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Antitumor drug nelarabine powder-injection composition

An anti-tumor drug, the technology of nelarabine powder, which is applied in the field of medicine, can solve the problems of differences in bioavailability, etc., and achieve the effects of small differences in loading, significant drug efficacy, and high yield

Inactive Publication Date: 2017-05-31
临沂草之美医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Different crystalline forms of the same drug may have significantly different bioavailability

Method used

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  • Antitumor drug nelarabine powder-injection composition
  • Antitumor drug nelarabine powder-injection composition
  • Antitumor drug nelarabine powder-injection composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Preparation of Nelarabine Crystals

[0036] (1) Add 10g of crude nelarabine to 110ml of ethanol and acetonitrile (1:1) mixture, heat to 75°C and stir for 1 hour;

[0037] (2) When the crude nelarabine is completely dissolved, add 0.02g activated carbon, continue to heat to reflux, keep for 20 minutes, filter while hot, and concentrate the filtrate;

[0038] (3) Add 330ml isopropanol under stirring, and let it cool to room temperature;

[0039] (4) Continue to stand for 2 hours, cool to -10°C to crystallize in an ice bath, grow crystals for 8 hours, filter, wash the crystals with a small amount of absolute ethanol cooled to 0°C at least once, and dry under reduced pressure (the drying temperature is controlled at 50 The temperature is below ℃, the pressure is controlled at 10mmHg, and the drying time is 12 hours) to obtain 9.875 g of Nelarabine crystal compound with a yield of 98.75% and a purity of 99.99%.

[0040] The X-ray powder diffraction pattern of the prepared ...

Embodiment 2

[0043] Example 2: Preparation of Nelarabine Crystals

[0044] (1) Add 10g of crude nelarabine to 105ml of ethanol and acetonitrile (1:1) mixture, heat to 78°C and stir for 0.8 hours;

[0045] (2) When the crude nelarabine is completely dissolved, add 0.025g of activated carbon, continue to heat to reflux, keep for 15 minutes, filter while hot, and concentrate the filtrate;

[0046] (3) Add 420ml isopropanol under stirring, and let it cool to room temperature;

[0047] (4) Continue to stand for 2.5 hours, cool down to -15°C to crystallize in an ice bath, grow crystals for 7 hours, filter, wash the crystals with a small amount of absolute ethanol cooled to 0°C at least once, and dry under reduced pressure (the drying temperature is controlled at 50 The temperature is below ℃, the pressure is controlled at 12mmHg, and the drying time is 13 hours) to obtain 9.856g of Nelarabine crystal compound with a yield of 98.56% and a purity of 99.99%.

[0048] The X-ray powder diffraction pattern of ...

Embodiment 3

[0049] Example 3: Preparation of Nelarabine Crystals

[0050] (1) Add 10g of crude nelarabine to 115ml of ethanol and acetonitrile (1:1) mixture, heat to 72°C and stir for 1.2 hours;

[0051] (2) When the crude nelarabine is completely dissolved, add 0.015 g of activated carbon, continue to heat to reflux, keep for 25 minutes, filter while hot, and concentrate the filtrate;

[0052] (3) Add 230ml of isopropanol under stirring, let it cool to room temperature;

[0053] (4) Continue to stand for 1.5 hours, cool down to -5°C to crystallize in an ice bath, grow crystals for 9 hours, filter, wash the crystals with a small amount of absolute ethanol cooled to 0°C at least once, and dry under reduced pressure (the drying temperature is controlled at 50 The temperature is below ℃, the pressure is controlled at 8mmHg, and the drying time is 11 hours) to obtain 9.849g of Nelarabine crystal compound, with a yield of 98.49% and a purity of 99.99%.

[0054] The X-ray powder diffraction pattern of t...

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Abstract

The invention relates to an antitumor drug nelarabine powder-injection composition and belongs to the technical field of medicines. The powder-injection composition is composed of nelarabine and arginine. The nelarabine is crystal. The X-ray powder diffraction pattern obtained through Cu-K alpha ray measurement is as shown in the Figure 1. The new crystal of nelarabine is different from the crystal structure in the prior art. Through experimental verification, it is found that the new crystalline compound has high purity, good fluidity and water solubility and high stability, is not easy to absorb moisture and is safe and reliable in clinic application. The powder-injection composition prepared by the use of the new crystalline compound has advantages of high purity, low impurity content and good clarity. In addition, sub-packaging efficiency in production can be guaranteed; content uniformity is low; rate of adverse reaction is greatly reduced; and stability is better.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and relates to an antitumor drug nerabine powder injection composition. Background technique [0002] The chemical name of Nelarabine is 2-amino-9-β-D-arabinofuranosyl-6-methoxy-9H-purine, which is a deoxyguanosine analogue 9-β-D-arabinofuranoguanine ( ara-G), which was approved for marketing in 2005 and can be used to treat T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL). The structural formula is as follows: [0003] [0004] Nelarabine is a white or almost white crystalline powder, slightly soluble in water, and its solubility in water is about 8-9mg / ml (25℃, pH=4-10). Due to the poor solubility of Nelarabine in water, this limits its application in medicine to a certain extent. [0005] "Research Progress on the Synthesis of Nelarabine" [Liang Ping, Yin Xianqing, Li Weijia. Fine Chemical Intermediates, 2008, 38(5): 8-10], CN101348511A, CN101092441A all disclos...

Claims

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Application Information

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IPC IPC(8): A61K9/14C07H19/19C07H1/00A61K31/7076A61P35/00
CPCC07H19/19A61K9/0019A61K9/145A61K31/7076A61K47/183C07B2200/13C07H1/00
Inventor 杨献美
Owner 临沂草之美医药科技有限公司
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