for 12 hours under an argon atmosphere, and then filtered. Add 1mol / L HCl to the filtrate to acidify to pH 3~4, producing a large amount of dark red precipitate. Extract with ethyl acetate three times, add anhydrous magnesium sulfate to the extract and dry for 3-4h, remove the solvent and recrystallize. A smal...

Embodiment 3

[0048] Add 3.83g of tellurium powder into a 100mL branched round bottom flask, add 15mL of deoxidized deionized water, and stir evenly. Under an ice bath and an argon atmosphere, a solution containing 2.27 g of sodium borohydride was added dropwise to the system until the system was colorless. Sodium telluride hydride solution is obtained, denoted as NaHTe. Dissolve 6.5 g of trichloropropionic acid in 15 mL of deoxygenated deionized water, and add Na 2 CO 3 Adjust the pH to 8.0. The trichloropropionic acid solution was added to the sodium hydride telluride solution, reacted at room temperature for 12 hours under an argon atmosphere, and then filtered. Add 1mol / L HCl to the filtrate to acidify to pH3~4. Extract with ethyl acetate three times, add anhydrous magnesium sulfate to the extract and dry for 3-4h, remove the solvent and recrystallize. A small tellurium-containing molecule with carboxyl groups modified at both ends was obtained, Te(CH 2 CH 2 COOH) -2 , yield 55%...

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Abstract

The invention belongs to the fields of biomedical polymer materials and particularly relates to a selenium or tellurium containing polymer as well as a preparation method and application of the selenium or tellurium containing polymer. The polymer is a selenium or tellurium containing amphiphilic block copolymer obtained by chemically bonding selenium or tellurium containing micromolecules and an amphiphilic block copolymer. The polymer can form micelles, microparticles, vesicles and microspheres under a proper condition and has the functions such as reductive response and coordination response. The particles can coat a drug to form a controlled-release drug conveying system, injection administration can be realized through various ways, and the coated drug can be released from the conveying system in a controlled-release way according to demands, so that the administration frequency is reduced, the treating effect is improved, and the toxic and side effects of the drug are reduced.

Description

technical field [0001] The invention belongs to the technical field of medical polymer materials, and in particular relates to a polymer containing selenium or tellurium, a preparation method and application thereof. Background technique [0002] Biomedical polymer materials have many advantages such as good biocompatibility and easy-to-adjust biodegradability, and are an important direction in the research of biomedical materials. They have broad application prospects in the fields of drug sustained and controlled release, tissue engineering, etc. . Among them, degradable amphiphilic block copolymers have received special attention. [0003] The relationship between human health and trace elements is a research hotspot today. As one of the essential trace elements for the human body, selenium has unique functions such as redox response and coordination response, especially anti-oxidation, so that selenium compounds can remove excess free radicals in the body. These uniqu...

Claims

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Application Information

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IPC IPC(8): C08G63/664C08G63/91A61K9/52A61K47/34A61P35/00
Inventor 俞麟栾家斌丁建东
Owner FUDAN UNIV
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