Nelarabine injection composition and preparation method thereof

The technology of a composition and injection, which is applied in the field of medicine, can solve the problems of crystallization, blockage of microcirculation, and damage to health of nelarabine injection, and achieve the effect of simple and feasible preparation method, reduction of precipitation, and solution of crystallization problems

Active Publication Date: 2013-07-10
山东罗欣乐康制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] However, studies have shown that because sodium chloride can promote the precipitation of nelarabine, the nelarabine injectio

Method used

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  • Nelarabine injection composition and preparation method thereof
  • Nelarabine injection composition and preparation method thereof
  • Nelarabine injection composition and preparation method thereof

Examples

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Effect test

Embodiment 1

[0042] [Example 1] Preparation of Nelarabine Crystalline Compound

[0043] Get 25.0 g of the nalarabine crude product and put it into 800 ml of anhydrous methanol, heat to reflux for 2 hours, the nalarabine crude product is basically dissolved, then add 1 gram of activated carbon and reflux for 15 minutes, filter while it is hot, drop to room temperature, and cool to -5°C, crystallize, filter with suction, wash the filter cake with a small amount of ice methanol to obtain 11.6 g of fine nelarabine, which is the crystalline compound of nelarabine.

[0044] The obtained nelarabine crystalline compound is subjected to the following X-ray powder diffraction analysis:

[0045] Sample treatment: the prepared nelarabine crystalline compound was ground and passed through a 100-mesh sieve, and 50 mg was weighed as a sample for powder X-ray diffraction experiment.

[0046] Experimental instrument: Japan Rigaku D / max-2550 powder X-ray diffractometer.

[0047] Experimental conditions: C...

Embodiment 2

[0053] [embodiment 2] preparation of nelarabine crystalline compound

[0054] Take 25.0 g of crude nalarabine and put it into 750 ml of anhydrous methanol, heat to reflux, stir for 3 hours, and the nalarabine is basically dissolved, then add 1 g of activated carbon and reflux for 10 minutes, filter while it is hot, drop to room temperature, and cool down in an ice-salt bath At 0°C, crystallize, filter with suction, and wash the filter cake with a small amount of ice methanol to obtain 11.8 g of fine nelarabine, which is the crystalline compound of nelarabine.

Embodiment 3

[0055] [Example 3] Preparation of Nelarabine Crystalline Compound

[0056] Take 25.0 g of nalarabine crude product and put it into 875 ml of anhydrous methanol, heat to reflux, stir for 1 hour, and the nalarabine is basically dissolved, then add 1 g of activated carbon and reflux for 20 minutes, filter while it is hot, drop to room temperature, and cool down in an ice-salt bath At -3°C, crystallize, filter with suction, and wash the filter cake with a small amount of ice methanol to obtain 11.9 g of fine nelarabine, which is the crystalline compound of nelarabine.

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Abstract

The invention relates to a nelarabine injection composition, wherein the active ingredients of the drug are nelarabine and sodium chloride, wherein the nelarabine is nelarabine crystal compound; the crystal compound is measured by a powder X-ray diffractive determination method; and the obtained X-ray powder diffraction pattern is shown in a figure 2. By adopting the nelarabine injection composition provided by the invention, on one hand, the crystallization problem of the nelarabine injection can be well solved; the used nelarabine is a novel crystal nelarabine compound which is different from that in the prior art, so that the solubility of the nelarabine is increased because of change of the nelarabine crystal type; the nelarabine is fully dissolved, so as to reduce precipitation and avoid crystalline polamer; and on the other hand, the injection composition contains a drug active ingredient sodium chloride, so that normal internal physiological and biochemical activities and functions are fully ensured.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a nelarabine injection composition and a preparation method thereof. Background technique [0002] Nelarabine is the prodrug of the deoxyguanosine analogue 9-β-D-arabinofuranosylguanine (ara-G), which was approved for marketing in 2005 and can be used for the treatment of T-cell acute lymphoblastic leukemia (T -ALL) and T-cell lymphoblastic lymphoma (T-LBL). [0003] Nelarabine has the following structural formula, and its chemical name is 2-amino-9-β-D-arabinofuranosyl-6-methoxy-9H-purine. [0004] [0005] The research found that nelarabine is basically stable under the conditions of light (4500Lx±500Lx), high temperature (40°C, 60°C) and high humidity (25°C RH75%, 25°C 92.5%), and is stable under oxidation (10% hydrogen peroxide). , heated in a water bath for 1 hour), acid (1.0mol / L hydrochloric acid, heated in a boiling water bath for 1 hour) and alkali (1.0mol / L sodium...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/7076A61K47/02A61P35/02A61P35/00
Inventor 商世云李晓峰郑建伟肖锋
Owner 山东罗欣乐康制药有限公司
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