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

A technology of methoxyestradiol and methoxyestradiol, which is applied in the field of medicine, can solve the problems of short half-life, low oral bioavailability, poor water solubility, etc., and achieves improved stability, huge economic benefits and social benefits. Effective, high encapsulation efficiency

Inactive Publication Date: 2009-04-22
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 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

Method used

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

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Weigh 20 mg of 2-methoxyestradiol, 500 mg of egg yolk lecithin and 250 mg of cholesterol, dissolve in 20 ml of ether, dissolve 15 mg of poloxamer-188 in 20 ml of PBS buffer solution (phosphate buffer solution), and then Slowly inject the ether phase into the buffer solution at a constant speed at 50°C, and shake off the ether with magnetic stirring to obtain a milky white liposome suspension. Dissolve 1000mg trehalose in the liposome suspension, and then pass it through a high-pressure milk homogenizer three times or Ultrasonic pulverization process obtains liposome, Co-60 sterilizes, sub-packs with vials, freeze-dries to obtain freeze-dried powder injection, freeze-dried powder injection is redissolved with water for injection, and the encapsulation rate is 85%, The average particle size is 200nm, and the Zeta potential is -25mV.

[0021] The in vitro release results of the product of this example are shown in Table 1, and the results show that the preparation has sust...

Embodiment 2

[0023] Weigh 20mg of 2-methoxyestradiol, 500mg of egg yolk lecithin and 150mg of cholesterol, dissolve in 20ml of ether, remove the ether by rotary evaporation at 37-45°C, and add 20ml of citric acid-sodium citrate buffer at pH 6.0 after film formation The solution (containing 15mg poloxamer-188) was hydrated, 500mg sucrose and 500mg lactose were dissolved in the liposome suspension, liposomes were obtained by ultrasonication, sterilized by Co-60 irradiation, and packed in vials , freeze-dried to obtain a freeze-dried powder injection, and the freeze-dried powder injection was reconstituted with water for injection, and the encapsulation rate was measured to be 80%, the average particle size was 340nm, and the Zeta potential was -30mV.

[0024] The in vitro release results of the product of this example are shown in Table 1, and the results show that the preparation has sustained release capability. The distribution results in rats are shown in Table 2, which shows that it has...

Embodiment 3

[0026] Weigh 20 mg of 2-methoxyestradiol, 1000 mg of egg yolk lecithin, and 200 mg of cholesterol, dissolve them in 30 ml of ether, and dissolve in 20 ml of carbonic acid-sodium carbonate buffer solution (containing 25 mg of poloxamer-188) at pH 6.0. Evaporate the organic solvent on a rotary film under reduced pressure to make it into a colloidal state, and continue the rotary evaporation to form a milky white suspension. Dissolve 1000mg of glucose in the liposome suspension, and reduce the particle size through a high-pressure milk homogenizer three times or ultrasonic pulverization to obtain liposomes, which are sterilized by Co-60 irradiation, subpackaged in vials, and freeze-dried The freeze-dried powder injection was obtained, and the freeze-dried powder injection was reconstituted with water for injection. The measured encapsulation rate was 55%, the average particle diameter was 208nm, and the Zeta potential was -35mV.

[0027]The in vitro release results of the product...

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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 [0001] 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 [0002] 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, liv...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/127A61K31/565A61P35/00
Inventor 张振中杜斌赵娅李赢陈成群王舒雨赵芝兰
Owner ZHENGZHOU UNIV
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