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Tandospirone hydrochloride crystal form II and preparation method thereof

A technology of tandospirone hydrochloride and tandospirone hydrochloride, applied in the field of tandospirone hydrochloride crystal form II and preparation thereof, can solve problems such as reports of tandospirone hydrochloride crystal form, and achieve water solubility and stability Good, simple preparation process, and the effect of improving bioavailability and safety

Active Publication Date: 2014-03-26
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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  • Tandospirone hydrochloride crystal form II and preparation method thereof
  • Tandospirone hydrochloride crystal form II and preparation method thereof
  • Tandospirone hydrochloride crystal form II and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation method of tandospirone hydrochloride crystal form II

[0038] Weigh 2 kg of tandospirone, add 16 L of a mixed solution of tetrahydrofuran and acetonitrile (volume ratio 90:10), heat up to 80 ° C, after the dissolution is complete, add 2.6 L of 2 mol / L hydrochloric acid aqueous solution, stop heating, and naturally Cool to room temperature and stand for 2 hours, then stand at -5±5°C for 12 hours, filter with suction, wash, and dry to obtain 2.07 kg of tandospirone hydrochloride crystal form II with a yield of 94.8%.

[0039] The measured melting point of tandospirone hydrochloride crystal form II is 225.5-226.5°C, and the X-ray powder diffraction pattern is shown in figure 1 (Using X’Pert Pro MPD Philips X-ray powder diffractometer to analyze the crystal phase of the sample, the radiation source Cu K α , graphite monochromator, tube voltage 40KV, tube current 35mA. ), the diffraction related data are shown in Table 1 (2θ measurement error is ±0.2)...

Embodiment 2

[0042] Example 2 Preparation method of tandospirone hydrochloride crystal form II

[0043] Weigh 2 kg of tandospirone, add 10 L of a mixed solution of tetrahydrofuran and acetonitrile (volume ratio 75:25), heat up to 60 °C, and after the dissolution is complete, add 3.9 L of 2 mol / L hydrochloric acid aqueous solution, stop heating, and naturally Cool to room temperature and stand for 5 hours, then stand at -5±5°C for 5 hours, filter with suction, wash and dry to obtain 2.05 kg of tandospirone hydrochloride crystal form II with a yield of 93.9%. The structural analysis results of the obtained product are not significantly different from those of Example 1.

Embodiment 3

[0044] Example 3 Preparation method of tandospirone hydrochloride crystal form II

[0045] Weigh 2 kg of tandospirone, add 30 L of a mixed solution of tetrahydrofuran and acetonitrile (volume ratio 50:50), heat up to 40 ° C, after the dissolution is complete, add 5 L of 2 mol / L hydrochloric acid aqueous solution, stop heating, and let it cool naturally Stand at room temperature for 3 hours, then place at -5±5°C for 8 hours, filter with suction, wash, and dry to obtain 2.03 kg of tandospirone hydrochloride Form II, with a yield of 92.9%. 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 tandospirone hydrochloride crystal form II. The characteristic absorption peaks exist at the diffraction angle 2*theta within 2.127-2.527 degrees, 16.078-16.478 degrees, 19.157-19.557 degrees, 19.321-19.721 degrees, 19.499-19.899 degrees, 22.561-22.961 degrees, 29.437-29.837 degrees and 35.530-35.930 degrees in the X-ray powder diffraction diagram of the crystal form II. The invention further provides a preparation method of the crystal form II. Compared with the conventional tandospirone hydrochloride product, the tandospirone hydrochloride crystal form II provided by the invention is more excellent in water solubility and stability, and provides the possibility of improving bioavailability and safety of drugs; in addition, the preparation technology of the crystal form II is simple, the yield of the crystal form II is high, and the preparation method is suitable for industrial production.

Description

technical field [0001] The invention relates to tandospirone hydrochloride crystal form II 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 anxiolytic drugs. 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...

Claims

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Application Information

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