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2-methoxy estradiol vena NANO emulsions

A methoxyestradiol and nanoemulsion technology, applied in the field of medicine, can solve the problems of easily causing hemolysis and allergic reactions, poor clinical treatment compliance, lack of sustained release and targeting, etc.

Inactive Publication Date: 2008-08-27
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 2-Methoxyestradiol is a poorly soluble drug in water, and its solubility in water is less than 5 mg / L. The injection of this type of drug can be an injection suspension, which requires the drug to have a high pharmacological Active, that is, there is a small dosage, and it can only be injected intramuscularly and subcutaneously, but the conventional dosage of 2-methoxyestradiol needs to reach more than 400mg; the second is to use organic solvents as solvents, or use ethanol Polyoxyethylene hydrogenated castor oil is added to the solvent as a solubilizer. The fatal flaw of the injection solution solubilized by organic solvents and surfactants is that it is easy to cause hemolysis and allergic reactions, and lacks sustained release and targeting, such as products already on the market It is clearly stipulated that corticosteroids and antihistamines should be used for desensitization before clinical use. In the process of use, there are still high clinical allergic reactions, which makes the compliance of clinical treatment poor

Method used

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  • 2-methoxy estradiol vena NANO emulsions
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  • 2-methoxy estradiol vena NANO emulsions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 200 mg of 2-methoxyestradiol and 2.0 g of soybean lecithin, dissolve them in 5 ml of chloroform, evaporate to dryness under reduced pressure with a rotary thin-film evaporator, and remove the chloroform to form a drug liquid crystal film. 20g of soybean oil, shake to disperse the liquid crystal film, add 4% glucose solution filtered through a 0.22μm microporous membrane to 100ml, stir to form colostrum, and then go through the micro-jet high-pressure milk homogenizer three times, the operating pressure is 17k psi , use 0.1Mol / L hydrochloric acid or 0.1Mol / L sodium hydroxide to adjust the pH value to 5.5-8.0, filter through a 0.45μm microporous membrane, purify nitrogen flow protection, fill and package, and sterilize with a rotary autoclave at 121°C After 20 minutes, rinse with hot water and gradually cool to room temperature.

[0021] The product of this embodiment, the average particle diameter 240nm, Zeta potential-35mV is measured by the laser scattering parti...

Embodiment 2

[0023]Weigh 150 mg of 2-methoxyestradiol and 1880.9 g of poloxamer, dissolve in 5 ml of chloroform, evaporate to dryness under reduced pressure with a rotary thin-film evaporation to remove the chloroform to form 2-methoxyestradiol and poloxamer Then add 20 g of olive oil filtered through a 0.22 μm microporous membrane, shake to disperse the solid dispersion, add 2.5% glycerin solution filtered through a 0.22 μm microporous membrane to 100 ml, stir to form colostrum, Then go through the micro-jet high-pressure milk homogenizer for three times, the operating pressure is 15k psi, adjust the pH to 5.5-8.0 with 0.1Mol / L hydrochloric acid or 0.1Mol / L sodium hydroxide, filter with a 0.45μm microporous membrane, and protect with purified nitrogen flow Fill and seal, rotate the autoclave at 121°C, sterilize for 20 minutes, pour hot water and gradually cool to room temperature, ready to serve.

[0024] The product of this embodiment, the average particle diameter 290nm, Zeta potential-...

Embodiment 3

[0026] Weigh 250 mg of 2-methoxyestradiol and 2.0 g of egg yolk lecithin, dissolve them in 5 ml of chloroform, evaporate to dryness under reduced pressure with a rotary thin-film evaporation to remove the chloroform to form a drug liquid crystal film, and then add in 0.22 μm microporous membrane filter 30g of soybean oil, shake to disperse the liquid crystal film, add the solution containing 0.5%% poloxamer and 5% sorbitol filtered through a 0.22μm microporous membrane to 100ml, stir to form colostrum, and then pass through the microjet The high-pressure milk homogenizer is homogenized three times, the operating pressure is 16k psi, the pH is adjusted to 5.5-8.0 with 0.1Mol / L hydrochloric acid or 0.1Mol / L sodium hydroxide, the 0.45μm microporous membrane is filtered, the nitrogen flow protection is filled and packaged, and the rotation Autoclave at 121°C, sterilize for 20 minutes, rinse with hot water and gradually cool to room temperature to get ready.

[0027] The product of...

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Abstract

The invention relates to a 2-methoxyestradiol nano-emulsion for intravenous injection. The nano-emulsion contains 0.05-0.5 w / v% of 2-methoxyestradiol, 5-50 w / v% of oil for injection, 0.05-0.5 w / v% of emulsifier, 2-6 w / v% of isoosmotic adjusting agent, pH regulators and water for injection in balance, wherein 2-methoxyestradiol and emulsifier are dissolved with organic solvents and then evaporated under reduced pressure to remove organic solvents completely, so as to obtain a crystalline or solid dispersion of emulsifier; the oil for injection is filtered and then added in the dispersion or water phase is filtered and then added in the dispersion, followed by stirring, to obtain a primary emulsion; the primary emulsion is subjected to a high-pressure homogenizer, the pH regulator is added to regulate the pH value and the water for water is added; and the resulting mixture is further filtered, sealed, sterilized and cooled down to room temperature. The nano-emulsion is suitable for intravenous injection and has properties of sustained release and target drug delivery in vivo. The nano-emulsion has no problems of oral preparations and has high safety and reliability. The invention is an innovation in the medicine field and has significant social and economic benefits.

Description

1. Technical field [0001] The invention relates to the field of medicine, in particular to a nanoemulsion composition composed of a water-insoluble anticancer drug 2-methoxyestradiol and an auxiliary material that can be physiologically accepted by veins: 2-methoxyestradiol intravenous nanoemulsion. 2. Background technology [0002] 2-methoxyestradiol (1,3,5-triene-2,3,17β-trihydroxy-2-methyl ether sterol) is a physiological metabolite of estradiol in vivo (Schumacher G et al. J Cancer Res ClinOncol.127: 405-410, (2001)), has obvious anti-tumor activity, and its anti-cancer mechanism may be the induction of tumor and endothelial cell apoptosis (Lin HL et al. Cancer. 92: 500-509 (2001) ), also anti-tumor angiogenesis (Figg WD ​​et al. Invest New Drug.20: 183-194 (2002)) and its ability to inhibit the proliferation of tumor cells (Kumar AP et al. Carcinog. 31: 111-124 (2001)) . Some scholars have also found that 2-methoxyestradiol inhibits cell proliferation in a time-dose-d...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/24A61K47/34A61K47/44A61K31/565A61P35/00A61K47/10
Inventor 张振中张正全刘伟郭新红胡海英张丽娜宋涵
Owner ZHENGZHOU UNIV
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