Sustained-release microsphere injection containing antitumor drug (2-methoxyestradiol)

A technology of methoxyestradiol and anti-tumor drug, applied in the field of medicine, can solve problems such as side effects, unsatisfactory tumor treatment effect, etc., and achieve the effect of improving curative effect

Inactive Publication Date: 2012-11-28
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a kind of sustained-release microsphere injection c...

Method used

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  • Sustained-release microsphere injection containing antitumor drug (2-methoxyestradiol)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] By weight percentage: 0.5% of 2-methoxyestradiol and 99.5% of slow-release excipients are mixed together, dissolved in dichloromethane, filtered with a membrane-type inorganic microporous glass membrane, collected microspheres, washed with water, After drying at room temperature for 48 hours, the slow-release microspheres were obtained, subpackaged, and sterilized by radiation for later use; 0.5~3.0% carboxymethylcellulose sodium salt was filtered through a 0.22 μm microporous membrane to obtain a microsphere suspension medium, and divided ready to use after autoclaving; before use, suspend 5% of the slow-release microspheres and 95% of the microsphere suspension medium in terms of weight percentage; the slow-release excipients have a peak molecular weight of 1- 30,000 polylactic acid.

Embodiment 2

[0024] In terms of weight percentage: 30% of the effective anti-tumor drug and 70% of the slow-release auxiliary material are mixed together, dissolved in chloroform, filtered with a membrane tubular inorganic microporous glass membrane, collected microspheres, washed with water, and dried at room temperature in vacuum for 48 Hours later, the slow-release microspheres will be subpackaged and sterilized by radiation for later use; filter 0.1-2% chitosan through a 0.22 μm microporous membrane to obtain a microsphere suspension medium, subpackaged, and then sterilized by autoclaving for later use ; Before use, by weight percentage: 30% of slow-release microspheres and 70% of microsphere suspension medium are suspended; the effective anti-tumor drug is: by weight percentage: 2-methoxy A compound of 5% estradiol and 95% paclitaxel; the sustained-release auxiliary material is a copolymer of 10-90% lactic acid and 10-90% glycolic acid with a peak molecular weight of 40,000-60,000 perc...

Embodiment 3

[0026]In terms of weight percentage: 50% of effective anti-tumor drugs and 50% of sustained-release excipients are mixed together, dissolved with supercritical fluid carbon dioxide, filtered with a membrane-type inorganic microporous glass membrane, collected microspheres, washed with water, and dried at room temperature in vacuum After 48 hours, the slow-release microspheres were obtained, subpackaged, and sterilized by radiation for later use; 0.1~2% tragacanth gum was filtered through a 0.22 μm microporous membrane to obtain a microsphere suspension medium, subpackaged, and autoclaved for later use use; before use, by weight percentage: slow-release microsphere 50% and microsphere suspension medium 50% suspension; A compound of 95% estradiol and 5% tarequita; the sustained-release excipient is poly 3-hydroxybutyric acid with a peak molecular weight of 70,000-100,000.

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Abstract

The invention relates to a sustained-release microsphere injection containing an antitumor drug (2-methoxyestradiol), and the sustained-release microsphere injection can be used for effectively solving the problems that a conventional drug delivery system for 2-methoxyestradiol is not ideal in tumor treatment effect and has side effects. The technical scheme adopted for solving the problems is as follows: the sustained-release microsphere injection consists of the following parts by weight percent: 5-50% of sustained-release microspheres and 50-95% of solvent system, or independent sustained-release microsphere. The sustained-release microsphere injection can be used for realizing the purpose that the effect of drug can be sustained for a long time by one-time drug delivery, and overcoming the defects and shortcomings of a conventional 2-methoxyestradiol delivery system; and according to the sustained-release microsphere injection, the effective blood concentration can be maintained in the body for a long time, the dosage amount is only 1/30 that of the conventional drug delivery, the tumor inhibiting efficiency is 62% and is higher than that of the intravenous injection drug delivery by about 45%. The sustained-release microsphere injection can be used for reducing the dosage of the drug (toxic and side effects) and has the obvious advantages of improving the drug therapeutic effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a sustained-release microsphere injection containing antitumor drug 2-methoxyestradiol for injection in or around tumors. Background technique [0002] 2-Methoxyestradiol is a natural metabolite of estrogen in the body. It has a wide range of anti-tumor activities at an appropriate concentration, and has time- and dose-dependent pharmacological characteristics. 2-Methoxyestradiol is water-soluble Poor activity (about 0.22μg / ml), poor oral absorption efficiency, and lack of correlation between dose and blood drug concentration after oral administration, and the maximum oral blood drug concentration is less than 100ng / ml (Jehana James et al .Invest new drugs.25:41-48(2006), but the in vitro pharmacodynamic studies of most tumor cell lines showed that 2-methoxyestradiol inhibited half of most cell lines, such as breast cancer, prostate cancer, etc. Concentration (IC 50 ) are grea...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/16A61K31/565A61K31/675A61K38/13A61K47/36A61K47/38A61P35/00
Inventor 张振中张正全胡海英刘伟郭新红连晓培王文佳张建平杨兰侠
Owner ZHENGZHOU UNIV
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