Traditional chinese medicine Monascus purpureus went using Lovastatin salt as main active and its preparation component

A technology of lovastatin and active ingredients, which is applied in the fields of medicine and chemistry, can solve the problems of poor lipid-lowering effect, poor water solubility, and high cost, and achieve the goals of preventing and treating cardiovascular and cerebrovascular diseases, reducing toxic side effects, and improving absorption efficiency Effect

Inactive Publication Date: 2004-07-21
云南永安制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Recently, people have used modern technology to develop red yeast rice with different characteristics for medicinal or edible functions. Chinese patent No. 01119961 discloses "a water-soluble lipid-lowering red yeast rice pigment". The purpose is to overcome the complicated process of the existing methods. , high cost, poor water solubility, and poor lipid-lowering effect, the main functional component of the developed red yeast rice is water-soluble red pigment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1. Take lovastatin sodium salt as the preparation of main component mixture (II)

[0016] Take 50g of the solid state fermented Monascus with a certain content of statin, adjust the pH value to 8.5 with 1% NaOH without stirring, and continue stirring until the pH value of the solid matter is uniform. Then the solid was moved to an oven at 70° C. and dried to constant weight to obtain 28 g of mixture (II). The statin content measured by HPLC was 25 mg statin / g red yeast rice, wherein lovastatin sodium accounted for 90% of the total statin content.

Embodiment 2

[0017] Embodiment 2. Pulverize the mixture (II) obtained in Example 1, add 75% ethanol 60ml of pH=9, extract with ultrasonic treatment for 3 minutes, after that, stand still for 10 minutes, filter, collect the filtrate, and transfer the filtered solids to 40ml In the 75% ethanol solution of pH=9, stir 5 minutes, extract, stand still 3 minutes, filter and merge filtrate, obtain 92ml filtrate, remove ethanol solution with vacuum distillation by filtrate to obtain solid powder mixture (II) 1.8g, use The content of statin was measured by HPLC, and the content of lovastatin sodium was 94%.

Embodiment 3

[0018] Example 3. The mixture (II) obtained in Example 2 was dissolved in a pH=9 aqueous solution, and column chromatography was used. This was carried out several times, and the purity of the separated components was detected by HPLC, and 23 mg of lovastatin sodium [compound (I)] was obtained after separation.

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PUM

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Abstract

A Chinese medicine 'Red koji' containing lovestatin as its main active component in the form of tablet, capsule, powder, dripping pill, or particles for preventing and treating cardiovascular and cerebrovascular diseases is prepared through fermenting and extracting.

Description

[0001] Technical field: The present invention relates to the technical fields of chemistry and medicine, in particular to a traditional Chinese medicine red yeast rice and its preparation with lovastatin salt as the main active ingredient. Background technique [0002] In 1979, Japanese scholars Endo et al. isolated the HMG-CoA reductase inhibitor Monacolin K from Monascus. In 1980, American researchers Alberts et al. isolated the substance Mevinolic acid with the same structure from Aspergillus terreus. The compound was transformed into lovastatin (Lovastatin and Mevinolin, marketed under the trade name "Mevacor", and it was widely used, which promoted the research and development of statin drugs. After that, several statin drugs were launched, among which Modonsa Company is in the market of Lovastatin Based on this, the second-generation statin was launched: Simvastatin. Among all the statin drugs on the market and in the research and development stage, only lovastatin and si...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/366A61P3/06A61P9/10
Inventor 陈春珍李占铭王立新李朝晖
Owner 云南永安制药有限公司
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