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Pharmaceutical composition of fludarabine phosphate and preparation method thereof

A technology of fludarabine phosphate and its composition, which is applied in the pharmaceutical composition of fludarabine phosphate and its preparation field, and can solve the problems of high impurity content and potential safety hazards of fludarabine phosphate, so as to ensure drug safety Sex, reduce dosage, improve curative effect

Active Publication Date: 2014-05-14
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the content of impurities in the fludarabine phosphate applied for in this patent is relatively high, and there will be certain safety hazards in clinical use

Method used

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  • Pharmaceutical composition of fludarabine phosphate and preparation method thereof
  • Pharmaceutical composition of fludarabine phosphate and preparation method thereof
  • Pharmaceutical composition of fludarabine phosphate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] (1) Prepare a mixed solvent according to the volume ratio of water: acetone and ethanol is 5:1:1, prepare a solution according to the ratio of adding 80g of fludarabine phosphate solid per liter of mixed solvent, heat to 45°C, stir until completely dissolved ;

[0035] (2) Distill under reduced pressure at 50°C. When the volume of the mixed solvent is reduced to 20%, stop the reduced-pressure distillation and cool down the mixed solvent to 1°C at a cooling rate of 2°C / min; let the crystal grow for 5 hours After obtaining the crystals, filter and dry in vacuum for 4 hours to obtain a white crystalline powder of fludarabine phosphate.

[0036] The prepared fludarabine phosphate is obtained by measuring the X-ray powder diffraction pattern of Cu-Kα ray as figure 1 Shown; detected by high performance liquid chromatography, its purity is 99.5%; melting point: 206 ~ 207 ℃.

Embodiment 2

[0038] (1) Prepare a mixed solvent according to the volume ratio of water: acetone and ethanol of 5:2:2, and prepare a solution according to the ratio of adding 100g of fludarabine phosphate solid per liter of mixed solvent, heat to 50°C, stir until completely dissolved ;

[0039] (2) Distill under reduced pressure at 50°C. When the volume of the mixed solvent is reduced to 10%, stop the reduced-pressure distillation, cool down the mixed solvent to 5°C at a cooling rate of 1.5°C / min, and let the crystal grow for 2 hours After obtaining the crystals, filter and dry in vacuum for 2 hours to obtain a white crystalline powder of fludarabine phosphate.

[0040] The prepared fludarabine phosphate is obtained by measuring the X-ray powder diffraction pattern of Cu-Kα ray as figure 1 Shown; detected by high performance liquid chromatography, its purity is 99.5%; melting point: 206 ~ 207 ℃.

Embodiment 3

[0042] (1) Prepare a mixed solvent according to the volume ratio of water: acetone and ethanol of 5:2:1, and prepare a solution according to the ratio of adding 50-120 g of fludarabine phosphate solid per liter of mixed solvent, heat to 45°C, and stir until completely Press to dissolve;

[0043] (2) Distill under reduced pressure at 45°C. When the volume of the mixed solvent decreases to 15%, stop the reduced-pressure distillation, and cool the mixed solvent to 2°C at a cooling rate of 1°C / min; stand for 4 hours to grow crystals After obtaining the crystals, filter and dry in vacuum for 3 hours to obtain a white crystalline powder of fludarabine phosphate.

[0044] The prepared fludarabine phosphate is obtained by measuring the X-ray powder diffraction pattern of Cu-Kα ray as figure 1 Shown; detected by high performance liquid chromatography, its purity is 99.5%; melting point: 206 ~ 207 ℃.

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Abstract

The invention relates to fludarabine phosphate, in particular to a pharmaceutical composition of fludarabine phosphate. The pharmaceutical composition comprises fludarabine phosphate, sodium chloride and excipient in weight ratio of 10: (1-5): (6-12) and preferably 10: (1-3): (6-10). The excipient is selected from at least one type of mannite, glucose, dextran, sorbitol and lactose, and preferably mannite or sorbitol. The pharmaceutical composition of fludarabine phosphate has low impurity content, is highly stable, and is suitable for clinical application.

Description

technical field [0001] The invention relates to fludarabine phosphate, in particular to a pharmaceutical composition of fludarabine phosphate and a preparation method thereof. Background technique [0002] Fludarabine phosphate is a fluorinated nucleotide analogue of the antiviral drug vidarabine, and its chemical name is 9-β-D-arabinic acid-furanose-2-fluoroadenine-5-phosphate. The molecular formula is C10H13FN5O7P, and the molecular weight is 365.2. Relatively resistant to deamination by adenine deaminase. [0003] Fludarabine phosphate is an antineoplastic drug used in the treatment of chronic lymphocytic leukemia. Fludarabine phosphate is rapidly dephosphorylated in vivo to 2F-ara-A, which can be taken up by cells and then phosphorylated by intracellular deoxycytidine kinase to become active triphosphate 2F-ara-A ATP. This metabolite can inhibit DNA synthesis by inhibiting the activities of ribonucleic acid reductase, DNA polymerase α, DNA primase and DNA ligase. In...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7076A61K47/04A61K9/19A61P35/00A61P35/02C07H19/20C07H1/06
Inventor 钟正明刘春燕王进宇陈颖江
Owner HAINAN JINRUI PHARMA CO LTD
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