2-methoxyestradiol lipidosome freeze-dried injection and preparation method thereof

Abstract

The invention relates to 2-methoxyl estradiol lipidosome freeze-dried powder injection and a preparation method thereof. The invention can effectively solve the problems of poor water solubility of 2-methoxyl estradiol, short half-life and low oral administration bioavailability, and adopts the technical proposal that the 2-methoxyl estradiol lipidosome freeze-dried powder injection comprises the following raw materials in weight portion: 1 portion of the 2-methoxyl estradiol, 3 to 100 portions of phospholipid, 1 to 30 portions of cholesterol, surfactant and freeze-dried preservative, wherein according to the weight ratio of the phospholipid, 0.1 to 10 portions of the freeze-dried preservative is added into 1 portion of the phospholipid, and the adding quantity of the surfactant is 0.2 to 3 percent of the total amount of the freeze-dried powder injection. The freeze-dried powder injection using the components as raw materials can be realized by three preparation methods, namely, a film dispersion method, a reverse phase evaporation method and an injection method, has high medicament content, is suitable for intravenous administration, has the advantages of slow release capability, in vivo targeting property and the like, can overcome the defects of oral preparations, is safe and reliable, and has large economic benefit and social benefit.

Description

1. Technical field The invention relates to the field of medicine, in particular to a nano-liposome complex composed of a water-insoluble antitumor drug 2-methoxyestradiol and an auxiliary material with good physiological compatibility: 2-methoxyestradiol lipid Plastid freeze-dried powder injection and preparation method thereof. 2. Background technology 2-Methoxyestradiol (1,3,5-triene-2,3,17β-trihydroxy-2-methyl ether sterol) referred to as 2-ME, is a steroid hormone compound, belonging to a new type of hormone Anti-tumor drugs are a physiological metabolite of natural steroids in the body, and studies have shown that they have very significant anti-tumor activity. Can induce tumor and endothelial cell apoptosis (Lin H.L. et al. Cancer.92 (2001): 500-509), has the effect of inhibiting neovascularization and tumor cell growth (Barchiesi F. et al. Circ.Res.99 (2006) :266-274), studies have shown that it has very significant anti-tumor activity (myeloma, liver cancer, lung ...

AI Technical Summary

Problems solved by technology

In view of the above situation, in order to overcome the defects of the prior art, the object of the present invention is to provide a kind of 2-methoxyestradiol liposome freeze-dried powder injection and preparation method thereof, which can effectively solve the problem of 2-methoxyestradiol Its water-solubility of diol is poor, and half-life is short, and the problem of oral bioavailability is low, and the technical scheme of its solution is, 2-methoxyestradiol liposome freeze-dried powder injection of the present invention is by weight ratio: 2 - 1 part of methoxyestradiol, 3 to 100 parts of phospholipids, 1 to 30 parts of cholesterol, surfactants and freeze-drying protective agents as raw materials, the addition of said freeze-drying protective agents is based on the weight ratio of phospholipids Calculated, add 0.1 to 10 parts of lyoprotectant to 1 part of phospholipid, and the amount of surfactant added is 0.2 to 5% of the total amount of lyophilized powder injection

Images