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Production process of Lipstatin

A production process, lipox technology, applied in the field of drug synthesis, can solve the problems of low fermentation titer and high production cost, and achieve the effect of low fermentation cost, low cost and short fermentation time

Inactive Publication Date: 2013-03-13
GUANGZHOU MINGSHIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, the process of fermentative production of riprestatin has the disadvantages of high production cost (about 2500-3000 yuan / kg) and low fermentation titer (about 7000mg / L)

Method used

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  • Production process of Lipstatin
  • Production process of Lipstatin
  • Production process of Lipstatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 A production process of riprestatin

[0037] Including the following steps:

[0038] A. Preparation of fermentation medium

[0039] In terms of mass percentage, the formula of 20L fermentation medium is: 2.5% glycerin, 3% soybean powder, 1.5% lecithin, 5% sunflower oil, 0.01% magnesium sulfate, 0.05% calcium carbonate, appropriate amount of trace elements (chlorinated Manganese: 0.001%, zinc chloride 0.0015%), and the balance is deionized water. Sterilize the culture medium by conventional methods.

[0040] B. Inoculation, fermentation culture

[0041] Streptomyces toxin was inoculated in the fermentation medium, the inoculum amount was 5% (V / V) of the fermentation broth, and the strain concentration of the bacteria solution was 15%; fermented at 27°C±1°C for 8 days; using hydrogen oxidation Sodium and hydrochloric acid are automatically balanced to adjust the pH value of the fermentation broth, so that the pH value is maintained at 7.0; during the ferment...

Embodiment 2

[0051] Embodiment 2 A kind of production process of riprestatin

[0052] Including the following steps:

[0053] A. Preparation of fermentation medium

[0054] In terms of mass percentage, the formula of 20L fermentation medium is: 3% glycerin, 4.5% soybean powder, 2% lecithin, 8% sunflower oil, 0.05% magnesium sulfate, 0.2% calcium carbonate, appropriate amount of trace elements (chloride Manganese: 0.001%, zinc chloride 0.0015%), and the balance is deionized water. Sterilize the culture medium by conventional methods.

[0055] B. Inoculation, fermentation culture

[0056]Streptomyces toxin was inoculated in the fermentation medium, the inoculation amount was 8% (V / V) of the fermentation broth, and the strain concentration of the bacteria solution was 20%; fermented at 27°C±1°C for 7 days; using hydrogen oxidation Sodium and hydrochloric acid are automatically balanced to adjust the pH value of the fermentation broth, so that the pH value is maintained at 7.0; during the ...

Embodiment 3

[0066] Example 3 A production process of riprestatin

[0067] Including the following steps:

[0068] A. Preparation of fermentation medium

[0069] In terms of mass percentage, the formula of 20L fermentation medium is: 4.5% glycerin, 6.5% soybean powder, 4% lecithin, 9% sunflower oil, 0.15% magnesium sulfate, 0.4% calcium carbonate, appropriate amount of trace elements (chloride Manganese: 0.001%, zinc chloride 0.0015%), and the balance is deionized water. Sterilize the culture medium by conventional methods.

[0070] B. Inoculation, fermentation culture

[0071] Streptomyces toxin was inoculated in the fermentation medium, the inoculation amount was 10% (V / V) of the fermentation broth, and the strain concentration of the bacteria solution was 20%; fermented at 27°C±1°C for 8 days; using hydrogen oxidation Sodium and hydrochloric acid are automatically balanced to adjust the pH value of the fermentation broth, so that the pH value is maintained at 7.0; during the ferment...

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Abstract

The invention discloses a production process of Lipstatin, which adopts a special fermentation medium to ferment and culture streptomyces toxytricini; and the Lipstatin can be prepared by fermenting, purifying and refining the streptomyces toxytricini. According to the production technology, soybean meal, sunflower oil, glycerol and the like are taken as nitrogen source and carbon source of the fermentation medium; the high-purity Lipstatin can be prepared by regulation fermentation technology and purification technology, so that the production cost of the Lipstatin is greatly reduced, the fermentation valence is improved, and the problems of high production cost and low fermentation valence in the prior art can be solved.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and more specifically, the invention relates to a new production process of liprestatin. Background technique [0002] Lipstatin (English name Lipstatin), a white oily substance, is a pharmaceutical intermediate used to produce a new type of weight-loss drug, Orlistat. Orlistat is produced from the fermented liprestatin by one-step hydrogenation reduction. Orlistat is currently the only weight-loss drug in the world. It is a long-acting and potent specific gastrointestinal lipase inhibitor. The covalent bond inactivates the enzyme to play a therapeutic role. The inactivated enzyme cannot hydrolyze the fat in food, mainly triglyceride, into absorbable free fatty acid and monoacylglycerol. Undigested triglycerides cannot be absorbed by the body, thereby reducing caloric intake and controlling weight. [0003] Streptomyces toxin (Latin scientific name: Streptomycestoxytricini) belongs to the family ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P17/02C12R1/465
Inventor 安鸿尹海滨
Owner GUANGZHOU MINGSHIN PHARMA
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