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Decitabine liquid composition and preparation method of its lyophilized preparation

The technology of a liquid composition and decitabine, which is applied in the field of medicine, can solve problems such as high requirements for instruments and operating environment, difficult operation, and large amount of solvent, and achieve simplified production equipment process and cost, improved solubility, and related substances The effect of low content

Inactive Publication Date: 2012-08-01
NANJING CHANGAO PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Invention patent CN200910033897.7 (CN 101584670A) uses 5-80% tert-butanol as a freeze-drying solvent, the amount of solvent is large, and there are many residues
[0007] After reviewing many domestic preparation patents and many documents, there are corresponding special requirements in production, which bring certain difficulties to industrial production. For example, CN200910033897.7 requires low-temperature preparation of solutions, filling of sterile powder for injection, etc. on instruments and operations. The environmental requirements are high, and it is difficult to dilute the sample before use

Method used

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  • Decitabine liquid composition and preparation method of its lyophilized preparation
  • Decitabine liquid composition and preparation method of its lyophilized preparation
  • Decitabine liquid composition and preparation method of its lyophilized preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] prescription

[0028] Decitabine 50g

[0029] Potassium dihydrogen phosphate 68g

[0030] Sodium hydroxide 11.6g

[0031] Ethanol 250ml

[0032] Water for injection 9.75L

[0033]

[0034] A total of 1000 bottles were made

[0035] Preparation Process:

[0036] 1. Dissolve potassium dihydrogen phosphate and sodium hydroxide in water for injection.

[0037] 2. Uniformly disperse decitabine in the prescribed amount of organic solvent ethanol.

[0038] 3. Mix and stir the two phases at room temperature to dissolve, add activated carbon, filter, fill, and freeze-dry.

[0039] 4. Start the freeze dryer, after pre-freezing at -45°C for 5 hours, turn on the vacuum pump, raise the temperature to -20°C, and keep it for 7 hours; the second step is to raise the temperature to 0°C, keep it for 9 hours; then raise the temperature to 40°C and dry for 6 hours.

[0040] 5. Vacuum stopper, aluminum cover.

[0041] 6. After passing the ...

Embodiment 2

[0043] prescription

[0044] Decitabine 50g

[0045] Potassium dihydrogen phosphate 68g

[0046] Sodium hydroxide 11.6g

[0047] Ethanol 200ml

[0048] Mannitol 200g

[0049] Sodium bisulfite 20g

[0050] Water for injection 9.8L

[0051]

[0052] A total of 1000 bottles were made

[0053] Preparation Process:

[0054] 1. Dissolve potassium dihydrogen phosphate, sodium hydroxide, mannitol, and sodium bisulfite in water for injection.

[0055] 2. Uniformly disperse decitabine in the prescribed amount of organic solvent ethanol.

[0056] 3. Mix and stir the two phases at room temperature to dissolve, add activated carbon, filter, fill, and freeze-dry.

[0057] 4. Start the freeze dryer, after pre-freezing at -45°C for 5 hours, turn on the vacuum pump, raise the temperature to -20°C, and keep it for 7 hours; the second step is to raise the temperature to 0°C, keep it for 9 hours; then raise the temperature to 40°C and dry...

Embodiment 3

[0061] prescription

[0062] Decitabine 50g

[0063] Potassium dihydrogen phosphate 68g

[0064] Sodium hydroxide 11.6g

[0065] Ethanol 250ml

[0066] Glycine 125g

[0067] EDTA-2Na 5g

[0068] Water for injection 9.75L

[0069]

[0070] A total of 1000 bottles were made

[0071] Preparation Process:

[0072] 1. Dissolve potassium dihydrogen phosphate, sodium hydroxide, glycine, EDTA-2Na in water for injection.

[0073] 2. Uniformly disperse decitabine in the prescribed amount of organic solvent ethanol.

[0074] 3. Mix and stir the two phases at room temperature to dissolve, add activated carbon, filter, fill, and freeze-dry.

[0075] 4. Start the freeze dryer, after pre-freezing at -45°C for 5 hours, turn on the vacuum pump, raise the temperature to -20°C, and keep it for 7 hours; the second step is to raise the temperature to 0°C, keep it for 9 hours; then raise the temperature to 40°C and dry for 6 hours.

[007...

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PUM

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Abstract

The invention which belongs to the medicinal preparation field relates to a decitabine liquid composition and a preparation method of its lyophilized preparation. The liquid composition contains decitabine, potassium dihydrogen phosphate, sodium hydroxide, ethanol and injection water, wherein the application amount of ethanol accounts for 1.0-4.0% of the volume of the liquid composition. The liquid composition is lyophilized to obtain the lyophilized preparation of decitabine. The stability and the like of the lyophilized preparation of decitabine provided in the invention reach high level, and the process is simultaneously simplified.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a preparation method of a novel decitabine liquid composition and a freeze-dried preparation thereof. Background technique [0002] Decitabine is 5-aza-2′-deoxycytidylic acid, a natural 2′-deoxycytidylic acid adenosine analog, by inhibiting DNA methyltransferase, reducing DNA methylation, thereby Inhibit tumor cell proliferation and prevent drug resistance. It cannot inhibit DNA synthesis in vitro, but can induce hypomethylation in tumor cells, and has related cell differentiation and proliferation control functions to maintain genes. Non-proliferating cells are relatively insensitive to decitabine. Decitabine is a chemotherapeutic drug, and clinical reports show that it has broad-spectrum antitumor activity against hematologic malignancies and solid tumors. [0003] The molecular structural formula of 5-aza-2'-deoxycytidine is shown in the following formula: [0004] [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/706A61K47/10A61P35/00A61P35/02
Inventor 宋巧莉吴小涛何红燕储刚范婧钟雪斌霍立茹刘彩连
Owner NANJING CHANGAO PHARMA SCI & TECH CO LTD
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