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Low-cost preparation method of pharmaceutical adjuvant sodium stearyl fumarate

A technology of sodium stearyl fumarate and pharmaceutical excipients, which is applied to the preparation of carboxylic acid esters, the preparation of organic compounds, and organic chemical methods, and can solve problems such as unfavorable preparation processes, high preparation costs, and increased consumption of alkali solutions , to achieve high catalytic efficiency, high product quality, and reduce production costs

Active Publication Date: 2021-04-09
南京紫鸿生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In the above-mentioned method, hydrochloric acid is all adopted as isomerization catalyst, in the process of adding alkali solution to form salt subsequently, can increase the consumption of alkali solution; The intermediate product needs to be separated in advance, which is not conducive to simplifying the preparation process, and the preparation cost is high

Method used

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  • Low-cost preparation method of pharmaceutical adjuvant sodium stearyl fumarate
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  • Low-cost preparation method of pharmaceutical adjuvant sodium stearyl fumarate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] (1) PS microspheres with an average particle size of 10 μm were added to concentrated sulfuric acid, reacted at a temperature of 60 °C and stirred for 12 h, the reaction product was washed with water and anhydrous ethanol in turn, and dried in vacuum at a temperature of 60 °C to obtain Sulfonated polystyrene microspheres; the obtained sulfonated polystyrene microspheres were added to a 20% mass concentration of aluminum chloride ethanol solution for ultrasonic treatment for 2 h to carry out adsorption and immobilization reaction, washed with ethanol, and vacuum dried at 60°C to obtain sulfonation Aluminum trichloride supported on polystyrene microspheres.

[0047] (2) adding stearyl alcohol to maleic anhydride in a molar ratio of 1:1.02 into a toluene solvent, heating to 120-130° C., stirring and refluxing for 4 hours to obtain monostearyl maleate. The detected yield is 95%, and the product is detected according to the Chinese Pharmacopoeia CP2020 version. The peak time...

Embodiment 2

[0052] (1) PS microspheres with an average particle size of 50 μm were added to concentrated sulfuric acid, reacted at a temperature of 80 °C for 8 h under stirring conditions, the reaction product was washed with water and anhydrous ethanol in turn, and dried in vacuum at a temperature of 80 °C to obtain Sulfonated polystyrene microspheres; the obtained sulfonated polystyrene microspheres were added to a 10% mass concentration of aluminum chloride ethanol solution for ultrasonic treatment for 4 hours to carry out adsorption and immobilization reaction, washed with ethanol, and vacuum dried at 80°C to obtain sulfonation Aluminum trichloride supported on polystyrene microspheres.

[0053] (2) adding stearyl alcohol and maleic anhydride in a molar ratio of 1:1.05 to a toluene solvent, heating to 120-130° C., stirring and refluxing for 5 hours to obtain monostearyl maleate. The detected yield was 97.5%, and the product was detected according to the Chinese Pharmacopoeia CP2020 ve...

Embodiment 3

[0058] (1) PS microspheres with an average particle size of 80 μm were added to concentrated sulfuric acid, reacted at a temperature of 40 °C and stirring for 24 h, the reaction product was washed with water and anhydrous ethanol in turn, and vacuum-dried at a temperature of 80 °C to obtain Sulfonated polystyrene microspheres; the obtained sulfonated polystyrene microspheres were added to a 20% mass concentration of aluminum chloride ethanol solution for ultrasonic treatment for 4 h to carry out adsorption and immobilization reaction, washed with ethanol, and vacuum dried at 80°C to obtain sulfonation Aluminum trichloride supported on polystyrene microspheres.

[0059] (2) adding stearyl alcohol to maleic anhydride in a molar ratio of 1:1.1 into a cyclohexane solvent, heating to 90° C., stirring and refluxing for 5 hours to obtain monostearyl maleate. The yield was 90.7%. The product was detected according to the Chinese Pharmacopoeia CP2020 version. The peak time of monostear...

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Abstract

The invention belongs to the technical field of preparation of pharmaceutic adjuvants, and discloses a low-cost preparation method of a pharmaceutical adjuvant sodium stearyl fumarate. The method comprises the following steps: adding octadecanol and maleic anhydride into an organic solvent, performing heating to 90-130DEG C, carrying out a stirring reaction to obtain monooctadecanol maleate, adding a solid isomerization catalyst, continuously carrying out a heat preservation stirring reaction at 90-130DEG C to obtain monooctadecanol fumarate, performing filtering to separate a solid isomerization catalyst in the system, adding an alkali solution into the reaction system, carrying out stirring reaction at the temperature of 35-55DEG C, and separating and purifying a product to obtain the sodium stearyl fumarate. The solid isomerization catalyst and a one-pot method are adopted for synthesis, after catalysis is completed, separation can be conducted from a reaction system in a simple filtering mode, the production process is simplified, the production cost is reduced, and the product quality is high.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical excipients, in particular to a low-cost preparation method of a pharmaceutical excipient sodium stearyl fumarate. Background technique [0002] Sodium Stearyl Fumarate (C 22 H 39 NaO 4 ) is a widely used and important pharmaceutical excipient. During the metabolic process of sodium stearyl fumarate in animals, most of it can be absorbed, and hydrolyzed to produce stearyl alcohol and stearic acid, and a small part can be directly and quickly metabolized, which is non-toxic and non-irritating. In the pharmaceutical field, sodium stearyl fumarate is added to pharmaceutical preparations, which can be used as a lubricant for tablets and capsules, and can also form a protective film in effervescent tablets, which can solve the problem of stearate lubricants. The existing problems, such as the influence of the main drug, excessive lubrication, can improve the disintegration of the drug and pro...

Claims

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Application Information

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IPC IPC(8): C07C67/08C07C67/333C07C67/28C07C69/60B01J31/10
CPCC07C67/08C07C67/333C07C67/28B01J31/10C07B2200/09B01J2231/52C07C69/60Y02P20/584
Inventor 洪怡沈惠母逸青
Owner 南京紫鸿生物科技有限公司
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