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

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...

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 the agent, 2% to 6% of the isotonic regulator, the pH regulator and the balance are made of water for injection, and the preparation process is complicated.

[0006] There is no relevant report on self-emulsifying 2-methoxyestradiol intravenous injection