Epirubicin VES (vitamin E succinate) compound and preparation method and application thereof

A technology of epirubicin and compound, which is applied in the field of epirubicin VES compound, can solve the problems of drug efficacy, toxicity and side effects, and achieve the effect of high activity and reduced toxicity and side effects

Active Publication Date: 2018-08-24
XIAMEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of the present invention is to overcome the deficiencies of the prior art, provide a kind of epirubicin VES compound and its preparation method and its application, solve the problems of drug efficacy and side effects in the above-mentioned background technology

Method used

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  • Epirubicin VES (vitamin E succinate) compound and preparation method and application thereof
  • Epirubicin VES (vitamin E succinate) compound and preparation method and application thereof
  • Epirubicin VES (vitamin E succinate) compound and preparation method and application thereof

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Embodiment 1

[0029] For an epirubicin VES complex in this embodiment, the mass ratio of epirubicin (or epirubicin hydrochloride) to VES (ie vitamin E succinate) is 1:1.

[0030] The preparation method of the above complex is as follows: 3 mg of epirubicin (or epirubicin hydrochloride) and 3 mg of VES are dissolved in 10 mL of dimethylformamide, and stirred and mixed for 12 hours at 20 ° C to obtain epirubicin The organic solution of mycin VES complex; remove the organic solution to obtain the epirubicin VES complex;

[0031] A preparation method of epirubicin VES composite nanoparticles is as follows: the above-mentioned composite organic solvent (or composite) is dialyzed with deionized water for 8 hours, the molecular weight cut-off of the dialysis bag used in the dialysis is 3500, and the organic solution is removed to obtain epirubicin. Doxorubicin VES complex nanoparticles.

[0032] A preparation method of an epirubicin VES complex sustained-release preparation is as follows: adding ...

Embodiment 2

[0034] 3mg of epirubicin (or epirubicin hydrochloride) and 6mg of VES were dissolved in 10mL of dimethylformamide, stirred and mixed for 12 hours at 20°C to obtain an organic solution of epirubicin VES complex, Then dialyze with deionized water for 8 hours, the molecular weight cut-off of the dialysis bag used in the dialysis is 3500, and remove the organic solution to obtain epirubicin VES complex nanoparticles.

[0035] After that, poloxamer and sodium chloride are added to the epirubicin VES complex nanoparticle solution, and the epirubicin VES complex slow-release preparation is obtained after vacuum freeze-drying.

Embodiment 3

[0037] 3mg of epirubicin (or epirubicin hydrochloride) and 9mg of VES were dissolved in 10mL of dimethylformamide, stirred and mixed for 12 hours at 20°C to obtain an organic solution of epirubicin VES complex, Then dialyze with deionized water for 8 hours, the molecular weight cut-off of the dialysis bag used in the dialysis is 3500, and remove the organic solution to obtain epirubicin VES complex nanoparticles.

[0038] After that, poloxamer and sodium chloride are added to the epirubicin VES complex nanoparticles, and the epirubicin VES complex slow-release preparation is obtained after vacuum freeze-drying.

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Abstract

The invention discloses an epirubicin VES compound and a preparation method and application thereof, and relates to a compound of epirubicin (EPI) and vitamin E succinate (VES) having the antitumor activity and a sustained release preparation thereof, wherein the vitamin E succinate can induce apoptosis of tumor cells with high selectivity while causing no toxic and side effect on normal cells. The compound nano particles of the invention can be obtained through a method of co-assembly and nano precipitation, have the property of slowing release of drugs, can efficiently intake tumor cells, and have relatively wide application prospect in the tumor treatment field. In addition, the compound utilizes different antitumor mechanisms of the vitamin E succinate and the epirubicin to play the strong synergistic effect, the administration dosage of the epirubicin can be reduced, and accordingly the toxic and side effects of the epirubicin are lowered.

Description

technical field [0001] The invention relates to an epirubicin VES complex, a preparation method and application thereof. Background technique [0002] Epirubicin (EPI) is an anthracycline antitumor antibiotic synthesized by Italian scholar Arcamone in 1975 through a semi-synthetic route. The main function of epirubicin is to intercalate directly between DNA base pairs, interfere with the transcription process, and prevent the formation of mRNA. EPI can inhibit the synthesis of DNA and RNA, so it has effects on all stages of the cell cycle, and is a non-specific drug for the cell cycle. EPI acts on both the cell membrane and the transport system, but the most important site of action is the nucleus. In addition, EPI also inhibits topoisomerase II. At present, epirubicin is mainly used clinically for various solid tumors such as acute leukemia and malignant lymphoma, breast cancer, ovarian cancer, bladder cancer, testicular cancer, gastric cancer, and liver cancer. There a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/19A61K47/22A61K31/704A61P35/00
CPCA61K9/19A61K9/5123A61K31/704A61P35/00
Inventor 侯振清李阳侯鲁王衍戈张秀明
Owner XIAMEN UNIV
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