Self-emulsified 2-methoxyestradiol intravenous injection and preparation method thereof

A technology of methoxyestradiol and injection, applied in the field of self-emulsifying 2-methoxyestradiol intravenous injection and its preparation, can solve the problem of self-emulsifying 2-methoxyestradiol intravenous injection, preparation Complicated process and other issues, to achieve good industrialization and commercialization prospects, simple preparation process, high drug loading effect

Inactive Publication Date: 2017-12-01
HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The Chinese invention patent 2-methoxyestradiol intravenous nanoemulsion whose publication number is CN 101249070A consists of 0.05% to 0.5% of 2-methoxyestradiol in weight to volume ratio, 5% to 50% of injection oil, emulsified 0.05% to 5% of

Method used

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Effect test

Embodiment 1

[0033] The self-emulsifying 2-methoxyestradiol intravenous injection of the present invention is made of the following raw materials in percentage by weight: 10% of 2-methoxyestradiol, 10% of saturated caprylic triglyceride, 15% of soybean lecithin, ethanol 65%.

[0034] The preparation method of self-emulsifying 2-methoxyestradiol intravenous injection of the present invention comprises the following steps:

[0035] Mix the formula amount of saturated caprylic triglyceride, soybean lecithin, and ethanol evenly, dissolve, add the formula amount of 2-methoxyestradiol to dissolve, and then form a clear and transparent self-emulsifying 2-methoxyestradiol preparation. When in use, take 1 mL of the injection and add it to 5 mL of normal saline, and shake gently to form an emulsion. The particle size is 156 nm and the PDI is 0.152 as measured by dynamic light scattering.

Embodiment 2

[0037] The self-emulsifying 2-methoxyestradiol intravenous injection of the present invention is made of the following raw materials in percentage by weight: 5% of 2-methoxyestradiol, 10% of soybean oil, 50% of Tween80 and 35% of propylene glycol.

[0038] The preparation method of self-emulsifying 2-methoxyestradiol intravenous injection of the present invention comprises the following steps:

[0039] Mix the soybean oil, Tween80 and propylene glycol in the formulated amount evenly, dissolve them, add the 2-methoxyestradiol in the formulated amount to dissolve, and then form a clear and transparent 2-methoxyestradiol self-emulsifying preparation. When in use, take 1 mL of the injection and add it to 5 mL of 5% glucose, and shake gently to form an emulsion with light blue opalescence. The particle size is 56 nm and PDI 0.152 as measured by dynamic light scattering.

Embodiment 3

[0041] The self-emulsifying 2-methoxyestradiol intravenous injection of the present invention is made of the following raw materials in percentage by weight: 1% 2-methoxyestradiol, 5% soybean oil, 40% Pluronic F68, polyethylene glycol 400 54%.

[0042] The preparation method of self-emulsifying 2-methoxyestradiol intravenous injection of the present invention comprises the following steps:

[0043] Mix the soybean oil, Pluronic F68, and polyethylene glycol 400 in the formulated amount, dissolve them, add the 2-methoxyestradiol in the formulated amount, and dissolve to form a clear and transparent self-emulsifying 2-methoxyestradiol preparation.

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Abstract

The invention relates to a self-emulsified 2-methoxyestradiol intravenous injection and a preparation method thereof, and belongs to the field of medicinal preparation. The self-emulsified 2-methoxyestradiol intravenous injection comprises, by weight, 0.1-10% of 2-methoxyestradiol, 4.9-30% of oil for injection, 10-80% of emulsifier and 0-85% of co-emulsifier. The prepared self-emulsified 2-methoxyestradiol intravenous injection is high in drug-loading rate and good in stability and has a certain targeting ability, the efficacy is increased, the toxic and side effects are reduced, and safety is good; and the preparation technology is simple, the cost is low, and good industrialization and commercialization prospects are achieved.

Description

technical field [0001] The invention relates to a self-emulsifying 2-methoxyestradiol intravenous injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] 2-Methoxyestradiol is a steroid hormone compound, an endogenous metabolite of estradiol, and belongs to a new type of hormone antitumor drug. Since the 1990s, a large number of studies have shown that 2-methoxyestradiol has the effects of inducing tumor cell apoptosis and differentiation, anti-tumor angiogenesis, and inhibiting tumor cell proliferation. , breast cancer, liver cancer, gastric cancer, etc., have anti-tumor activity. [0003] Clinical studies have shown that 2-methoxyestradiol is active orally, but, like other steroid hormones, 2-ME has poor solubility, the solubility in water is about 2μg / mL, and the bioavailability after oral administration is low, and After oral administration, its pharmacokinetics in vivo are irregular, and there is...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/14A61K47/24A61K47/10A61K47/44A61K47/26A61K47/12A61K47/22A61K47/28A61K31/565A61P35/00
CPCA61K9/0019A61K9/107A61K31/565A61K47/10A61K47/12A61K47/14A61K47/22A61K47/24A61K47/26A61K47/28A61K47/44
Inventor 和素娜李杰李瑞芳王建刚吴银萍王学廷
Owner HENAN UNIV OF SCI & TECH
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