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

A doxorubicin and polymer technology, which can be used in medical preparations containing active ingredients, medical preparations without active ingredients, organic active ingredients, etc., can solve the problems of low solubility, short half-life, high toxicity, etc. Easy to dissolve, extended half-life, excellent results

Active 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

[0042] 1) The mixture of 80 g of sebacic acid in 800 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0043] 2) Mix the 10g product of step 1) and 3-arm polyethylene glycol ending in a hydroxyl group into a flask, and conduct a solution polymerization reaction under reduced pressure at 180°C for 1 hour; when the polymer is cooled to room temperature, dissolve it with chloroform, and use petroleum washed with ether and dried;

[0044] 3) Put 120mg of doxorubicin and the 800mg polymer of step 2 into 8ml of dimethyl sulfoxide and 12ml of dichloromethane solution for 48 hours; ultrasonic for 3 minutes; then place in an oven for 1 hour; Stir at a high speed in a homogenizer at 20°C for 3 minutes, then put into 1% polyvinyl alcohol solution and stir at 600 rpm for 2 hours; collect by centrifugation and freeze-dry to obtain the nanoparticles of the final product.

Embodiment 2

[0046] 1) The mixture of 100 g of sebacic acid in 900 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0047] 2) Mix the product of step 1) and 18 g of 3-arm polyethylene glycol ending in a hydroxyl group into a flask, and conduct a solution polymerization reaction under reduced pressure at 180° C. for 1 hour; when the polymer is cooled to room temperature, dissolve it with chloroform, and use petroleum washed with ether and dried;

[0048] 3) Put 200mg of doxorubicin and 1000mg of the polymer in step 2 into 6ml of dimethyl sulfoxide and 14ml of dichloromethane solution for 24 hours; ultrasonic for 2 minutes; then put in an oven for 2 hours; at minus 10 degrees Stir in a medium homogenizer at an ultra-high speed for 2 minutes, then put into 10% cholic acid solution and stir at 600 rpm for 3 hours; collect by centrifugation and freeze-dry to obtain the nanoparticles of the final product.

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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, a preparation method and an application of the polymer. Background technique [0002] Doxorubicin is an antimitotic and extremely cytotoxic drug. Doxorubicin can successfully inhibit a variety of malignancies, including acute leukemia, lymphoma, soft tissue and osteosarcoma, childhood malignancies, and adult solid tumors. Its mechanism of action is that the drug can penetrate into the cell and bind to the chromosome. The planar loop in the drug structure is inserted between base pairs to form a complex with DNA, which seriously interferes 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 the concentration of the drug at the tumor site in clinical treatment. In addition, doxorubicin is also related to the redox effect, and ...

Claims

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Application Information

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