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Mifepristone medicinal preparation and preparation method thereof

A technology for mifepristone and pharmaceutical preparations, applied in the directions of pharmaceutical formulations, pharmaceutical combinations, medical preparations containing active ingredients, etc., can solve the problems of low dissolution rate, instability, influence on curative effect or curative effect, etc., and achieves improved dissolution rate , low manufacturing cost, and the effect of improving bioavailability

Inactive Publication Date: 2009-06-17
HUBEI GEDIAN HUMANWELL PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Purpose of the present invention is exactly for the existing mifepristone pharmaceutical preparation in water dissolution rate is very low, can affect the defective of curative effect or unstable curative effect after taking, provide a kind of mifepristone pharmaceutical preparation and preparation method, it can improve The dissolution rate and bioavailability of the drug formulation, thereby improving the efficacy of the drug

Method used

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  • Mifepristone medicinal preparation and preparation method thereof
  • Mifepristone medicinal preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] 10g of mifepristone raw material is heated to about 70°C and dissolved in 50ml of ethanol solution, 50ml of water is added dropwise to the solution, the temperature is lowered, and after being kept at room temperature for 3 hours, the temperature is then lowered to below 0°C, and crystals are precipitated in the solution. Filter, wash the filtrate with cold ethanol / water, and dry under vacuum at 50°C. Obtain mifepristone: 6g. HPLC purity: 99.54%, melting point: 135-140°C. Mifepristone is pulverized and micronized to obtain mifepristone micronized particle size distribution measurement results

[0025] Numbering Particle sizeum accumulation% Interval % Numbering Particle sizeum accumulation% Interval % 1 0.39 0 0 11 2.15 44.53 13.41 2 0.46 0 0 12 2.55 59.84 1631 3 0.55 0.50 0.50 13 3.02 74.05 14.21 4 0.65 1.58 1.08 14 3.58 85.65 11.60 5 0.77 3.05 1.47 15 4.24 93.79 8.14 6 0.92 5.53 2.4...

Embodiment 2

[0028] Heat 10g of mifepristone raw material to about 70°C and dissolve in 50ml of n-butanol solution, add 50ml of water dropwise to the solution, cool down, keep at room temperature for 3 hours, then cool down to below 0°C, and precipitate out of the solution Crystals, filtered, the filtrate was washed with cold water, and dried under vacuum at 50°C. Obtain mifepristone: 6g. HPLC purity: 99.60%, melting point: 135-140°C. Mifepristone is pulverized and micronized to obtain mifepristone granules.

Embodiment 3

[0030] Heat 10g of mifepristone raw material to about 70°C and dissolve in 50ml of isopropanol solution, add 50ml of water dropwise to the solution, cool down, keep at room temperature for 3 hours, then cool down to below 0°C, and precipitate out of the solution Crystals, filtered, the filtrate was washed with cold water, and dried under vacuum at 50°C. Obtain mifepristone: 6g. HPLC purity: 99.52%, melting point: 135-140°C. Mifepristone is pulverized and micronized to obtain mifepristone granules.

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Abstract

The invention relates to a pharmaceutical preparation of mifepristone and preparation method thereof. The pharmaceutical preparation of mifepristone is prepared by the step of mixing the raw materials as follows according to mass ratio: 5-30 % of mifepristone particles, 10-40% of microcrystalline cellulose, 2-10% of adhesive, 20-40% of starch, 20-40% of dextrin, 05.-2% of lubricant, and 0.5-1% of glidant. The invention can improve dissolution and bioavailability of the mifepristone preparation having obviously increased action against early pregnancy of animals, comparatively simple preparation method, and low manufacturing cost.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a mifepristone pharmaceutical preparation and a preparation method thereof. Background technique [0002] Mifepristone, an antiprogestin drug, its chemical name is 11β-[4-(N,N-dimethylamino)phenyl-17β-hydroxy-17-α-(1-propynyl)-estr ster-4,9-dien-3-one]. It was first synthesized by Rousel-Ucalf Company in France in 1980, and it has been widely used clinically at home and abroad. Mifepristone 150 mg combined with prostaglandins can effectively terminate early pregnancy within 49 days, and its effective rate of anti-early pregnancy is 92-94%. The effective rate of emergency contraception within 72 hours of mifepristone 10-25mg is over 90%. [0003] Mifepristone is insoluble in water, but soluble in 0.1m / L hydrochloric acid solution, so the dissolution rate in water is very low, and the curative effect will be affected or unstable after taking. Ther...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/567A61P15/04
Inventor 杨艳青刘俊勇陈芳乔伟俊张丽
Owner HUBEI GEDIAN HUMANWELL PHARMACEUTICAL CO LTD
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