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Stable azacitidine freeze-drying preparation and preparing method thereof

An azacitidine and freeze-drying technology, which is applied in freeze-dried delivery, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. Glycoside hydrolysis and other problems, to achieve the effect of accelerating the dissolution rate, reducing the crystal size and reducing the degradation

Active Publication Date: 2019-04-19
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the main impurity of azacitidine for injection is the hydrolysis impurity. As a reducing agent, vitamin C cannot inhibit the hydrolysis of azacitidine, and it is difficult to solve the stability of this product.

Method used

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  • Stable azacitidine freeze-drying preparation and preparing method thereof
  • Stable azacitidine freeze-drying preparation and preparing method thereof
  • Stable azacitidine freeze-drying preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Add to 2400ml (80%)

[0032] Preparation:

[0033] Measure 80% of water for injection, add the prescribed amount of mannitol into the water for injection, stir and dissolve, and cool down to 0-4°C, add the prescribed amount of azacitidine into tert-butanol and stir to disperse; add the mannitol aqueous solution Mix with azacitidine tert-butanol dispersion, and add the remaining amount of water for injection to obtain an intermediate liquid, keep the intermediate liquid at 0-4°C; filter the intermediate liquid through nitrogen pressure to 0.2 μm Filter the membrane, and sub-pack 24ml into injection bottles, freeze-dry, stopper, crimp the cap, pack, and obtain the azacitidine freeze-dried preparation. The freeze-drying process is as follows: Pre-freezing: keep at -45°C for 1.5h, -10°C for 1h, and -45°C for 2h; primary drying: keep at -10°C for 20h; secondary drying: keep at 40°C for 10h.

Embodiment 2

Add to 2400ml (80%)

[0036] Preparation:

[0037] Measure 80% of water for injection, add the prescribed amount of mannitol into the water for injection, stir and dissolve, and cool down to 0-4°C, add the prescribed amount of azacitidine into propylene glycol and stir to disperse; Zacytidine propylene glycol dispersions were mixed, and the remaining amount of water for injection was added to obtain an intermediate medicinal solution, which was kept at 0-4°C; the intermediate medicinal solution was filtered through a 0.2 μm filter membrane under nitrogen pressure, and Pack 24ml into injection vials, freeze-dry, cork, cap, and pack to obtain the azacitidine freeze-dried preparation. The freeze-drying process is the same as in Example 1.

Embodiment 3

Add to 2400ml (80%)

[0040] Preparation:

[0041] Measure 80% of water for injection, add the prescribed amount of mannitol into the water for injection, stir and dissolve, and cool down to 0-4°C, add the prescribed amount of azacitidine into isopropanol and stir to disperse; add the mannitol aqueous solution Mix with azacitidine isopropanol dispersion, and add the remaining amount of water for injection to obtain the intermediate drug solution, keep the intermediate drug solution at 0-4°C; filter the intermediate drug solution through nitrogen pressure to 0.2 μm Filter the membrane, and sub-pack 24ml into injection bottles, freeze-dry, stopper, crimp the cap, pack, and obtain the azacitidine freeze-dried preparation. The freeze-drying process is the same as in Example 1.

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Abstract

The invention discloses a stable azacitidine freeze-drying preparation and a preparing method thereof, belongs to the technical field of pharmaceutical preparations, and particularly provides a stableazacitidine freeze-drying preparation for injection and a preparing method thereof. The freeze-drying preparation comprises azacitidine and mannitol; medicine liquid before free-drying also containsan organic solvent and water for injection. The organic solvent is selected from a mixed solution of teritary butanol, isopropanol and propanediol. By means of the freeze-drying preparation, the dissolution speed of azacitidine is greatly increased, the stability of azacitidine is greatly improved, and the redissolving time of the freeze-drying preparation is shortened.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a stable freeze-dried preparation of azacitidine for injection and a preparation method thereof. Background technique [0002] Azacitidine (Azacitidine) is a DNA methyltransferase inhibitor, which can cause DNA hypomethylation and has direct cytotoxicity, developed by Pharmion Pharmaceutical Company of the United States. In May 2004, the U.S. FDA approved the listing of the lyophilized preparation Vidaza for the treatment of myelodysplastic syndromes (myelodysplastic syndromes, MDS) and acute myeloid leukemia (AML). [0003] The structural formula of azacitidine is as follows: [0004] [0005] There are two main difficulties in the development of azacitidine freeze-dried preparations. First, azacitidine is slightly soluble in water, easily aggregates in water, has poor solubility, and takes a long time to prepare. Second, azacitidine is easi...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/26A61K31/706A61P7/00A61P35/02
CPCA61K9/0019A61K9/19A61K31/706A61K47/26A61P7/00A61P35/02
Inventor 郭彦亮申升秦梦余俊杜祖银
Owner JIANGSU HANSOH PHARMA CO LTD
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