Production tech. of acid type lovastatin and production tech of its salt and pharmaceutical application

A technology of lovastatin and production process, which is applied in the field of production process of acid lovastatin and acid lovastatin salt, which can solve the problems of toxic side effects, muscle pain, elevated transaminase, liver damage, etc., and avoid toxic and side effects , the effect of increasing the burden on the liver

Inactive Publication Date: 2007-07-18
吴娟
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The current lipid-regulating lovastatin fermented by Aspergillus terreus (i.e. monacolin K, lovastatin) is in the form of lactone, and the lactone form itself has no pharmacological effect and is only the precursor of the active substance, which is secreted by the liver in the body. After enzymatic hydrolysis, it is transformed into an active substance (acid structure), so lovastatin has obvious toxic side effects, damages the liver, causes muscle pain and increases transaminase

Method used

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Embodiment Construction

[0006] The preparation method of lovastatin acid: use 95% ethanol and NaOH (100:8 ~ 13 ie m 内酯结构 :m NaOH ) to make an alkaline solution, dissolve the lactone lovastatin powder in the solution, and bathe in a water bath at 50-75°C for 30 minutes. After the water bath is completed, measure the pH value with a pH meter (usually pH10-14), Adjust the PH value so that it is between PH7.5-9.0, control the temperature at 50-75°C, and distill under reduced pressure at a pressure of -0.08MP to evaporate most of the ethanol, and then adjust the pH of the mother liquor to make it PH as Between 4.0-6.8, continue to distill under reduced pressure to obtain a concentrated solution, and then use solvent and anhydrous CaCl 2 Acid lovastatin (namely monacolin K, lovastatin) with a concentration of more than 90% is obtained through extraction.

[0007] The preparation method of acid lovastatin salt: adopt 95% ethanol and NaOH (100:8~13 namely m 内酯结构 :m NaOH ) to make an alkaline solution, di...

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Abstract

A lovastatin acid and lovastatin acid salt production processes and their application, to solve the problem of significantly toxicity of lactone form lovastatin, such as liver injury and causing muscle pain and elevating transaminase. The invention uses 95% ethanol and NaOH (13 ~ 100:8 that m lactone structure: mNaOH) to modulate into alkaline solution, makes lactone lovastatin powder dissolved in solution, and uses HCl adjust PH to obtain the acid form and salt state compounds, widely used for lipid drug.

Description

technical field [0001] The invention relates to a medicine production process, in particular to the production process of acid lovastatin (ie monacolin K, lovastatin) and acid lovastatin (ie monacolin K, lovastatin) salt and its application. Background technique [0002] The current lipid-regulating lovastatin fermented by Aspergillus terreus (i.e. monacolin K, lovastatin) is in the form of lactone, and the lactone form itself has no pharmacological effect and is only the precursor of the active substance, which is secreted by the liver in the body. After enzymatic hydrolysis, it is transformed into an active substance (acid structure), so lovastatin has obvious toxic and side effects, which can damage the liver, cause muscle pain and increase transaminase. Contents of the invention [0003] The task of the present invention is to provide the production process and application of acid lovastatin and acid salt with little toxic and side effects, no damage to the liver, and ...

Claims

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Application Information

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IPC IPC(8): C07C69/732A61K31/22A61K9/00A61P3/06
Inventor 施与文
Owner 吴娟
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