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Nonlinear polymer having doxorubicin structure, and preparation method and application thereof

A doxorubicin and polymer technology is applied to medical preparations containing active ingredients, medical preparations with non-active ingredients, organic active ingredients, etc. It can solve problems such as low solubility, short half-life, and high toxicity, and achieve Easy to dissolve, excellent effect, half-life extended effect

Inactive Publication Date: 2014-07-09
张雅珍
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Doxorubicin is currently widely used, but it is often necessary to turn it into a salt from a clinical point of view, such as doxorubicin. The common medicinal form is doxorubicin hydrochloride, which needs to be turned into hydrochloride. Its solubility is very low, it cannot be converted into salt form, so it cannot be used
After becoming hydrochloride, the pharmacodynamic function of doxorubicin is greatly reduced, so this brings great difficulties to clinical application.
[0004] Another disadvantage of doxorubicin is that due to its strong cytotoxicity, it is very toxic. It often shows obvious bone marrow suppression about 10 days after use. After one week of use, it can show very obvious gastrointestinal tract. Adverse reactions and cardiotoxicity, so the drug must be accurately calculated before it can be used, and the half-life of the drug is very short, which also limits the application

Method used

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  • Nonlinear polymer having doxorubicin structure, and preparation method and application thereof
  • Nonlinear polymer having doxorubicin structure, and preparation method and application thereof
  • Nonlinear polymer having doxorubicin structure, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] 1) A mixture of 80 g of sebacic acid in 800 ml of acetic anhydride was refluxed to form acetyl-sebacic acid;

[0052] 2) Mix the 1st) step with the 6-arm polyethylene glycol 14g product terminated with hydroxyl and put it into a flask, and at 180 ° C under reduced pressure solution polymerization reaction 1 hour; ether washed and dried;

[0053] 3) Put 120 mg of doxorubicin and 800 mg of polymer from step 2 into 8 ml of dimethyl sulfoxide and 12 ml of dichloromethane solution for 48 hours; ultrasonicate for 3 minutes; then place in an oven for 1 hour; The homogenizer was stirred at an ultra-high speed at 20 degrees for 3 minutes, and then put into a 1% polyvinyl alcohol solution and stirred at 600 rpm for 2 hours; centrifuged, collected, and freeze-dried to obtain nanoparticles of the final product.

Embodiment 2

[0055] 1) A mixture of 100 g of sebacic acid in 900 ml of acetic anhydride was refluxed to form acetyl-sebacic acid;

[0056] 2) Mix the 1st) step with the 6-arm polyethylene glycol 19g product terminated with hydroxyl and put it into a flask, and at 180 DEG C. under reduced pressure for 1 hour; ether washed and dried;

[0057] 3) Put 200mg of doxorubicin and 1000mg of polymer from step 2 into 6ml of dimethyl sulfoxide and 14ml of dichloromethane solution for 24 hours; ultrasonicate for 2 minutes; then put in an oven for 2 hours; at minus 10 degrees The medium homogenizer was stirred at an ultra-high speed for 2 minutes, and then put into a 10% cholic acid solution and stirred at 600 rpm for 3 hours; after centrifugation, collection, and freeze-drying, the nanoparticles of the final product were obtained.

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Abstract

The invention discloses a nonlinear polymer having a doxorubicin structure, and a preparation method and an application thereof. The doxorubicin coupled nonlinear polymer has better effects on treatment of age-related macular degeneration compared with other forms of drugs or medicaments.

Description

technical field [0001] The invention discloses a non-linear polymer containing a doxorubicin structure and a preparation method and application of the polymer. Background technique [0002] Doxorubicin is an anti-mitotic and highly cytotoxic drug. Doxorubicin successfully inhibits a variety of malignancies, including acute leukemia, lymphoma, soft tissue and osteosarcoma, childhood malignancies, and adult solid tumors. Its mechanism of action is that drugs can penetrate into cells and bind to chromosomes. The planar loops in the drug structure are inserted between base pairs to form complexes with DNA, which seriously interfere with DNA synthesis, DNA-dependent RNA synthesis and protein synthesis. However, the concentration of doxorubicin required to produce an antiproliferative effect through this mechanism is higher than that of the drug at the tumor site in clinical treatment. In addition, doxorubicin is also related to redox, and can participate in the reaction to obt...

Claims

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Application Information

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IPC IPC(8): C08G65/48C08G63/91A61K31/704A61K47/48A61P27/02
Inventor 张雅珍李铁力白毅
Owner 张雅珍
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