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Macromolecule-cis-platinum compound, preparation method and application thereof

A complex and macromolecular technology, which is applied in the field of macromolecular-cisplatin complexes, can solve the problems of low effective binding rate of cisplatin in the complex drug load, large amount of carrier, and low release rate, etc., to achieve increased effective binding rate, improved release behavior, and reduced drug dose

Inactive Publication Date: 2013-08-21
FANTAI INST OF CHEM MEDICINES NANJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Preparation and biological activity of γ-polyglutamic acid aspartic acid-cisplatin complex [J] China Medical Biotechnology, 2010, 5(2): 98-104.) Amino acid was used as a carrier to link cisplatin to prepare the γ-polyglutamic acid aspartic acid-cisplatin complex. Both of them obtained good results, and the water solubility and toxicity of cisplatin were greatly improved, but the former only used The small molecule γ-polyglutamic acid is used as a carrier, and the drug loading of the prepared complex is only 9-12%, which has the disadvantages of low drug loading, large amount of carrier and low release rate. Although the latter has been improved, the complex The drug loading and the effective binding rate of cisplatin are still low, and the effective binding rate of cisplatin is only 30%.

Method used

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  • Macromolecule-cis-platinum compound, preparation method and application thereof
  • Macromolecule-cis-platinum compound, preparation method and application thereof
  • Macromolecule-cis-platinum compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Preparation and structure characterization of γ-polyglutamic acid

[0048] (1) Degradation conditions

[0049] Weigh an appropriate amount of γ-polyglutamic acid, add distilled water to dissolve to obtain a 2% solution, directly adjust the pH to 2-3 with concentrated hydrochloric acid, react at 121°C and 0.1MPa for 20 minutes, cool in an ice bath, and use 1mol / L Adjust the pH to 7-8 with NaOH, terminate the reaction, purify by dialysis, and freeze-dry to obtain small molecule γ-polyglutamic acid.

[0050] (2) Structural characterization

[0051] Ultraviolet scanning spectrum analysis Take an appropriate amount of dry pure γ-polyglutamic acid, add distilled water to dissolve, and scan in the range of 200-400nm, the results are shown in figure 1 .

[0052] Infrared spectrum analysis Take an appropriate amount of dry pure γ-polyglutamic acid, grind it with a small amount of KBr, and press it into a tablet to prepare a sample. At room temperature, scan in the range of 40...

Embodiment 2

[0055] Synthesis and Structure Characterization of γ-Polyglutamic Acid-Citrate Polymer

[0056] Precisely weigh 129mg of small molecule γ-polyglutamic acid, add 10ml of water to dissolve, stir in ice bath for a while, add EDCI 384mg, NHSS 60mg, continue stirring in ice bath for a while, take 210mg of citric acid and dissolve in appropriate amount of distilled water to adjust pH To neutrality, slowly add it dropwise to the above reaction solution, stir evenly, adjust the pH to 7.5-8.0, stir overnight at room temperature, dialyze against deionized water for 24 hours, and then freeze-dry to obtain the polymer.

[0057] Structural characterization Take an appropriate amount of dry pure polymer of γ-polyglutamic acid-citric acid, dissolve in D 2 In O, H NMR spectroscopy ( 1 HNMR) detection, see the results Figure 4 .

Embodiment 3

[0059] Preparation of γ-polyglutamic acid citrate-cisplatin complex

[0060] Preparation of γ-polyglutamic acid citrate-cisplatin complex Precisely weigh 60 mg of cisplatin, 68 mg of silver nitrate and 100 ml of water to dissolve, react at room temperature in the dark for 24 hours, centrifuge, take the supernatant and filter it through a 0.45 μm filter membrane, collect The filtrate was placed in a 250ml three-necked bottle, and an equivalent amount of the above polymer was added, stirred to dissolve, adjusted to pH 7.5-8.0, reacted at room temperature for 48 hours, dialyzed against deionized water for 24 hours, and then freeze-dried to obtain the drug-loaded complex.

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Abstract

The invention relates to a macromolecule-cis-platinum compound, a preparation method and application thereof. The preparation method comprises the following steps of: degrading or purifying polyamino acid serving as a raw material to obtain a polyamino acid carrier with appropriate molecular weight; performing reaction of a small molecular acid serving as a modifier and side chain active groups of the small molecular acid, modifying a structure of the small molecular acid, and connecting cis-platinum to the polymer skillfully to prepare the medicine-carrying compound. The result of the study on the properties of the medicine-carrying compound indicates that the properties of the medicine-carrying compound are obviously superior to the conventional report, and the prepared compound is low in toxicity and does not have hemolysis.

Description

Technical field: [0001] The invention relates to a macromolecule-cisplatin complex, and provides a preparation method and application of the complex, belonging to the field of preparation of anticancer drugs. Background technique: [0002] Cancer has become the second leading cause of death in humans, and a large amount of human, material and financial resources have been invested in the development of anticancer drugs. At present, there are more than a hundred kinds of anticancer drugs in the world, and these anticancer drugs mainly include cisplatin, paclitaxel, doxorubicin and camptothecin. Most of these anti-tumor drugs used in clinical treatment have high toxicity to tissues, low solubility, difficulty in administration, and many side effects, so there are great limitations in clinical use. [0003] Cisplatin [cis-dichlorodiammineplatinum(II), CDDP] is a heavy metal complex, which is widely used clinically in the treatment of various malignant tumors. Broad spectrum. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K33/24A61P35/00
Inventor 涂家生吴建梅蒋薇薇
Owner FANTAI INST OF CHEM MEDICINES NANJING
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