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Metacavir crystal form, preparation method thereof and medicinal composition containing metacavir crystal form

A technology of metacavir and crystal form, which is applied in the field of metacavir crystal form, its preparation and pharmaceutical composition containing it, can solve the problems of poor water solubility of ddG, unstable temperature, difficulty and the like, and achieves less solvent amount. , good stability and high yield

Active Publication Date: 2011-05-25
GUANGZHOU YIPINHONG PHARMA +5
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is mainly due to the physical and chemical properties of ddG. ddG has poor water solubility and is extremely unstable to temperature. It generally needs to be stored at -20°C and is easily degraded in the body, so it is difficult to become a drug.

Method used

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  • Metacavir crystal form, preparation method thereof and medicinal composition containing metacavir crystal form
  • Metacavir crystal form, preparation method thereof and medicinal composition containing metacavir crystal form
  • Metacavir crystal form, preparation method thereof and medicinal composition containing metacavir crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of metacavir

[0022] Add 80ml of ethanol to 11 grams of metacavir (moisture content 2.1%), heat to dissolve at 40°C, heat filter, and crystallize at 15°C for 24 hours. Filter, rinse with an appropriate amount of cold ethanol, vacuum dry, monitor the water content, and pulverize to obtain 7.8 grams of white powder metacavir with a water content of 2.0%. Measure under the following experimental conditions to obtain the powder X-ray diffraction pattern ( figure 1 ):

[0023] XTRA X-ray diffractometer;

[0024] Start Angle: 2 End Angle: 40 Step Size: 0.2

[0025] Scan speed: 10 Target type: Cu

[0026] Pipe flow Pipe pressure: 40KV 40mA Slit: 2 / 4 / 0.5 / 0.2

[0027] The following table is the powder X-diffraction spectrum data of the metacavir prepared by applying this method

[0028]

[0029]

Embodiment 2

[0030] Embodiment 2: the preparation of metacavir

[0031] Add 750ml of ethanol to 110 grams of metacavir (moisture content 2.1%) product, heat to dissolve at 40°C, heat filter, and crystallize at 12°C for 24 hours. Filter, rinse with an appropriate amount of cold ethanol, vacuum dry, monitor the water content, and pulverize to obtain 80 grams of white powder metacavir with a water content of 1.8%. Its powder X-diffraction spectrum pattern is consistent with embodiment 1.

Embodiment 3

[0032] Embodiment 3: the preparation of metacavir

[0033] Add 4000ml of ethanol to 550 grams of metacavir (moisture content 2.1%) product, heat to dissolve at 40°C, heat filter, and crystallize at 18°C ​​for 24 hours. Filter, rinse with an appropriate amount of cold ethanol, vacuum dry, monitor the water content, and pulverize to obtain 410 g of white powdered metacavir with a water content of 1.6%. Its powder X-diffraction spectrum pattern is consistent with embodiment 1.

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PUM

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Abstract

The invention belongs to the field of medicines, and relates to a novel specific crystal form of metacavir, and a preparation method thereof. The novel specific crystal form of metacavir is characterized by a powder X-ray diffraction map. The invention also relates to a medicinal preparation consisting of the crystal form and pharmaceutically acceptable auxiliary materials, and application of the crystal form in preparing anti-hepatitis B medicines.

Description

technical field [0001] The invention relates to a specific crystal form of metacavir and a preparation method thereof; a pharmaceutical preparation composed of the crystal form and pharmaceutically acceptable auxiliary materials and its use in the preparation of drugs for reducing heart rate and in the preparation of drugs for treating or preventing angina pectoris Applications. Background technique [0002] Hepatitis B (hepatitis B), referred to as hepatitis B, is an infectious disease caused by hepatitis B virus (HBV), which mainly causes liver lesions and can cause damage to various organs. More than 500,000 people die from primary liver cancer every year in the world, and as many as 80% of the primary liver cancers are caused by chronic hepatitis B. Of the 400 million chronic hepatitis B patients, 75% live in Asia, and my country is the country with the highest incidence of hepatitis B. The latest data show that the number of deaths due to liver disease in my country i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/16A61K31/708A61P1/16
Inventor 刘彩连
Owner GUANGZHOU YIPINHONG PHARMA