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Method for preparing acyclovir 2/3 hydrate

一种水合物、化合物的技术，应用在2/3水合物的制备领域，能够解决未见文献报道ACV2/3水合物制备方法和XRD表征数据等问题，达到良好晶型稳定性、晶型保持不变、制备工艺简单的效果

Active Publication Date: 2009-12-16
ZHEJIANG CHARIOTEER PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But there is no literature report on the preparation method and XRD characterization data of ACV2 / 3 hydrate

Method used

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  • Method for preparing acyclovir 2/3 hydrate
  • Method for preparing acyclovir 2/3 hydrate
  • Method for preparing acyclovir 2/3 hydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Heat the mixture of 10g crude acyclovir and 120ml water to 95°C, stir to dissolve, filter, cool the filtrate to 20-25°C, crystallize for 5 hours, filter, and dry the obtained solid in vacuum at 50°C for 20 hours to obtain aciclovir 9.8 g of Lowe crystals were determined by HPLC, and the content was 99.6%. Grind into a powder with a particle size of 200 mesh. Cu-Kα radiation, X-ray powder diffraction represented by 2θ angle and interplanar spacing (d value) at about 7.0 (12.7), about 10.5 (8.4), about 13.1 (6.8), about 16.1 (5.5), about 18.3 There are obvious characteristic absorption peaks at about 21.0 (4.2), about 24.9 (3.7), about 26.2 (3.4), and about 29.2 (3.0). Thermogravimetry (TG) has a weight loss of about 5.1%. Infrared absorption spectrum (KBr tablet) at about 3522, about 3471, about 3438, about 3294, about 3180cm -1 , about 2854cm -1 , about 2698, about 1716cm -1 , about 1631cm -1 , about 1610cm -1 , about 1483cm -1 , about 1388cm -1 , about 1182cm ...

Embodiment 2

[0029] Heat the mixture of 10g crude acyclovir and 150ml water to 90°C, stir to dissolve, filter, cool the filtrate to 20-25°C, crystallize for 5 hours, filter, and dry the obtained solid in vacuum at 50°C for 20 hours to obtain aciclovir 9.6 g of Lowe crystals were determined by HPLC, and the content was 99.7%. Grind into a powder with a particle size of 200 mesh. Cu-Kα radiation, X-ray powder diffraction represented by 2θ angle and interplanar spacing (d value) at about 7.0 (12.7), about 10.5 (8.4), about 13.1 (6.8), about 16.1 (5.5), about 18.3 There are obvious characteristic absorption peaks at about 21.0 (4.2), about 24.9 (3.7), about 26.2 (3.4), and about 29.2 (3.0). Thermogravimetry (TG) has a weight loss of about 5.1%. Infrared absorption spectrum (KBr tablet) at about 3522, about 3471, about 3438, about 3294, about 3180cm -1 , about 2854cm -1 , about 2698, about 1716cm -1 , about 1631cm -1 , about 1610cm -1 , about 1483cm -1 , about 1388cm -1 , about 1182cm ...

Embodiment 3

[0031] Heat the mixture of 10g crude acyclovir and 200ml water to 90°C, stir to dissolve, filter, cool the filtrate to 20-25°C, crystallize for 10 hours, filter, and dry the obtained solid in vacuum at 50°C for 20 hours to obtain aciclovir 9.5 g of Lowe crystals were determined by HPLC, and the content was 99.7%. Grind into a powder with a particle size of 200 mesh. Cu-Kα radiation, X-ray powder diffraction represented by 2θ angle and interplanar spacing (d value) at about 7.0 (12.7), about 10.5 (8.4), about 13.1 (6.8), about 16.1 (5.5), about 18.3 There are obvious characteristic absorption peaks at about 21.0 (4.2), about 24.9 (3.7), about 26.2 (3.4), and about 29.2 (3.0). Thermogravimetry (TG) has a weight loss of about 5.1%. Infrared absorption spectrum (KBr tablet) at about 3522, about 3471, about 3438, about 3294, about 3180cm -1 , about 2854cm -1 , about 2698, about 1716cm -1 , about 1631cm -1 , about 1610cm -1 , about 1483cm -1 , about 1388cm -1 , about 1182cm...

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Abstract

The invention discloses a method for preparing acyclovir 2 / 3 hydrate, which comprises the following steps of: feeding acyclovir and water according to weight ratio of 1:5-50; dissolving at a temperature of between 50 and 100 DEG C, and filtering the mixed solution; and cooling a filtrate to the temperature of between 0 and 30 DEG C for crystallization, filtering and collecting crystal, and drying the crystal for 0.5 to 24 hours at the temperature of between 0 and 150 DEG C to obtain the acyclovir 2 / 3 hydrate. The method has a simple preparation process and is suitable for industrialized mass production; and the prepared ACV 2 / 3 hydrate has performance needed for large-scale preparation production and good stability of crystal type.

Description

(1) Technical field [0001] The invention relates to a preparation method of 2 / 3 hydrate of nucleoside medicine acyclovir (ACV). (2) Background technology [0002] Acyclovir is a new type of HBV-DNA polymerase preparation, and it is a new type of broad-spectrum antiviral drug, which has antiviral activity on animals and humans. [0003] Kristl (Int.J.Phar.1996,139,231-235) reported 2 / 3 hydrate, unstable anhydrous crystal form and anhydrous (stable) crystal form 1 and anhydrous crystal form of ACV, studies have shown that, with other Compared with several crystal forms, ACV2 / 3 hydrate has better water solubility, therefore has better bioavailability, and is suitable for the preparation of antiviral agents. ACV in the European Pharmacopoeia is 2 / 3 hydrate. But there is no literature report on the preparation method and XRD characterization data of ACV2 / 3 hydrate. The crystal form of ACV hydrate (Form 3) reported by Young (Arch.Pharm.Res.2008, 31, 231-234) has a weight loss of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18A61P31/12
CPCC07D473/18A61K31/522A61P31/12
Inventor 蒲通范一陈恬雷鸣王乃星杨振杨建明
Owner ZHEJIANG CHARIOTEER PHARMA
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