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Azacitidine for injection and preparation method thereof

A technology for azacitidine and injection, which is applied in the field of medicine and can solve the problems of clinical drug safety and effectiveness, poor product stability, and difficult control

Inactive Publication Date: 2013-08-21
FUKANGREN BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the active ingredient of the drug, azacitidine, is rapidly hydrolyzed in water, it is difficult to control the related substances of the freeze-dried preparation, and the stability of the product is poor during storage, which has a potential impact on the safety and effectiveness of clinical medication

Method used

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  • Azacitidine for injection and preparation method thereof
  • Azacitidine for injection and preparation method thereof
  • Azacitidine for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] 1.1 Prescription

[0040]

[0041]

[0042] 1.2 Freeze-drying procedure

[0043]

[0044] 1.3 Preparation method

[0045] (1) Measure 80% water for injection, add mannitol, and stir until completely dissolved;

[0046] (2) Add activated carbon, keep warm in 80°C water bath for 20 minutes, and filter to remove carbon;

[0047] (3) Make up the whole amount with water for injection, cool down to -1~-3°C, and adjust the pH to 6;

[0048] (4) Add azacitidine, stir until completely dissolved, and strictly control the temperature at -1~-3°C;

[0049] ⑸Filling, 25ml / bottle;

[0050] ⑹ Turn on the freeze dryer, and after pre-freezing at -50°C for 3 hours, turn on the vacuum pump and run the program;

[0051] ⑺Vacuum plugging, capping and packaging.

[0052] 1.4 Full inspection results

[0053] 1.4.1 Moisture: 1.25%±0.27 (n=6)

[0054] 1.4.2 Content: 100.12%±0.35(n=3)

[0055] 1.4.3 Related substances:

[0056]

Embodiment 2

[0058] 2.1 Prescription

[0059]

[0060] 2.2 Freeze-drying procedure

[0061]

[0062] 2.3 Preparation method

[0063] (1) Measure 80% water for injection, add mannitol, and stir until completely dissolved;

[0064] (2) Add activated carbon, keep warm in 80°C water bath for 20 minutes, and filter to remove carbon;

[0065] (3) Make up the full amount with water for injection, cool down to -1~-3°C, and adjust the pH to 6.5;

[0066] (4) Add azacitidine, stir until completely dissolved, and strictly control the temperature at -1~-3°C;

[0067] ⑸Filling, 25ml / bottle;

[0068] ⑹ Turn on the freeze dryer, and after pre-freezing at -50°C for 3 hours, turn on the vacuum pump and run the program;

[0069] ⑺Vacuum plugging, capping and packaging.

[0070] 2.4 Full inspection results

[0071] 2.4.1 Moisture: 0.24%±0.13(n=6)

[0072] 2.4.2 Content: 99.24%±0.27(n=3)

[0073] 2.4.3 Related substances:

[0074]

Embodiment 3

[0076] 3.1 Prescription

[0077]

[0078] 3.2 Freeze-drying procedure

[0079]

[0080]

[0081] 3.3 Preparation method

[0082] 1. Measure 80% water for injection, add mannitol, stir until completely dissolved;

[0083] 2. Add 0.1% activated carbon, stir in an 80-degree water bath for 20 minutes, and filter to remove carbon;

[0084] 3. Make up the full amount with water for injection, cool down to -1~-3°C, and adjust the pH to 7;

[0085] 4. Add azacitidine, stir until completely dissolved, and strictly control the temperature at -1~-3°C;

[0086] 5. Dispensing, 25ml / bottle;

[0087] 6. Turn on the freeze dryer, and after pre-freezing at -50°C for 3 hours, turn on the vacuum pump and run the program;

[0088] 7. Vacuum plugging, capping and packaging.

[0089] 3.4 Full inspection results

[0090] 3.4.1 Moisture: 2.29%±0.26(n=6)

[0091] 3.4.2 Content: 99.75%±0.56(n=3)

[0092] 3.4.3 Related substances:

[0093]

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Abstract

Azacitidine for injection and a preparation method thereof are disclosed. Main components of the azacitidine for injection contain main drugs of azacitidine and mannitol. Mainly by controlling pH value of an azacitidine aqueous solution, hydrolysis of azacitidine is effectively inhibited, related substances of freeze-dried product are minimized, and product quality of the azacitidine freeze-drying preparation is raised.

Description

technical field [0001] The invention relates to azacitidine for injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Azacitidine (Azacitidine) is a DNA methyltransferase inhibitor, which can cause DNA hypomethylation and has direct cytotoxicity. It was developed by Pharmion Pharmaceutical Company of the United States. In May 2004, the FDA approved the drug Vidaza for the treatment of all subtypes of myelodysplastic syndrome. Because the active ingredient of the drug, azacitidine, is rapidly hydrolyzed in water, it is difficult to control the related substances of the freeze-dried preparation, and the product has poor stability during storage, which has a potential impact on the safety and effectiveness of clinical medication. [0003] The structural formula of 5-azacytosine nucleoside is as follows: [0004] [0005] Azacitidine (compound 1) is a cytidine nucleoside analogue, which is easily hydrolyzed i...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/706A61K47/10A61P7/00
Inventor 王晓梅王晓丹
Owner FUKANGREN BIO PHARMA
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