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Preparation method of butenolide compound composite nanocrystals

A crotonic acid lactone and nanocrystal technology is applied in the preparation of organic compounds, the preparation of carboxylic acid esters, organic chemical methods, etc., and can solve the problems of not easy to maintain for a long time, poor stability, restrictions on promotion and use, etc., and achieve stable solutions. Sexual issues, low cost, simple steps

Active Publication Date: 2021-03-30
THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its poor stability, it is not easy to maintain for a long time at room temperature, which has greatly restricted its promotion and use.

Method used

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  • Preparation method of butenolide compound composite nanocrystals
  • Preparation method of butenolide compound composite nanocrystals
  • Preparation method of butenolide compound composite nanocrystals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The butyrolactone compound in this example is the fermentation compound butyrolactone I (abbreviation: BTL-1) of Aspergillus terreus H768.

[0029] A method for preparing a butenolide compound nanocrystal, comprising the following steps:

[0030] S1, prepare a BTL-1 ethanol solution with a concentration of 100 mg / mL;

[0031] S2, configure 100mg / mL anhydrous sodium sulfite aqueous solution;

[0032] S3, the BTL-1 ethanol solution 1 in S1 and the anhydrous sodium sulfite aqueous solution 2 in S2 are respectively drawn into the catheter by pump one 3 and pump two 4 and injected into the microporous fiber tube bundle nanocrystallizer 5 respectively, and set to feed into BTL -1 The rotating speed of the pump one of the ethanol solution is 100rpm, and the rotating speed of the pump two which is set to pass into anhydrous sodium sulfite aqueous solution is 300rpm, so that the two are mixed in the microporous fiber tube bundle nano crystallizer 5, and the two interact to form...

Embodiment 2

[0035] The butyrolactone compound in this example is the fermentation compound butyrolactone I (abbreviation: BTL-1) of Aspergillus terreus H768.

[0036] A method for preparing a butenolide compound nanocrystal, comprising the following steps:

[0037] S1, prepare a BTL-1 ethanol solution with a concentration of 100 mg / mL;

[0038] S2, configure 5mg / mL anhydrous sodium sulfite aqueous solution;

[0039] S3, the BTL-1 ethanol solution 1 in S1 and the anhydrous sodium sulfite aqueous solution 2 in S2 are pumped into the catheter through pump one 3 and pump two 4 respectively and then injected into the microporous fiber tube bundle nano crystallizer 5 respectively, and the setting is passed into The rotating speed of the pump one of BTL-1 ethanol solution is 30rpm, and the rotating speed of setting the pump two that feeds anhydrous sodium sulfite aqueous solution is 300rpm, makes the two mix in microporous fiber tube bundle nano crystallizer 5, and the two interact to form cont...

Embodiment 3

[0042] The butyrolactone compound in this example is the fermentation compound butyrolactone I (abbreviation: BTL-1) of Aspergillus terreus H768.

[0043] A method for preparing a butenolide compound nanocrystal, comprising the following steps:

[0044] S1, prepare a BTL-1 ethanol solution with a concentration of 100 mg / mL;

[0045] S2, configure 100mg / mL sodium bisulfite aqueous solution;

[0046] S3, the sodium bisulfite aqueous solution 2 in the BTL-1 ethanol solution 1 in S1 and the sodium bisulfite solution 2 in S2 are pumped into the catheter by pump one 3 and pump two 4 respectively and inject in the microporous fiber tube bundle nano crystallizer 5 respectively, set the pass Enter the rotating speed of the pump one of BTL-1 ethanol solution to be 300rpm, set the rotating speed of the pump two that feeds sodium bisulfite aqueous solution to be 200rpm, make the two mix in microporous fiber tube bundle nano crystallizer 5, the two interact Forming a mixed solution conta...

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Abstract

The invention discloses a preparation method of butenolide compound composite nanocrystals, and belongs to the technical field of pharmaceutical compounds. The preparation method comprises the following steps: reacting an organic solution of butenolide compounds with an antioxidant aqueous solution in a microporous fiber tube bundle nanocrystallizer, and controlling the proper flow rate and solution concentration, and forming the butenolide compound composite nanocrystals; the composite nanocrystals can greatly improve the solubility and the stability of butenolide compounds, and more specifically, the composite nanocrystals of the fermentation compound butyractone I of the butenolide compounds aspergillus terreus H768 can be used for preparing, researching and developing medicines thereofso as to have good application prospect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical compounds, in particular to a method for preparing a butenolide compound nanocrystal. Background technique [0002] In the process of drug development, the promotion and application of drugs are often hindered due to the instability of the drug itself. Among them, the oxidation reaction of drugs is one of the main factors causing drug instability. The oxidative degradation of most drugs is an autoxidative process involving free radicals, in which very little oxygen is required to initiate a reaction. Oxygen in the air accounts for 21%. In the presence of such a large amount of oxygen, the drug does not need the participation of other oxidants, and can spontaneously cause "autooxidation reaction" at room temperature. The process of this reaction is very complicated, and it belongs to the "chain reaction" induced by free radicals. Light and heat can accelerate the progress of this reaction,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/68C07C69/84C07C67/00A61K31/365A61P37/08
CPCC07D307/68C07C69/84C07C67/00A61P37/08C07B2200/07C07B2200/13
Inventor 杨献文谢春兰何志辉鄢庆祥肖宏秀
Owner THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
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