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Decitabine freeze-dried preparation and preparation method thereof

A technology of decitabine and freeze-dried preparations, which is applied in the field of medicine, can solve problems such as increasing safety risks, and achieve the effects of ensuring product quality, good physical and chemical stability, and excellent comprehensive performance

Active Publication Date: 2012-01-18
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN101637458A discloses adding freeze-dried proppant and controlling solution pH value and temperature and then freeze-drying method to prepare decitabine freeze-dried powder injection, this method does not adopt organic solvent solubilization, because the solubility of decitabine in water is very low Small, it has been proved by experiments that this method cannot completely dissolve decitabine to obtain a 25mg / ml solution before lyophilization, and this method adds more lyophilized proppants lactose, mannitol, etc. than the imported product Dakota, which increases the Safety Risks in Clinical Use

Method used

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  • Decitabine freeze-dried preparation and preparation method thereof
  • Decitabine freeze-dried preparation and preparation method thereof
  • Decitabine freeze-dried preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Take 9.925ml of water for injection, add 68mg of potassium dihydrogen phosphate and 11.6mg of sodium hydroxide, stir to dissolve completely, cool to 0-10°C; use it as a pre-cooled aqueous solution for later use.

[0028] Take 50 mg of decitabine in a beaker, add 0.075 ml of absolute ethanol, stir to disperse evenly, transfer to a pre-cooled aqueous solution containing potassium dihydrogen phosphate and sodium hydroxide, stir to dissolve completely, and adjust the pH of the solution to 7.0. Then use 0.45 micron and 0.22 micron filter membranes to sterilize and filter, divide into glass bottles, freeze-dry to remove ethanol and water, and fill with nitrogen to protect, stopper and cover for storage. The ethanol residue of the obtained decitabine freeze-dried preparation was 0.03%, and the related substances were 0.35%.

Embodiment 2

[0030] Take 9.95ml of water for injection, add 68mg of potassium dihydrogen phosphate and 11.6mg of sodium hydroxide, stir to dissolve completely, cool to 0-10°C as a pre-cooled aqueous solution for later use.

[0031] Take 50 mg of decitabine in a beaker, add 0.05 ml of absolute ethanol, stir to disperse evenly, transfer to a pre-cooled aqueous solution containing potassium dihydrogen phosphate and sodium hydroxide, stir to dissolve completely, and adjust the pH of the solution to 6.9. Then use a 0.22-micron filter membrane to sterilize and filter, divide into glass bottles, freeze-dry to remove ethanol and water, and fill with nitrogen to protect, stopper and cover for storage. The ethanol residue of the obtained decitabine product was 0.03%, and the related substances were 0.35%.

Embodiment 3

[0033] Take 9.8ml of water for injection, add 68mg of potassium dihydrogen phosphate and 11.6mg of sodium hydroxide, stir to dissolve completely, cool to 0-10°C as a pre-cooled aqueous solution for later use.

[0034] Take 50mg of decitabine in a beaker, add 0.2ml of absolute ethanol, stir to disperse evenly, transfer to a pre-cooled aqueous solution (0-10°C) containing potassium dihydrogen phosphate and sodium hydroxide, stir to dissolve completely, adjust the solution The pH is 7.2. Then use a 0.45 micron and / or 0.22 micron filter membrane to sterilize and filter, divide into glass bottles, freeze-dry to remove ethanol and water, and store in vacuum protection with stoppers and caps. The ethanol residue of the obtained decitabine product was 0.02%, and the related substances were 0.21%.

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Abstract

The invention provides a Decitabine freeze-dried preparation and a preparation method thereof. The solution before being subject to freeze-drying process comprises Decitabine, organic solvent, pH regulator, and water for injection. The preparation method comprises the following steps: uniformly dispersing Decitabine in the organic solvent, putting the mixture in a 0-10 DEG C solution of water forinjection dissolving the pH regulator to dissolve Decitabine completely, so as to let the organic solvent account for 0.3-4.0 % of the total volume of the final mixture; then filtering, degerming, carrying out split charging in glass bottles, carrying out freeze drying to remove the organic solvent and the water for injection, so as to obtain the Decitabine freeze-dried preparation for clinical use. According to the invention, in the freeze-dried preparation, the content of the organic solvent residues is less than 0.8%, the preparation process is simple and convenient, the production steps are easy to control, the pollution to production equipment and environment caused by the organic solvent is reduced, and the product quality is guaranteed.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a decitabine freeze-dried preparation and a preparation method thereof. Background technique [0002] Decitabine (Decitabine) is an anti-tumor drug produced by Pharmachemie B.V. in the Netherlands. Its chemical name is 4-amino-1-(2-deoxy-β-D-erythro-ribofuranose)-1,3,5-tri Azin-2(1H)-one. In 2006, the US FDA approved it for the treatment of primary and secondary myelodysplastic syndromes. The trade name is Dacogen. In September 2008, it was approved to be imported and listed in China. Dako is a freeze-dried powder injection, the specification is 50 mg, and the prescription consists of decitabine, potassium dihydrogen phosphate, and sodium hydroxide. [0003] Decitabine is slightly soluble in water, the solubility in water at room temperature is about 8-12mg / ml, slightly soluble in ethanol / water (50 / 50), methanol / water (50 / 50) and methanol, and dimethyl sulfoxide (...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/706A61K47/10A61K47/20A61P35/00
Inventor 王晶翼刘宝明杨清敏郑威威张明会亓伟伟
Owner QILU PHARMA HAINAN
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