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Decitabine lyophilized preparation and preparation method thereof

A technology of freeze-dried preparations and decitabine, which is applied in the field of decitabine freeze-dried preparations and its preparation, can solve the problems of low solubility, instability and easy degradation of decitabine, and achieve good product quality and high product quality. The effect of high quality and high safety

Active Publication Date: 2013-08-21
CHONGQING LUMMY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor intends to use this discovery to prepare decitabine freeze-dried preparations under extremely low temperature conditions. This method not only solves the problem of low solubility of decitabine in the preparation process, but also overcomes the instability and easy degradation of decitabine. The shortcoming of decitabine obtains the decitabine freeze-dried preparation that meets pharmaceutical requirements

Method used

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  • Decitabine lyophilized preparation and preparation method thereof
  • Decitabine lyophilized preparation and preparation method thereof
  • Decitabine lyophilized preparation and preparation method thereof

Examples

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preparation example Construction

[0029] The preparation method of decitabine freeze-dried preparation of the present invention comprises the following steps:

[0030] (1) Dissolving decitabine in a mixed solvent composed of dimethyl sulfoxide and a water-miscible organic solvent, and freezing to below -30°C; the organic solvent is selected from methanol, ethanol, isopropyl Alcohol, n-butanol, tert-butanol;

[0031] (2) Dilute the solution obtained in step (1) with water for injection in which the pH regulator has been dissolved to prepare a mixed solution, filter, and sub-package. The temperature during this operation needs to be controlled at -20 ~ -30°C, so as to facilitate the control of the mixed solution at - 20~-30℃;

[0032] (3) Freeze-drying is made into freeze-dried preparation;

[0033] Wherein, in the mixed solution described in step (2): dimethyl sulfoxide accounts for 5% to 20% of the total volume of the mixed solution, and the "water-miscible organic solvent" accounts for 10 to 35% of the tota...

Embodiment 1

[0062] prescription

[0063]

[0064] Precisely weigh decitabine, dissolve it with dimethyl sulfoxide, mix it with ethanol, and freeze it to about -30°C; prepare a water solution for injection containing potassium dihydrogen phosphate and sodium hydroxide in the prescribed amount, and refrigerate it until 2- After 5°C, mix with the above-mentioned organic solvent in which decitabine is dissolved, stir to dissolve, keep warm at -30~-25°C, filter through a 0.22 micron filter membrane, pack in vials, freeze-dry, and wait for After the solvent of the finished product is completely removed, the stopper is pressed, and the cover is tied, and the product is obtained. After inspection, the RS10 content of the finished product is 0.02%, the total impurities of the finished product are 0.48%, and the content of dimethyl sulfoxide is 0.01%.

Embodiment 2

[0066] prescription

[0067]

[0068] Precisely weigh decitabine, add dimethyl sulfoxide and ethanol to dissolve, and freeze the solvent at -30°C; prepare a water-for-injection solvent containing prescription potassium dihydrogen phosphate and sodium hydroxide, and refrigerate to 2-5°C , mix the prepared two solvents, stir to dissolve, keep warm at -25°C to -20°C, after passing the intermediate inspection, filter through a 0.22 micron filter membrane, pack in cillin varieties, freeze-dry, and wait for the finished product After the solvent is completely removed, the plug is pressed, and the cover is tied, and the product is obtained. After inspection, the RS10 content of the finished product is 0.02%, the total impurities of the finished product are 0.50%, and the content of dimethyl sulfoxide is 0.01%.

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Abstract

The invention belongs to the field of pharmacy and specifically relates to a decitabine lyophilized preparation and a preparation method thereof, so as to realize control on increase of decitabine related substances as well as rapid dissolution of decitabine under extreme low temperature. The preparation method comprises the steps of: (1) dissolving decitabine into a mixed solvent containing dimethyl sulfoxide and an organic solvent miscible with water, and refrigerating the mixed solution to lower than -30 DEG C; (2) diluting the mixed solution obtained in the step (1) by injection water dissolved with pH conditioning agent, filtering and carrying out split charging, wherein a temperature during the operation process is -20- -30 DEG C; (3) lyophilizing the mixed solution to obtain the lyophilized preparation. The mixed solution mentioned in the step (2) comprises dimethyl sulfoxide accounting for 5-20% of a bulk volume of the mixed solution, 10-35% of organic solvent miscible with water and 50-85% of injection water. The obtained lyophilized preparation contains dimethyl sulfoxide residue less than 0.05% and impurity RS10 no more than 0.03%.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a decitabine freeze-dried preparation and a preparation method thereof. Background technique [0002] Decitabine, decitabine is a DNA methyltransferase inhibitor, has the clinical effect of treating myelodysplastic syndrome, and is a cytosine anticancer drug. Its chemical name is 4-amino-1-(2-deoxy-β-D-erythro-ribofuranose)-1,3,5-triazin-2(1H)-one, decitabine is the common name, At present, there is no domestic market, and the product listed in the United States is named DACOGEN). [0003] Decitabine is extremely unstable in aqueous solution, and the aqueous solution environment will cause the 5-azacytosine ring to be broken and degraded into α-type inactive isomers and ring-opening formylated derivatives. When the inventors of the present invention were studying the stability of decitabine, they found a group of ring-opening formylated derivatives after hydrolysis of decita...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/706A61P35/00
Inventor 许辉川
Owner CHONGQING LUMMY PHARMA
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