Antineoplastic 2-methoxyestradiol injection containing cyclodextrin or cyclodextrin derivates

Abstract

The invention relates to 2-methoxyestradiol injection, an anti-tumor drug containing cyclodextrin or cyclodextrin derivatives, and solves the problem that 2-methoxyestradiol is hard to be dissolved in water. The technical scheme to be solved is as follows: the anti-tumor drug, that is, the 2-methoxyestradiol injection containing cyclodextrin or cyclodextrin derivatives, is prepared from 2-methoxyestradiol and cyclodextrin or cyclodextrin derivatives with the mole ratio being 1:(2-10); and the mass concentration of 2-methoxyestradiol in the final water solution of the 2-methoxyestradiol injection is 0.1mg / ml to 25mg / ml. The invention is prepared by mixing 2-methoxyestradiol and cyclodextrin or cyclodextrin derivatives having good water solubility and biocompatibility, thereby effectively solving the problem that 2-methoxyestradiol is hard to be dissolved in water, avoiding the allergic reaction, greatly reducing the hemolytic activity and ensuring good cell inhibitory activity and highstability. The invention is an innovation in the field of medicine.

Description

1. Technical field [0001] The invention relates to the medical field, in particular to an antitumor drug 2-methoxyestradiol injection containing cyclodextrin or a cyclodextrin derivative. 2. Technical background [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 has anti-tumor angiogenesis (Figg WD ​​et al. Invest New Drug. 20: 183 ~ 194 (2002)) and it can 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-dependent manner in the study of the effect of 2-methoxyestradiol on myeloma cells, and its inhibitory effect is the...

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Problems solved by technology

[0003] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a kind of antitumor drug 2-methoxyestradiol injection containing cyclodextrin or cyclodextrin derivatives, which can effectively solve the problem of 2-methoxyestradiol injection. The problem that base estradiol is difficult to dissolve in water, the technical scheme of its solution is, the antitumor drug containing cyclodextrin or cyclodextrin derivative made from 2-methoxyestradiol and cyclodextrin or cyclodextrin derivative Drug 2-methoxyestradiol injection, the molar ratio of 2-methoxyestradiol and cyclodextrin or cyclodextrin derivatives is 1:2~10, the final aqueous solution of 2-methoxyestradiol injection The mass concentration of 2-methoxyestradiol in the medium is 0.1mg / ml~25mg / ml, and the said cyclodextrin derivatives are hydroxypropyl β-cyclodextrin, hydroxyethyl β-cyclodextrin, methyl Any of β-cyclodextrin, glucosyl β-cyclodextrin, maltosyl β-cyclodextrin, sulfonate β-cyclodextrin

The invention has good water solubility and good biocompatibility by mixing cyclodextrin or cyclodextrin derivatives with 2-methoxyestradiol, thereby effectively solving the problem that 2-methoxyestradiol is difficult to dissolve in water. No allergic reaction, significantly reduced hemolytic activity and good cytostatic activity, high stability, is an innovation in the medical field

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