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Hydrochloric tandospirone crystal form I and preparation method of crystal form I

A technology for tandospirone hydrochloride and tandospirone hydrochloride, applied in the field of tandospirone hydrochloride crystal form I and its preparation, can solve problems such as reports of tandospirone hydrochloride crystal form, and achieve water solubility and stability Good, high yield, improved bioavailability and safety

Active Publication Date: 2014-04-30
SICHUAN CREDIT CHEMWERTH PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there are patents disclosing the preparation method of tandospirone hydrochloride, such as patent CN101880274A, US4507303, but there is no report about the crystal form of tandospirone hydrochloride

Method used

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  • Hydrochloric tandospirone crystal form I and preparation method of crystal form I
  • Hydrochloric tandospirone crystal form I and preparation method of crystal form I
  • Hydrochloric tandospirone crystal form I and preparation method of crystal form I

Examples

Experimental program
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Embodiment 1

[0040] Embodiment 1 Preparation method of tandospirone hydrochloride crystal form I

[0041]Weigh 500g of tandospirone, add 12.5L of a mixed solution of acetone and ether (40:60 in volume ratio), heat up to 40°C, and after the dissolution is complete, slowly add 0.13L of 10mol / L aqueous hydrochloric acid solution dropwise, drop Stop heating after finishing, let cool to room temperature naturally for 12 hours, filter with suction, wash, and dry to obtain 519 g of tandospirone hydrochloride crystal form I with a yield of 95.0%.

[0042] The measured melting point of tandospirone hydrochloride crystal form I is 224.0-225.0°C, and the X-ray powder diffraction pattern is shown in figure 1 (Using DX-2700 X-ray powder diffractometer to analyze the crystal phase of the sample, Cu Kα radiation, tube voltage 40KV, tube current 30mA), the relevant diffraction data are shown in Table 1 (2θ measurement error is ±0.2), and the infrared spectrum is shown in Figure 4 .

[0043] Table 1 X-r...

Embodiment 2

[0045] Embodiment 2 The preparation method of tandospirone hydrochloride crystal form I

[0046] Weigh 500g of tandospirone, add 8.0L of a mixed solution of acetone and ether (65:35 in volume ratio), heat up to 50°C, after the dissolution is complete, add 0.2L of 10mol / L aqueous hydrochloric acid solution dropwise, Afterwards, stop heating, cool naturally to room temperature for 2 hours, then place at -5±5°C for 8 hours, filter with suction, wash, and dry to obtain 513 g of tandospirone hydrochloride Form I, with a yield of 94.0%. The structural analysis results of the obtained product are not significantly different from those of Example 1.

Embodiment 3

[0047] Embodiment 3 Preparation method of tandospirone hydrochloride crystal form I

[0048] Weigh 500g of tandospirone, add 5.0L of a mixed solution of acetone and ether (80:20 by volume), heat up to 30°C, and after the dissolution is complete, add 0.26L of 10mol / L aqueous hydrochloric acid solution dropwise, Afterwards, stop heating, cool naturally to room temperature for 6 hours, then place at -5±5°C for 5 hours, filter with suction, wash, and dry to obtain 516 g of tandospirone hydrochloride crystal form I with a yield of 94.5%. The structural analysis results of the obtained product are not significantly different from those of Example 1.

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Abstract

The invention provides a hydrochloric tandospirone crystal form I. The hydrochloric tandospirone crystal form I is characterized in that an X-ray powder diffraction pattern of the crystal form I shows that characteristic absorption peaks appear at 2 theta diffraction angles of 6.597+ / -0.2, 10.352+ / -0.2, 12.676+ / -0.2, 15.362+ / -0.2, 15.922+ / -0.2, 17.122+ / -0.2, 18.752+ / -0.2, and 25.522+ / -0.2 degrees. The invention also provides a preparation method of the crystal form I. Compared with the existing hydrochloric tandospirone product, the hydrochloric tandospirone crystal form I, provided by the invention, has the advantages that the water solubility and the stability are improved, and the bioavailability and the safety of a drug can be improved; in addition, the crystal form is simple in preparation process, high in yield, and suitable for industrial production.

Description

technical field [0001] The invention relates to tandospirone hydrochloride crystal form I 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. It is a 5-HT receptor agonist and belongs to the third generation of anxiolytics. Its mechanism of action is to highly selectively interact with 5-HT that is concentrated in the hippocampus, septum, interpeduncular nucleus, amygdala and other brain limbic systems in the emotional center, as well as the suture gland nucleus. 1A Receptor binding, stimulant 5-HT 1A Autoreceptors, play an anxiolytic effect. [0003] Because tandospirone acts on 5-HT 1A The receptor is highly selective, so its drug safety is high, there are basically no adverse reactions such as sedation, sleep induction, convulsions, etc., and there is no muscle relaxation effect and dependence effect. Ketone and similar derivatives buspi...

Claims

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Application Information

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IPC IPC(8): C07D403/12A61K31/506A61P25/24A61P25/22A61P25/20A61P25/18A61P25/28A61P25/00A61P27/06A61P9/10A61P27/02
CPCC07D403/12
Inventor 傅霖邓丽敏李文婕陈刚
Owner SICHUAN CREDIT CHEMWERTH PHARMACEUTICAL CO LTD
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