Doxorubicin prodrug, its preparation method and injectable composition

A technology of doxorubicin and composition, applied in the field of doxorubicin prodrug and its injectable pH-sensitive hydrogel, can solve the problems of drug toxicity damage, increase patient pain, inability to distinguish, etc. The effect of long cleaning time and high safety

Active Publication Date: 2013-11-06
SOUTHERN MEDICAL UNIVERSITY
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Problems solved by technology

[0002] Cancer is a high-incidence and fatal disease. Although current chemotherapy drugs can kill cancer cells, they often cannot distinguish between no

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  • Doxorubicin prodrug, its preparation method and injectable composition
  • Doxorubicin prodrug, its preparation method and injectable composition
  • Doxorubicin prodrug, its preparation method and injectable composition

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[0046] The preparation method of the aforementioned adriamycin prodrug includes the following steps:

[0047] Dissolve MPEG-hydrazide and adriamycin in an anhydrous polar solvent, stir to complete the reaction, add excess triethylamine to continue the reaction to completion, and purify the adriamycin prodrug, named MPEG-DOX.

[0048] As a further improvement of the present invention, the MPEG-hydrazide synthesis method includes the following steps:

[0049] 1) Dissolve excess hydrazine sulfate salt in water and adjust its pH to alkaline to obtain reaction solution A;

[0050] 2) Add methoxypolyethylene glycol succinimide acetate into reaction solution A, stir the reaction to completion, dialyze to remove unreacted small molecules, and freeze-dry to obtain purified MPEG-hydrazide.

[0051] As a further improvement of the present invention, adding NaOH solution to adjust the pH of the hydrazine sulfate solution to 8.5~10. The molecular weight of the hydrazine sulfate salt is small and eas...

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Abstract

The invention discloses a doxorubicin prodrug, its preparation method and an injectable composition. The doxorubicin prodrug is formed by hydrazone key-type connection between MPEG and DOX. The preparation method of the doxorubicin prodrug is simple; requirements on reaction conditions are low; yield is high; and production costs are easier to control. The prodrug has low immunity and can effectively raise water solubility of doxorubicin. In addition, it will take a long time to remove the doxorubicin prodrug in vivo such that action time of the drug can be effectively prolonged. The doxorubicin prodrug has pH sensitivity and can release doxorubicin in situ in an acidic pH environment and simultaneously form PEG. The doxorubicin prodrug composition can be dissolved in an approximately-neutral aqueous solution to form an aqueous solution with stable performance. When pH changes to acid, supermolecule hydrogel can be formed within minutes. Long-acting in situ release of doxorubicin can be achieved. Doxorubicin diffusion can be effectively avoided. Functions of normal cells are influenced. Toxic and side effect of the drug is reduced.

Description

technical field [0001] The invention relates to a prodrug and a novel medicament prepared by using the prodrug, in particular to a doxorubicin prodrug and an injectable pH sensitive hydrogel. Background technique [0002] Cancer is a high-incidence and fatal disease. Although current chemotherapy drugs can kill cancer cells, they often cannot distinguish between normal cells and cancer cells and have corresponding side effects, causing normal tissues to be damaged by drug toxicity and increasing patient suffering. The methods to increase drug efficacy mainly include improving drug targeting selectivity and increasing the concentration of locally active drugs. At present, intravenous administration is the main way for drugs to reach solid tumors. The circulatory system and tumor arterial blood supply determine the effect of drug administration. Compared with intravenous administration, the method of local injection of drug hydrogel has the following advantages: [0003] 1....

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Application Information

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IPC IPC(8): A61K47/48A61K47/40A61K31/704A61K9/00A61P35/00
CPCA61K9/0019A61K47/40A61K47/60A61P35/00C07D309/14
Inventor 欧阳钧邢孟秋陈骏
Owner SOUTHERN MEDICAL UNIVERSITY
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