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A kind of azacitidine freeze-dried powder for injection

A technology of azacitidine and freeze-dried powder, applied in the field of pharmaceutical preparations, can solve the problems of not meeting the particle size requirements of the original research injection, unable to disperse quickly and uniformly, and uneven particle size distribution, and achieve good appearance, shorten the freeze-drying cycle, and settle slow effect

Active Publication Date: 2020-12-04
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Patent CN104739778A also discloses azacitidine freeze-dried powder for injection and its preparation method, which mainly improves the stability of azacitidine aqueous solution by adding phosphate buffer salt, and phosphate buffer salt can improve the stability of the drug. It is helpful to some extent, but it does not control the preparation temperature of the drug during the preparation process. Azacitidine aqueous solution is the most stable at 0-10°C, and the related substances increase significantly when it is higher than 10°C
And the sample prepared by this patented method has agglomeration phenomenon after settling, and cannot be dispersed quickly and evenly after shaking lightly
[0010] Patent CN105769775A also discloses azacitidine freeze-dried powder for injection and its preparation method, which mainly controls the hydrolysis of the drug by controlling the dispensing temperature and filling nitrogen to improve the stability of the product. Nitrogen filling has a certain effect on improving the stability of azacitidine aqueous solution, but the samples prepared by this patented method have large particles and uneven particle size distribution, which does not meet the particle size requirements of the original injection

Method used

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  • A kind of azacitidine freeze-dried powder for injection
  • A kind of azacitidine freeze-dried powder for injection
  • A kind of azacitidine freeze-dried powder for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] (1) Prescription

[0035]

[0036] (2) Preparation of azacitidine freeze-dried powder for injection:

[0037] 1. Preparation of Azacitidine aqueous solution:

[0038] The mannitol and sodium acetate of prescription quantity are taken by weighing in the water for injection of 80% prescription quantity, stir to make it dissolve. Add activated carbon to the above solution, stir for 30 minutes, and cool the filtrate to 0-10°C after decarbonization. Weigh the prescribed amount of azacitidine raw material and pass it through a 24-mesh sieve, slowly add it to the above solution, stir and dissolve for 8 minutes, add water for injection at 0-10°C to make up the full amount. The above solution was sterilized and filtered through a 0.22 μm filter, and after filtration, it was divided into vials, half-tightened, and placed in a freeze dryer to freeze-dry.

[0039] 2. The freeze-drying procedure of azacitidine freeze-dried powder for injection is as follows:

[0040] (a) Repe...

Embodiment 2

[0044] (1) Prescription

[0045]

[0046] (2) Preparation of azacitidine freeze-dried powder for injection:

[0047] 1. Preparation of Azacitidine aqueous solution:

[0048] Same as Example 1; during the preparation process, the raw materials were processed through a 50-mesh sieve, and the dissolution time of the raw materials was 5 minutes.

[0049] 2. The freeze-drying procedure of azacitidine freeze-dried powder for injection is as follows:

[0050] (a) Repeated pre-freezing: first cool the sample solution to be lyophilized to -48°C at full speed and maintain it for 30 minutes, then raise the temperature to -7°C at 10°C / h, maintain it for 30 minutes, then cool it down to -48°C at full speed and maintain it for 30 minutes , then raised the temperature to -7°C at 10°C / h, maintained for 30 minutes, then cooled to -48°C at full speed and maintained for 240 minutes.

[0051] (b) Sublimation drying: vacuumize the freeze dryer and maintain 0.15±0.02mbar, raise the temperatur...

Embodiment 3

[0054] (1) Prescription

[0055]

[0056] (2) Preparation of azacitidine freeze-dried powder for injection:

[0057] 1. Preparation of Azacitidine aqueous solution:

[0058] Same as Example 1; during the preparation process, the raw materials were processed through a 65-mesh sieve, and the dissolution time of the raw materials was 5 minutes.

[0059] 2. The freeze-drying procedure of azacitidine freeze-dried powder for injection is as follows:

[0060] (a) Repeated pre-freezing: first cool the sample solution to be lyophilized to -45°C at full speed and maintain it for 30 minutes, then raise the temperature to -10°C at 10°C / h, maintain it for 30 minutes, then cool it down to -45°C at full speed and maintain it for 30 minutes , then raised the temperature to -10°C at 10°C / h, maintained for 30min, then cooled down to -45°C at full speed and maintained for 240min.

[0061] (b) Sublimation drying: Vacuumize the freeze dryer and maintain 0.15±0.02mbar, raise the temperature o...

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Abstract

The invention discloses freeze-dried azacitidine powder for injection. The freeze-dried azacitidine powder comprises azacitidine, mannitol and sodium acetate. Meanwhile, the invention discloses a preparation method of freeze-dried azacitidine powder injection for injection and aims to solve the problems of instability of azacitidine aqueous solution, non-uniform particle distribution, substandardsuspending uniformity, small settling volume and the like through adding sodium acetate, sieving bulk drug, controlling preparation temperature, optimizing freeze-drying curve and the like. A productproduced according to the technical scheme provided by the invention is stable in quality, good in redissolving performance, and uniform in particle distribution; the particle size of prepared suspension satisfies the requirements of clinical medication, the settling speed is low, caking does not exist after settling, and particles can disperse uniformly after being shaken gently.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to azacitidine freeze-dried powder for injection. Background technique [0002] Azacitidine was first synthesized by Czechoslovakian scientists Piskala and Sorm, and was later isolated from the fermentation broth of Streptoverticillium ladakanus. The chemical name is 1-(β-D-furanucleoyl)-4-amino-1,3,5-triazin-2(1H)-one, also known as 5-azacytidine, azacytidine, commodity The name Vidaza (Vidaza) is a white needle-like crystal; it is a DNA methyltransferase inhibitor developed by Pharmion Company of the United States, and it was first listed in the United States in July 2004; it is a cell cycle-specific drug that acts on the S phase. It can quickly phosphorylate and penetrate into RNA (ribonucleic acid) and DNA (deoxyribonucleic acid) by destroying the smooth translation of nucleic acid into protein, inhibiting protein synthesis, and can also affect p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/26A61K47/12A61K31/706A61P7/06A61P35/02
CPCA61K9/0019A61K9/19A61K31/706A61K47/12A61K47/26
Inventor 张贵民李娜秦士慧
Owner LUNAN PHARMA GROUP CORPORATION
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