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Mifepristone lipidosome preparation and preparation method thereof

A technology of mifepristone lipid and mifepristone, which is applied in the direction of liposome delivery, medical preparations of non-active ingredients, and pharmaceutical formulations, and can solve the problems of long retention time, poor solubility of mifepristone, and packaging High encapsulation rate and other issues, to achieve the effect of reducing intake, broadening clinical application, and high encapsulation rate

Inactive Publication Date: 2014-08-06
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the present invention, mifepristone is encapsulated in liposomes, the encapsulation rate is high, no solid is separated out, and the problem of poor solubility of mifepristone is solved, and the addition of polyethylene glycol derivatized phospholipids makes the liposomes The preparation has a longer retention time in the body

Method used

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  • Mifepristone lipidosome preparation and preparation method thereof
  • Mifepristone lipidosome preparation and preparation method thereof
  • Mifepristone lipidosome preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Accurately weigh 100 mg of egg yolk lecithin, 10 mg of cholesterol, 5 mg of PEG2000-DSPE, and 8 mg of mifepristone and dissolve them in 10 ml of dichloromethane. Remove the dichloromethane under pressure, and after forming a uniform transparent film on the wall of the eggplant-shaped flask, add 10 ml of 0.02 mol / L pH 7.2 phosphate buffer solution, and continue to rotate in a water bath at 37°C for 30 minutes under normal pressure to make the film swell and hydrate , and the resulting suspension was ultrasonically treated with a cell pulverizer for 5-10 min in an ice bath to obtain a mifepristone liposome solution. Add 10 ml of 0.02 mol / L pH 7.2 phosphate buffer solution for dilution, add 2.0 g of sucrose as a freeze-drying protectant, filter and sterilize with a 0.22 μm microporous membrane, and pack to obtain the finished product. The finished product can be stored at 2°C-8°C or freeze-dried to make freeze-dried powder for injection. After determination, the encapsula...

Embodiment 2

[0029] Accurately weigh 100 mg of egg yolk lecithin, 10 mg of cholesterol, and 8 mg of mifepristone and dissolve them together in 10 ml of dichloromethane. After forming a uniform transparent film on the wall of the eggplant-shaped flask, add 10 ml of 0.02mol / L pH 7.2 phosphate buffer solution, and continue to rotate in a water bath at 37°C under normal pressure for 30 minutes to make the film swell and hydrate, and the resulting suspension Under ice bath, use a cell pulverizer to sonicate for 5-10 minutes to obtain mifepristone liposome solution. Add 10 ml of 0.02 mol / L pH 7.2 phosphate buffer solution for dilution, add 2.0 g of sucrose as a freeze-drying protectant, filter and sterilize with a 0.22 μm microporous membrane, and pack to obtain the finished product. The finished product can be stored at 2°C-8°C or freeze-dried to make freeze-dried powder for injection. It was determined that the encapsulation efficiency of the liposome sample obtained according to the above st...

Embodiment 3

[0031]Accurately weigh 100 mg of egg yolk lecithin, 10 mg of cholesterol, 8 mg of polyethylene glycol derivatized phospholipid PEG2000-PE, and 15 mg of mifepristone, and dissolve them in 10 ml of dichloromethane, and place the resulting solution in a 250 ml eggplant-shaped In the flask, dichloromethane was removed under reduced pressure in a water bath at 37°C. After a uniform transparent film was formed on the wall of the eggplant-shaped flask, 10 ml of 0.02 mol / L pH 7.2 phosphate buffer solution was added, and the water bath was continued at 37°C under normal pressure. Rotate for 30 minutes to make the film swell and hydrate, and the resulting suspension is ultrasonically treated with a cell pulverizer for 5-10 minutes in an ice bath to obtain the mifepristone liposome solution. Add 10ml of 0.02mol / L pH 7.2 phosphate buffer solution for dilution, add 2.0 g of sucrose as a proppant, filter and sterilize with a 0.22 μm microporous membrane, and pack to obtain the finished produ...

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Abstract

The invention discloses a mifepristone lipidosome preparation and a preparation method thereof. The lipidosome is prepared from the following raw materials: mifepristone, a phospholipid membrane material, cholesterol, a membrane stabilizing material, a buffer salt and a freeze-drying protective additive. The concrete preparation method comprises the following steps: dissolving the phospholipid membrane material, the cholesterol, the membrane stabilizing material and the mifepristone into an organic solvent; removing an organic solvent in vacuum; adding a buffer solution to swell the film after the film is formed, so as to form a suspension; dispersing by ultrasonic or homogeneous equipment, so as to obtain mifepristone lipidosome; adding the freeze-drying protective additive, and further freezing and drying to prepare lyophilized powder. The lipidosome prepared by the method is uniform in particle size distribution, high in encapsulation efficiency, high in drug loading capacity, and good in repeatability. The problem of poor water solubility of the mifepristone is solved, meanwhile, the lipidosome can be used for injection, and the administration mode of the lipidosome is expanded.

Description

Technical field [0001] The present invention is a drug preparation field, which involves a meterone lipid system and its preparation methods. Background technique [0002] Mifepristone (RU486), its chemical name is: 11β- [4- (n, n-dihylaminel) benzyl] -17β-hydroxyl -17α- (1-propyl) -Soya-4,9-dizide -3-ketone 1.3, molecular formula is C 29 H 35 NO 2 , The molecular weight is 429.61, the structure is as follows: [0003] [0004] Mi butterol is a progesterone receptor antagonist that has the effects of terminating early pregnancy, anti -bed, induced menstruation, and promoting cervical maturity.It has been widely used in the clinic to resist early pregnancy and menstruation and stop pregnancy, which has good results.In addition, according to the latest clinical and clinical research results, Mepatone can be used as a antitumor drug for breast cancer, prostate cancer, ovarian cancer, gastric cancer, endometrial cancer, and central nervous system tumors including benign tumors(CHEN...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/567A61K47/34A61P35/00
Inventor 高瑜吴福强顾颂恩李志洪解晓东陈海军贾力
Owner FUZHOU UNIV
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