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Method for preparing paracetamol-betaine cocrystal by supercritical anti-solvent particle production technique

A technology of supercritical anti-solvent and paracetamol, applied in the field of medicine and chemical industry, can solve the problems of drug absorption effect to be improved, uneven particle size distribution, large eutectic particle size, etc., achieve less additives and solvent residues, uniform particle size distribution, and The effect of uniform diameter

Active Publication Date: 2017-10-03
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the eutectic particle size prepared in this document is large, and the particle size distribution is uneven, and the drug absorption effect needs to be improved.

Method used

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  • Method for preparing paracetamol-betaine cocrystal by supercritical anti-solvent particle production technique
  • Method for preparing paracetamol-betaine cocrystal by supercritical anti-solvent particle production technique
  • Method for preparing paracetamol-betaine cocrystal by supercritical anti-solvent particle production technique

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Preparation of paracetamol and betaine co-crystal microparticle preparation: accurately measure 50ml DCM and 50ml EtOH to prepare a mixed solvent, accurately weigh 500mg paracetamol and 500mg betaine, and dissolve them in the mixed solvent to prepare a mixed solution. Open the cylinder, and use a high-pressure pump to inject the anti-solvent (frozen and high-pressure carbon dioxide solution) into the settling kettle, and control the flow rate of the anti-solvent to 30 g / min. The carbon dioxide solution becomes a gas, and the pressure in the settling tank increases. When the temperature and pressure in the settling tank reach the set value (set the settling tank temperature to 40℃ and pressure to 100bar), use another high-pressure pump to reduce the mixed solvent to 0.8 The rate of ml / min was passed into the settling kettle, after 15 minutes, the mixed solvent was stopped, and the mixed solution was injected at a rate of 0.8 ml / min. After the sample injection, continue to...

Embodiment 2

[0043] Preparation of paracetamol and betaine co-crystal microparticle preparation: accurately measure 80ml DCM and 20ml MTH to prepare a mixed solvent, accurately weigh 500mg paracetamol and 500mg betaine, and dissolve them in the mixed solvent to prepare a mixed solution. Open the cylinder, and use a high-pressure pump to inject the anti-solvent (frozen and high-pressure carbon dioxide solution) into the settling kettle, and control the flow rate of the anti-solvent to 30 g / min. The carbon dioxide solution becomes a gas, and the pressure in the settling tank increases. When the temperature and pressure in the settling tank reach the set value (set the settling tank temperature to 40℃ and pressure to 100bar), use another high-pressure pump to reduce the mixed solvent to 0.8 The rate of ml / min was passed into the settling kettle, after 15 minutes, the mixed solvent was stopped, and the mixed solution was injected at a rate of 0.8 ml / min. After the sample injection, continue to ...

Embodiment 3

[0047] Preparation of paracetamol and betaine co-crystal microparticle preparation: accurately measure 80ml DCM and 20ml MTH to prepare a mixed solvent, accurately weigh 500mg paracetamol and 500mg betaine, and dissolve them in the mixed solvent to prepare a mixed solution. Open the cylinder, and use a high-pressure pump to inject the anti-solvent (frozen and high-pressure carbon dioxide solution) into the settling kettle, and control the flow rate of the anti-solvent to 30 g / min. The carbon dioxide solution becomes a gas, and the pressure in the settling tank increases. When the temperature and pressure in the settling tank reach the set value (set the settling tank temperature to 40℃ and pressure to 100bar), use another high-pressure pump to reduce the mixed solvent to 0.8 The rate of ml / min was passed into the settling kettle, after 15 minutes, the mixed solvent was stopped, and the mixed solution was injected at a rate of 1.1 ml / min. After the sample injection, continue to ...

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Abstract

The invention discloses a method for preparing a paracetamol-betaine cocrystal by a supercritical anti-solvent particle production technique. The method comprises the following steps: adding paracetamol and betaine into an organic solvent respectively in a mole ratio of 1:1 or 1:2 to prepare a mixed solution; by using supercritical carbon dioxide as an anti-solvent, continuously introducing the anti-solvent into a settling kettle at a constant flow velocity by using a high-pressure pump; and when the temperature in the settling kettle is 35-50 DEG C and the pressure is 80-120bar, spraying the mixed solution into the settling kettle by using another high-pressure pump to precipitate the cocrystal drug particles. Compared with the grinding process in the past, the paracetamol-betaine cocrystal prepared by the method disclosed by the invention has the advantages of small particle size, uniform particle size distribution, high stability, higher solubility and higher dissolution rate. Different crystal forms can be obtained by changing the experimental conditions, thereby enhancing the bioavailability and drug effect of the paracetamol drug, and satisfying the medicinal requirements. The preparation method is simple to operate, has favorable repeatability, and can easily implement industrialized production.

Description

Technical field [0001] The invention belongs to the field of medicine and chemical industry, and relates to a preparation method of the antipyretic and analgesic paracetamol-betaine co-crystal. Background technique [0002] Paracetamol, the molecular formula is C 8 H 9 NO 2 ; Betaine, molecular formula is C 5 H 11 NO 2 It can be extracted from the roots, stems, leaves and fruits of natural plants. It is sweet, bactericidal and anti-inflammatory, and can be used medicinally; the molecular formula of paracetamol-betaine co-crystal is C 13 H 20 N 2 O 4 , The chemical structure is shown below. [0003] [0004] Paracetamol (APAP), also known as acetaminophen or acetaminophen, is the preferred antipyretic and analgesic recommended by the World Health Organization. Because of its fast oral absorption, no damage to the liver under normal doses, relatively few adverse reactions, little irritation to the gastrointestinal tract, and no effect on the blood coagulation mechanism. It is a safer...

Claims

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Application Information

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IPC IPC(8): C07C231/12C07C233/25C07C227/16C07C229/12
CPCC07B2200/13C07C227/16C07C231/12C07C233/25C07C229/12Y02P20/141Y02P20/54
Inventor 江燕斌赵紫怡胡曼林清刘川
Owner SOUTH CHINA UNIV OF TECH
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