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.