Tumor targeted mitomycin C and MTX (methotrexate) double-drug preparation and preparation method thereof

A mitomycin and tumor-targeting technology, which is applied in the field of pharmaceutical anti-tumor drug preparations, can solve the problems of no double-drug or multi-drug coordinated treatment effect, large dose, etc., and achieve strong targeting and good sustained-release characteristics , strong anti-tumor effect

Inactive Publication Date: 2015-02-18
XIAMEN CHITOSAN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the products of the former two invention patents can achieve the effect of targeted sustained-release treatment of tumors, the dosage is relatively large when used alone, and there is no dual-drug or multi-drug coordinated treatment effect

Method used

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  • Tumor targeted mitomycin C and MTX (methotrexate) double-drug preparation and preparation method thereof
  • Tumor targeted mitomycin C and MTX (methotrexate) double-drug preparation and preparation method thereof
  • Tumor targeted mitomycin C and MTX (methotrexate) double-drug preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0022] Weigh soybean lecithin and mitomycin (molar ratio: 4:1), put them in a round bottom beaker, add an appropriate amount of tetrahydrofuran to dissolve, react in a water bath at 40°C for 4 hours, remove the reaction solvent tetrahydrofuran under reduced pressure, and then add an appropriate amount of trihydrofuran Wash with methyl chloride, collect the solution by filtration, and dry by rotary evaporation to obtain a purple viscous substance, which is the mitomycin-lecithin complex;

[0023] Dissolve mitomycin lecithin complex, DSPE-PEG and MTX prodrug in dimethyl sulfoxide, add 2 times of deionized water, stir well, and use 3500 molecular weight dialysis bag for dialysis;

[0024] After dialysis for 8 hours, the dialysate was filtered with a 200 nm microporous membrane to obtain a micellar solution of a tumor-targeting dual-drug preparation of mitomycin C and methotrexate, which was lyophilized to obtain a nanomicelle preparation. The drug loading of the preparation prepa...

example 2

[0026] Weigh 300.0 mg of soybean lecithin and 102.8 mg of mitomycin (molar ratio: 3:1), put them in a round bottom beaker, add an appropriate amount of tetrahydrofuran to dissolve, react in a water bath at 40°C for 4 hours, remove the reaction solvent tetrahydrofuran under reduced pressure, and then Add an appropriate amount of dichloromethane to wash, collect the solution by filtration, and dry by rotary evaporation to obtain a purple viscous substance, which is the mitomycin-lecithin complex;

[0027] Dissolve mitomycin-lecithin complex, DSPE-PEG and MTX prodrug in dimethylformamide, add 2 times of deionized water, stir evenly, and use 3500 molecular weight dialysis bag for dialysis;

[0028] After dialysis for 6 hours, the dialysate was filtered with a 200 nm microporous membrane to obtain a micellar solution of a tumor-targeting dual preparation of mitomycin C and methotrexate, which was lyophilized to obtain a nanomicelle preparation. The drug loading of the preparation p...

example 3

[0030] Weigh 200.0 mg of soybean lecithin and 102.8 mg of mitomycin (molar ratio: 2:1), put them in a round bottom beaker, add an appropriate amount of tetrahydrofuran to dissolve, react in a water bath at 50°C for 3 hours, remove the reaction solvent tetrahydrofuran under reduced pressure, and then Add an appropriate amount of dichloromethane to wash, collect the solution by filtration, and dry by rotary evaporation to obtain a purple viscous substance, which is the mitomycin-lecithin complex;

[0031] Dissolve the split mycin lecithin complex, DSPE-PEG and MTX prodrug in dimethylformamide, add 3 times of deionized water, stir well, and then use a 3500 molecular weight dialysis bag for dialysis;

[0032] After dialysis for 8 hours, the dialysate was filtered with a 200 nm microporous membrane to obtain a micellar solution of a tumor-targeting dual-drug preparation of mitomycin C and methotrexate, which was lyophilized to obtain a nanomicelle preparation. The drug loading of t...

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Abstract

The invention relates to the field of medical anti-tumor drug preparations, in particular to a tumor targeted mitomycin C and MTX (methotrexate) double-drug preparation for preventing malignant tumor growth and recurrence and a preparation method of the double-drug preparation. The tumor targeted mitomycin C and MTX double-drug preparation comprises a crude drug of mitomycin C, a carrier material and an MTX prodrug with targeting and anti-cancer functions, wherein the carrier material adopts lecithin and DSPE-PEG (distearoyl phosphoethanolamine-polyethylene glycol), and the MTX prodrug adopts DSPE-PEG-MTX. The tumor targeted mitomycin C and MTX double-drug preparation is spherical, has the grain diameter distributed between 20 nm and 80 nm, is suitable for being used as an intravenous injection preparation and has the characteristics of high targeting, long circulation, low toxicity and collaborative treatment.

Description

technical field [0001] The invention relates to the field of pharmaceutical antitumor drug preparations, in particular to a tumor-targeting dual drug preparation of mitomycin C and methotrexate for preventing the growth and recurrence of malignant tumors and a preparation method thereof. Background technique [0002] Mitomycin C (MMC), Mr 334.37, an aziridine derivative, is an antitumor antibiotic isolated from the culture medium of the actinomycete Streptomyces caespitosus, and belongs to the cell cycle non-specific antitumor drug , Broad anti-tumor spectrum. Its mechanism of action is: after the carbamoyl group and aziridine functional group with alkylation function in the MMC molecule are activated under certain circumstances, they become different dissociation states. The main role of activated MMC is to form cross-links between complementary DNA double bonds, thereby inhibiting DNA replication and synthesis of tumor cells, rather than directly affecting RNA. When mito...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K47/48A61K9/51A61P35/00A61K31/407
CPCA61K9/1075A61K31/407A61K31/519A61K47/24A61K47/60
Inventor 侯振清蔺金燕侯鲁
Owner XIAMEN CHITOSAN BIO TECH
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