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2-methoxyestradiol dry powder inhalant serving as antitumor medicament and preparation method thereof

A methoxyestradiol and antitumor drug technology, applied in the field of medicine, can solve the problems of short administration half-life, poor administration effect, large administration dose, etc., and achieve growth inhibition and metastasis, low administration dose, The effect of dose reduction

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

[0003] For above-mentioned situation, in order to overcome the defective of prior art, the purpose of the present invention is exactly to provide a kind of antineoplastic drug 2-methoxyestradiol dry powder inhalation and preparation method thereof, can effectively solve the problem of 2-methoxyestradiol Poor oral administration effect, high dosage and short half-life of intravenous administration require frequent administration

Method used

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  • 2-methoxyestradiol dry powder inhalant serving as antitumor medicament and preparation method thereof
  • 2-methoxyestradiol dry powder inhalant serving as antitumor medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] In terms of weight percentage: 2-methoxyestradiol 50%, magnesium stearate 5%, lactose 40% and phospholipid 5%, mixed together, dispersed or dissolved in water to form a suspension, and wet Dyno mill (DYNO?-MILL) Grind 2-methoxyestradiol suspended in the solution to 0.5~5μm particles, then spray dry it into dry powder by spray drying method, pack it in plastic capsules, and serve.

Embodiment 2

[0012] In terms of weight percentage: 2-methoxyestradiol 90%, stearic acid 2%, sucrose 5% and oleic acid 3%, mixed together, dispersed or dissolved in water to form a suspension, and wet Dyno mill (DYNO?-MILL) Grind 2-methoxyestradiol suspended in the solution to 0.5~5μm particles, then spray dry it into dry powder by spray drying method, and pack it in aluminum-plastic blisters, that is, become.

Embodiment 3

[0014] In terms of weight percentage: 70% of 2-methoxyestradiol, 1% of magnesium stearate, 28% of mannitol and 1% of oleic acid are mixed together, dispersed or dissolved in water to form a suspension, and worn by wet method Nuomo (DYNO?-MILL) crushes 2-methoxyestradiol suspended in the solution to 0.5~5μm particles, and then sprays and dries it into dry powder by spray drying method, which is packaged in multi-dose dry powder in the form of storage Inhale into device and serve.

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Abstract

The invention relates to a 2-methoxyestradiol dry powder inhalant serving as an antitumor medicament and a preparation method, which can be used for effectively solving the problems of poor oral administration effect and large administration dosage of 2-methoxyestradiol and short half-life period and the need of frequent administration in intravenous injection administration. According to the technical scheme for solving the problems, the 2-methoxyestradiol dry powder inhalant consists of the following components in percentage by weight: 50-90 percent of 2-methoxyestradiol, 0-5 percent of a flow aid, 5-50 percent of a thinner and 0-5 percent of a surfactant, wherein the flow aid is magnesium stearate or stearic acid; the thinner is one or a mixture of more than two of lactose, glucose, cane sugar and mannitol; and the surfactant is one of phospholipid, oleic acid and poloxamer. The antitumor medicament has the advantages of convenience in using, low administration dosage, small toxic and side effects, high stability, high safety and capability of directly reaching a focus, and is an innovation on a treatment means for treating tumors with 2-methoxyestradiol.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an antitumor drug 2-methoxyestradiol dry powder inhalation for treating lung tumors and a preparation method thereof. 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 show that 2-methoxyestradiol has the effect on most cell lines, such as lung cancer, breast cancer, prostate cancer, etc. The half inhibitory conc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/565A61P35/00
Inventor 胡海英张振中张正全刘伟郭新红李雪冰曾肖肖
Owner ZHENGZHOU UNIV
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