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Nitric oxide donor modified copolymer, sustained release preparation containing same, and preparation method and application thereof

A technology of nitric oxide and sustained-release preparations, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., and can solve problems such as unfavorable long-acting sustained release and sudden release of large drugs. Achieve the effect of reducing side effects, improving utilization rate, good anticipation and controllability

Active Publication Date: 2020-08-18
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, due to the high water solubility of most nitric oxide donor small molecule drugs, when they are physically loaded in thermotropic hydrogels, there will be a large burst of drug release in the early stage of release, which is not conducive to their long-term effect. sustained release

Method used

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  • Nitric oxide donor modified copolymer, sustained release preparation containing same, and preparation method and application thereof
  • Nitric oxide donor modified copolymer, sustained release preparation containing same, and preparation method and application thereof
  • Nitric oxide donor modified copolymer, sustained release preparation containing same, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0056] A nitric oxide donor-modified amphiphilic block copolymer, adding dihydroxypolyethylene glycol (PEG1500) into a 250mL three-necked flask, and removing water under vacuum at 120°C for 3h. Cool to 80°C with argon, add lactide (LA), glycolide (GA) and stannous octoate (containing a small amount of toluene), and vacuum at 120°C for 30 minutes. Argon was blown, and the temperature was raised to 150°C for 12 hours. After the reaction was completed, vacuum filtration was performed for 2 hours to remove unreacted monomers and low-boiling products in the system. The product was poured into deionized water at 80°C while it was hot, washed three times repeatedly, and freeze-dried to obtain the BAB type triblock polymer PLGA-PEG-PLGA with a yield of about 83%. The number-average and weight-average molecular weight (M n ,M w ) are 5080 and 5930 respectively, the molecular weight distribution coefficient is 1.17, and its polymer water system has thermal gelation performance. Di...

Embodiment 2

[0058] A nitric oxide donor-modified amphiphilic block copolymer, adding dihydroxypolyethylene glycol (PEG1500) into a 250mL three-necked flask, and removing water under vacuum at 120°C for 3h. Cool to 80°C with argon, add ε-caprolactone (CL), glycolide (GA) and stannous octoate (containing a small amount of toluene), and vacuum at 100°C for 30 minutes. Argon was blown, and the temperature was raised to 150°C for 12 hours. After the reaction was completed, vacuum filtration was performed for 2 hours to remove unreacted monomers and low-boiling products in the system. The product was poured into deionized water at 80°C while it was hot, washed three times repeatedly, and freeze-dried to obtain the BAB type triblock polymer PCGA-PEG-PCGA with a yield of about 80%. The number-average and weight-average molecular weight (M n ,M w ) are 7550 and 10040 respectively, molecular weight distribution coefficient It is 1.33, and its polymer water system has heat-induced gelation perf...

Embodiment 3

[0060] A nitric oxide donor-modified amphiphilic block copolymer, adding dihydroxypolyethylene glycol (PEG1500) into a 250mL three-necked flask, and removing water under vacuum at 120°C for 3h. Cool to 80°C with argon, add ε-caprolactone (CL), lactide (LA) and stannous octoate (containing a small amount of toluene), and vacuum at 120°C for 30 minutes. Argon was blown, and the temperature was raised to 150°C for 12 hours. After the reaction, the product was poured into 80°C deionized water while it was still hot, washed three times, and freeze-dried to obtain the BAB-type triblock polymer PCLA-PEG-PCLA with a yield of about 80%. The number-average and weight-average molecular weight (M n ,M w ) are 8720 and 12060 respectively, molecular weight distribution coefficient It is 1.38, and its polymer water system has heat-induced gelation performance. In a 100 mL eggplant-shaped bottle, dissolve 1 mmol of the block copolymer Polymer-3 in 30 mL of toluene, azeotropically remove...

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Abstract

The invention belongs to the technical field of high polymer materials and medicines, and discloses a nitric oxide donor modified copolymer, a sustained-release preparation containing the same, and apreparation method and an application thereof. The nitrogen monoxide donor modified amphiphilic block copolymer comprises a hydrophilic block A, a hydrophobic block B and a nitrogen monoxide donor, wherein the nitrogen monoxide donor is covalently connected to the tail ends or branched chains of the hydrophilic block A and the hydrophobic block B through amido bonds or ester bonds; the nitric oxide gel sustained release preparation comprises a gel carrier material and a solvent, and the gel carrier material comprises one or more amphiphilic block copolymers modified by the nitric oxide donor.The gel sustained-release preparation is in a flowing sol state at low temperature or room temperature, can spontaneously form thermotropic hydrogel at body temperature along with temperature rise, and can realize long-acting sustained release of nitric oxide in a human body. Therefore, the compound can be applied to preparation of materials and medicines for cancer treatment, neurological diseasetreatment, cardiovascular disease treatment and wound repair.

Description

technical field [0001] The invention belongs to the technical field of polymer materials and medicine, and in particular relates to a nitric oxide donor-modified copolymer, a slow-release preparation containing it, a preparation method and application thereof. Background technique [0002] Nitric oxide is an endogenous signaling molecule in the human body, which is produced by the oxidation of arginine catalyzed by nitric oxide synthase, and participates in the regulation of various physiological processes. Nitric oxide can participate in physiological regulation through direct or indirect chemical action. The most typical example is that nitric oxide is directly combined with metal complexes of different proteins to form metal nitrosyl complexes to regulate their biological activities. For example, nitric oxide activates guanylate cyclase (sCG), which catalyzes the conversion of guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP). Signal transduction pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/91C08G63/664C08G64/42C08G64/18C08G69/48C08G69/40A61K47/59A61K9/06A61K33/00A61P9/00A61P25/00A61P35/00
CPCC08G63/912C08G63/664C08G64/42C08G64/183C08G69/48C08G69/40A61K47/59A61K9/06A61K9/0019A61K33/00A61P35/00A61P25/00A61P9/00
Inventor 俞麟王耀本丁建东
Owner FUDAN UNIV
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