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Tandospirone citrate stable crystal form and preparation method thereof

A technology of tandospirone citrate and tandospirone, which is applied in the field of a stable crystal form of tandospirone citrate and its preparation, and can solve the problems of complex operation, unfriendly environment and high cost of the preparation method problems, to achieve the effects of simplified preparation process, good medicinal safety and stable quality

Pending Publication Date: 2021-07-16
PKU HEALTHCARE CORP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned patent discloses various crystal forms of tandospirone citrate, they are all mixed crystal forms and the preparation method has disadvantages such as cumbersome operation, high cost, and unfriendly environment.

Method used

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  • Tandospirone citrate stable crystal form and preparation method thereof
  • Tandospirone citrate stable crystal form and preparation method thereof
  • Tandospirone citrate stable crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 Preparation of stable crystalline form of tandospirone citrate

[0032] Weigh 100.0g of tandospirone free base, 50.1g of citric acid, add 1500ml of methanol, stir and heat up to reflux, slowly cool down to 0-20°C, keep stirring for 2 hours, filter, and wash the filter cake with methanol to obtain Citron Tandospirone wet product. Dry the wet product at 65°C for 15 hours to obtain tandospirone citrate with a yield of 88.1% and a purity of 99.89%. The XRPD is as follows: figure 1 , DSC such as figure 2 .

Embodiment 2

[0033] Embodiment 2 Preparation of stable crystalline form of tandospirone citrate

[0034] Weigh 100.0 g of tandospirone free base, 60.1 g of citric acid, add 1500 ml of methanol, stir at room temperature until the solid precipitates, then stir for 2 hours, filter, and wash the filter cake with methanol to obtain the wet product of tandospirone citrate . The wet product was dried at 65°C for 15 hours to obtain tandospirone citrate with a yield of 91.4% and a purity of 99.82%.

Embodiment 3

[0035] Embodiment 3 Preparation of stable crystalline form of tandospirone citrate

[0036] Weigh 100.0g of tandospirone free base, 60.1g of citric acid, add 1500ml of ethanol, stir and heat up to reflux, slowly cool down to 0-20°C, keep stirring for 2 hours, filter, and wash the filter cake with ethanol to obtain Citron Tandospirone wet product. The wet product was dried at 80°C for 10 hours to obtain tandospirone citrate with a yield of 95.8% and a purity of 99.87%. The XRPD was as follows: image 3 .

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Abstract

The invention discloses a tandospirone citrate stable crystal form and a preparation method thereof. According to the preparation method, a one-step salt forming method is adopted, recrystallization operation in an existing preparation method is avoided, the preparation process is simplified, and the cost is reduced. The prepared tandospirone citrate has the characteristics of single crystal form, good crystal form stability and stable quality.

Description

technical field [0001] The invention relates to the technical field of crystal forms of tandospirone citrate, in particular to a stable crystal form of tandospirone citrate and a preparation method thereof. Background technique [0002] Tandospirone was first developed by Sumitomo Pharmaceutical Co., Ltd., and was approved for marketing in Japan in 1996. Tandospirone belongs to the class of azapirone (azapirone) drugs, which is the third generation of anti-anxiety drugs. It acts on 5-HT receptors and selectively binds to 5-HT1A receptors in the brain. The limbic system such as the hippocampus and amygdala in the center, and the raphe nucleus that projects 5-HT nerves. The drug regulates the 5-HT projected from the raphe nucleus to the hippocampus by stimulating the 5-HT1A autoreceptor, inhibits the 5-HT effect of the action inhibition system, and exerts an anxiolytic effect. Its structural formula is as follows: [0003] [0004] Benzodiazepines (BDZ) drugs mainly act o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12
CPCC07D403/12C07B2200/13
Inventor 袁平东曾庆东全继平吕勇均王丹张金生罗利唐凤
Owner PKU HEALTHCARE CORP LTD
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