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Process for purifying zidovudine palmitate raw materials and preparations thereof

A technology of palmitate and zidovudine, applied in the field of medicine, can solve problems such as no manufacturer's production

Inactive Publication Date: 2006-09-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Zidovudine palmitate is a compound formed by the esterification of zidovudine and palmitoyl chloride. It is a prodrug of the anti-AIDS drug zidovudine. At present, there is no manufacturer at home and abroad.

Method used

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  • Process for purifying zidovudine palmitate raw materials and preparations thereof
  • Process for purifying zidovudine palmitate raw materials and preparations thereof
  • Process for purifying zidovudine palmitate raw materials and preparations thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Take 10g of the synthetic zidovudine palmitate crude product, dissolve it in 400mL 95% ethanol at 50°C, add 0.5g of activated carbon, stir, mix well, remove the activated carbon by suction filtration, cool the filtrate, stir for 10 minutes, continue After cooling down to -20°C, a large amount of zidovudine palmitate precipitated after half an hour as needle crystals, and the pure product was obtained by suction filtration. The appearance is white, the related substance is 0.73% as determined by HPLC, and the purity is 99.27%.

Embodiment 2

[0043] Take 10g of the synthesized crude zidovudine palmitate, dissolve it in 300mL of methanol at 40°C, add 1g of silica gel, stir, mix well, remove the silica gel by suction filtration, cool the filtrate, stir for 10 minutes, and continue to cool down to - After 1 hour at 20°C, a large amount of zidovudine palmitate precipitated as needle crystals, and the pure product was obtained by suction filtration. The appearance is white, and the related substance is 0.78% as determined by HPLC, and the purity is 99.22%.

Embodiment 3

[0045] Take 10 g of the synthesized crude product of zidovudine palmitate, dissolve it in 100 mL of methanol-ethyl acetate (100:1) at 40 ° C, add 1 g of silica gel, stir, mix well, remove the silica gel by suction filtration, and cool the filtrate , stirred for 10 minutes, and continued to cool down to -20°C. After 1 hour, a large amount of zidovudine palmitate was precipitated as needle crystals, and the pure product was obtained by suction filtration. The appearance is white, and the related substance is 0.88% as determined by HPLC, and the purity is 99.12%.

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Abstract

The invention relates to a refining method for Azidothimidine palmitate (or stearate) stock and its preparation, which sets up a decontamination method for Azidothimidine palmitate and improves the medicinal satefty. The main technical project consists of dissolving the stock of Azidothimidine palmitate or stearate with right amount of organic solvents, adding adsorbent or not, heat-preserving at the indoor temperature of 80 DEG C and stirring for 5-500 minutes, filtering to remove the adsorbent, adjusting a low-temperature to 5--50 DEG C and dispensing for 1-100 hours, collecting the precipitate, and drying to obtain the target product. The purified Azidothimidine palmitate stock is white or similar to white, and its purity quotient is more than 99 % checked by HPLC. The purified Azidothimidine palmitate or stearate stock can further prepare various preparations which include emulsion, liposome, hard or soft capsule, tablet, granula and turbid agent. The internal pharmacokinetics after being injected by Azidothimidine palmitate is studied by the said liposome and emulsion prepared by the high-mass Azidothimidine palmitate stock, which provides an authentic criteria for clinical application.

Description

Technical field: [0001] The invention relates to the technical field of medicines, in particular to a method for refining zidovudine palmitate or stearate raw materials, relative quality indicators and a preparation prepared by using the refined raw materials. Background technique: [0002] Zidovudine palmitate is a compound formed by esterification of zidovudine and palmitoyl chloride. It is a prodrug of the anti-AIDS drug zidovudine. At present, there is no manufacturer at home and abroad. Domestic manufacturers of zidovudine include Northeast Pharmaceutical General Factory, Henan Tianfang Pharmaceutical Co., Ltd., Beijing Bokangjian Gene Technology Co., Ltd., Shanghai Modern Pudong Pharmaceutical Co., Ltd., Shandong Haishan Pharmaceutical Co., Ltd., Shanghai Desano Chemical Co., Ltd. Pharmaceutical Co., Ltd., Qilu Pharmaceutical Co., Ltd., Hubei Garrett Pharmaceutical Co., Ltd., Xiamen Mike Pharmaceutical Co., Ltd. and other 9 companies. The chemical structure of zidovud...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/06C07H1/06A61K31/7072A61K9/127A61P31/18
Inventor 邓意辉陈国良毕殿洲雷杰杰徐晖王绍宁周欣羽赵静王宁沈琳
Owner SHENYANG PHARMA UNIVERSITY
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