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Injectable clofarabine composition

A technology of clofarabine and composition, which is applied in the field of pharmaceutical preparations, can solve problems such as difficulties, increased costs, and low solubility of clofarabine, and achieve the effect of good clarity

Inactive Publication Date: 2006-07-19
吴葆金
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low solubility of clofarabine, it is difficult to prepare it into a high-concentration injection preparation, which also increases the cost for industrial production.

Method used

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  • Injectable clofarabine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Clofarabine Sodium Chloride Injection [100ml contains clofarabine 20mg, that is, the concentration is 0.02% (g / ml)]

[0024] prescription:

[0025] Clofarabine 0.2g

[0026] Lactic acid 0.4ml

[0027] Sodium chloride 9.0g

[0028] Water for injection up to 1000ml

[0029] Preparation process: Add 0.4ml of medicinal lactic acid to 100ml of water for injection, mix well, add clofarabine under stirring to dissolve; decolorize with activated carbon, filter to remove carbon; dilute to 850ml with water for injection.

[0030] Add sodium chloride to 100ml water for injection, heat to dissolve; decolorize with activated carbon, filter to remove carbon.

[0031] Slowly add the sodium chloride solution to the clofarabine dilution under stirring, adjust the pH value to 4 with 1→10 lactic acid, and add water for injection to the required amount. Filter with a 0.45μm filter membrane, fill in 100ml per bottle into an infusion bottle, and sterilize...

Embodiment 2

[0033] Clofarabine injection [2ml contains clofarabine 20mg, that is, the concentration is 1% (g / ml)]

[0034] prescription:

[0035] Clofarabine 10g

[0036] Citric acid 7g

[0037] Water for injection up to 1000ml

[0038] Preparation process: Add citric acid to 950ml of water for injection, stir to dissolve; add clofarabine, heat to 40°C, stir to dissolve, add water for injection to 1000ml (at this time, the pH of the solution is about 4.0). Filter and fill in 2ml ampoules. Melt and sterilize.

[0039] When the injection is used clinically, it needs to be diluted with 5% glucose injection or 0.9% sodium chloride injection and injected intravenously.

Embodiment 3

[0041] Clofarabine for injection (each bottle contains clofarabine 20mg)

[0042] prescription:

[0043] Clofarabine 20g

[0044] Lactic acid 8.0ml

[0045] Mannitol 80g

[0046] Water for injection up to 2000ml

[0047] Prepare 1000 bottles

[0048] Preparation process: Add 8.0ml of medicinal lactic acid to 1900ml of water for injection, mix well, add clofarabine, heat to 45°C, stir to dissolve, then add mannitol, stir to dissolve; add water for injection to 2000ml, adjust pH with lactic acid The value is at 4.5. Sterilize and filter, the filtrate is quantitatively filled in 7ml vials at a rate of 2ml / bottle, and is prepared into a freeze-dried powder through a freeze-drying process.

[0049] Reconstitution test At room temperature, add 1ml of water for injection, or 1ml of 0.9% sodium chloride injection, or 1ml of 5% glucose injection to 1 bottle of lyophilized powder, shake slightly, and dissolve into a clear solution in about 5...

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Abstract

The invention belongs to the field of pharmaceutical preparation, more specifically, the invention relates to a clofarabine composition for injection, which contains clofarabine and pharmaceutically acceptable acids. The composition has good water-solubility, and can be prepared into liquid preparation or freeze-dried preparation.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an injectable clofarabine composition. Background technique [0002] Clofarabine English name: Clofarabine; chemical name: 2-chloro-2'-fluoro-deoxy-9-β-D-arabinofuranosine. [0003] Its structural formula: [0004] [0005] Clofarabine was developed by HOFFMANN LA ROCHE in 1988 and filed a compound patent application in Europe with the publication number EP314011, which was later transferred to Genayme and Bioenvision of the United States. And in December 2004, it was approved to go on the market by the FDA of the United States, and the trade name was Clolar. [0006] Clofarabine is a new generation of purine nucleotide analogues, and it is the first drug approved by FDA so far for the treatment of childhood leukemia. [0007] Because the solubility of clofarabine in water is very small, only 0.02% (g / ml). Its concentration of clofarabine injection listed in the ...

Claims

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Application Information

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IPC IPC(8): A61K31/7076A61K9/08A61K9/19
Inventor 吴葆金
Owner 吴葆金
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