Prodrug of antitumor medicament as well as preparation method and application thereof

A technology of anti-tumor drugs and prodrugs, applied in the direction of anti-tumor drugs, drug combinations, medical preparations of non-active ingredients, etc., can solve the problem that vitamin E has no anti-tumor effect, so as to improve the anti-tumor effect and improve the long-term Cycle time, toxicity reduction effects

Inactive Publication Date: 2014-06-18
沈阳药大制剂新技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2013, Tang et al. reported that vitamin E is the main structure of the surfactant polyethylene glycol 1000 vitamin E succinate TPGS to overcome tumor multidrug resistance, and has the function of reversing tumor multidrug resistance, but vitamin E alone has no effect. any antitumor effect
[0004] In the prior art, pharmacists use various methods to improve the activity of anti-tumor drugs and reduce toxicity, so as to develop anti-tumor preparations with high efficiency and low toxicity, but the preparation of drugs into prodrugs, especially the method of linking vitamin E technology has not yet been reported

Method used

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  • Prodrug of antitumor medicament as well as preparation method and application thereof
  • Prodrug of antitumor medicament as well as preparation method and application thereof
  • Prodrug of antitumor medicament as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] prescription

[0046] PTX-VE

1g

Vitamin E

9g

TPGS

4g

buffered saline solution to

500mL

[0047] Weigh or measure the prodrug, injection oil and emulsifier according to the formula, mix and stir to dissolve at 20-80°C to obtain the oil phase, measure water for injection according to the formula, and add an appropriate amount of isotonic regulator to obtain the water phase , the oil phase and the water phase are mixed at 20-80°C, and the colostrum is prepared by shear emulsification or stirring emulsification; the colostrum is prepared by high-pressure homogenizer, ultrasonic emulsification, colloid mill emulsification dispersion or microfluidizer Prodrug injection emulsion was obtained.

[0048] The prodrug of vitamin E and paclitaxel of the present invention has better pharmacokinetic behavior. Rats were administered by intravenous injection, and the same dose of vitamin E-paclitaxel-linked prodrug emulsion and Taxo...

Embodiment 2

[0053] PTX-VE

[0054] The preparation method is the same as in Example 1.

Embodiment 3

[0056] PTX-S-VE

[0057] The preparation method is the same as in Example 1.

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PUM

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Abstract

The invention belongs to the technical field of medicines and relates to a prodrug of an antitumor medicament as well as a preparation method and application thereof. The prodrug is prepared by connecting vitamin E and the antitumor medicament by virtue of a chemical bond. The chemical bond is one of a sulfide bond, an ester bond, an interval disulfide bond and a hydrazone bond. The antitumor medicament is one of paclitaxel and docetaxel. The prodrug of the antitumor medicament and a pharmaceutically acceptable carrier can be prepared into a clinically acceptable dosage form for injection or oral administration, including lipidosome, an emulsion, a lipid microsphere and a PLGA (Poly(Lactic-co-Glycolic Acid) nanoparticle or microsphere. According to the prodrug and the preparation, the activity of the antitumor medicament can be obviously improved, the toxicity is reduced and the development of the preparation is facilitated.

Description

technical field [0001] The present invention relates to a prodrug of an antineoplastic drug, in particular to a prodrug of an antineoplastic drug and its preparation method and use. Background technique [0002] Paclitaxel, docetaxel, doxorubicin, 5-fluorouracil, etc. are currently the most widely used antineoplastic drugs, and have good curative effects in the treatment of multisystem tumors. However, paclitaxel and docetaxel have the disadvantage of being insoluble in both water and oil. Adriamycin and 5-fluorouracil have good water solubility but poor fat solubility. Great difficulty came. In addition, commonly used clinically used anti-tumor preparations have the disadvantage of high toxicity and side effects. For example, Taxol, a paclitaxel preparation, uses a 1:1 mixture of surfactant polyoxyethylene castor oil and absolute ethanol to dissolve paclitaxel and dilute it before use. Conversion, paclitaxel is easy to precipitate and precipitate, and the solubilizer poly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/337C07D407/12A61P35/00
Inventor 刘锋何仲贵王永军刘丹付强王钝
Owner 沈阳药大制剂新技术有限公司
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