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Preparation and application of dendritic polymer grafted with anthracycline antibiotic

A kind of polymer and dendritic technology, applied in the field of dendritic polymers, can solve the problems of low solubility, short half-life, difficult clinical application, etc., and achieve the effect of easy dissolution and excellent effect

Active Publication Date: 2014-07-16
张雅珍
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Anthracycline antibiotics are currently widely used, but they often need to be turned into salts from a clinical point of view, such as doxorubicin. The common pharmaceutical form is doxorubicin hydrochloride, which needs to be turned into hydrochloride. Star itself has very low solubility and cannot be converted into a 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.
[0003] Another disadvantage of anthracycline antibiotics is that due to their strong cytotoxicity, they are very toxic. They often have obvious bone marrow suppression about 10 days after use. After a week of use, they 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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  • Preparation and application of dendritic polymer grafted with anthracycline antibiotic
  • Preparation and application of dendritic polymer grafted with anthracycline antibiotic
  • Preparation and application of dendritic polymer grafted with anthracycline antibiotic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1 A mixture of 80 g of sebacic acid in 800 ml of acetic anhydride was refluxed to form acetylated sebacic acid

[0043] 2 Compound L5 containing a hydroxyl group and a polycarboxylic group: 200mg with Boc-NH-PEG-NH 2 2g is put into the flask and reacted, namely: React with L5, add 160 mg of dicyclohexylcarbodiimide and 8 mg of tetrahydrofuran at the same time, mix and add 15 ml of chloroform, and stir overnight at room temperature; then wash with ether and dry under vacuum to obtain a polyamino end with Boc protection Dendrimer A1:

[0044]

[0045] 3 Compound A1 is catalyzed by trifluoroacetic acid with unit carboxylic acid L3 containing polyalcohol After 30 mg reaction, the dendrimers A2 with polyol endings were obtained by filtration through a cellulose acetate membrane, A2:

[0046]

[0047] Mix acetyl-sebacic acid with compound A2, and react for 1 hour under reduced pressure solution polymerization (high vacuum melt polycondensation) at 175°C; after ...

Embodiment 2

[0057] A mixture of 100 g of sebacic acid in 900 ml of acetic anhydride is refluxed to form acetyl-sebacic acid;

[0058] 2 Compound L5 containing multiple carboxyl groups:

[0059] 46mg with Boc-NH-PEG-NH 2 3g was put into a flask for reaction, while 160mg of dicyclohexylcarbodiimide and 6mg of tetrahydrofuran were put in, mixed with 18ml of dichloromethane, stirred at room temperature overnight; then washed with ether, and dried under vacuum to obtain Protected polyamino-terminated dendrimers A1;

[0060] 3 Compound A1 is catalyzed by trifluoroacetic acid with unit carboxylic acid L3 containing polyalcohol After 45 mg of the reaction, filter through a cellulose acetate membrane to obtain a dendritic compound A2 with a polyol ending, mix acetyl-sebacic acid with the compound A2, and react under reduced pressure at 180°C for 1 hour; wait for the polymer to cool Dissolve with chloroform at room temperature, wash with petroleum ether and dry to obtain dendritic polymer B; ...

Embodiment 3

[0063] A mixture of 2 g of sebacic acid in 20 ml of acetic anhydride was refluxed to form acetyl-sebacic acid;

[0064] 2 Compound L5 containing multiple carboxyl groups: 300mg with Boc-NH-PEG-NH 2 Put 2.5g into a flask for reaction, put 120mg of dicyclohexylcarbodiimide and 5mg of tetrahydrofuran at the same time, mix and add 25ml of chloroform, stir overnight at room temperature; then wash with ether, and dry under vacuum to obtain The polyamino terminated dendrimer A1;

[0065] 3 Compound A1 is catalyzed by trifluoroacetic acid with unit carboxylic acid L3 containing polyalcohol After 30 mg of the reaction, filter through a cellulose acetate membrane to obtain a dendritic compound A2 with a polyol ending, mix acetyl-sebacic acid with compound A2, and react for 1 hour under reduced pressure at 175°C; wait for the polymer to cool Dissolve with chloroform at room temperature, wash with petroleum ether and dry to obtain dendritic polymer B;

[0066] 4 Put the polymer of s...

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Abstract

The invention discloses a dendritic polymer grafted with an anthracycline antibiotic structure, and a preparation method and an application thereof. The anthracycline antibiotic-grafted dendritic polymer has better effects on treatment of age-related macular degeneration disease than other forms of drugs or medicaments.

Description

technical field [0001] The invention discloses a dendritic polymer grafted with an anthracycline antibiotic structure, a preparation method and an application of the polymer. Background technique [0002] Anthracyclines are antimitotic and extremely cytotoxic drugs. Anthracyclines 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 ring in the drug structure is included between the 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, anthracycline antibiotics are ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48C08G63/685C08G63/91A61K31/704A61K47/48A61P27/02A61P9/10
Inventor 张雅珍李铁力白毅
Owner 张雅珍
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