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Tandospirone hydrochloride crystal form II and preparation method thereof

A technology of tandospirone hydrochloride and tandospirone, which is applied in the field of tandospirone hydrochloride crystal form II and its preparation, can solve problems such as the report of tandospirone hydrochloride crystal form, and achieve water solubility and stability Good, high yield, enhanced bioavailability and safety effects

Active Publication Date: 2015-10-14
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 2kg of tandospirone, add 16L of a mixed solution of tetrahydrofuran and acetonitrile (volume ratio is 90:10), heat to 80℃, after the dissolution is complete, add 2.6L of 2mol / L hydrochloric acid aqueous solution, stop heating, naturally It was cooled to room temperature and placed for 2 hours, then placed at -5±5°C for 12 hours, filtered with suction, washed, and dried to obtain 2.07 kg of Tandospirone hydrochloride crystal form II with a yield of 94.8%.

[0039] The melting point of Tandospirone Hydrochloride Form II was measured to be 225.5~226.5℃. 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 is shown in Table 1 (2θ measurement error is ±0.2), and th...

Embodiment 2

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

[0043] Weigh 2kg of tandospirone, add 10L of a mixed solution of tetrahydrofuran and acetonitrile (75:25 by volume), heat to 60°C, after the dissolution is complete, add 3.9L of 2mol / L hydrochloric acid aqueous solution, stop heating, naturally It was cooled to room temperature and placed for 5 hours, and then placed at -5±5°C for 5 hours, filtered with suction, washed, and dried to obtain 2.05 kg of tandospirone hydrochloride form II, with a yield of 93.9%. There is no significant difference between the structure analysis result of the obtained product and the structure analysis result of Example 1.

Embodiment 3

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

[0045] Weigh 2kg of tandospirone, add 30L of tetrahydrofuran and acetonitrile mixed solution (volume ratio is 50:50), heat to 40℃, after the dissolution is complete, add 5L of 2mol / L hydrochloric acid aqueous solution, stop heating, let cool naturally Place it at room temperature for 3 hours, then place it 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%. There is no significant difference between the structure analysis result of the obtained product and the structure analysis result 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 Japan's Sumitomo Pharmaceutical Co., Ltd. and was approved for listing in Japan in 1996. It is a 5-HT receptor agonist and belongs to the third generation of anxiolytics. The mechanism of action is the highly selective and concentrated distribution of 5-HT in the limbic system of the brain such as the hippocampus, septum, interpodal nucleus, amygdala, and the nucleus of the raphe nucleus in the emotional center. 1A Receptor binding, agonizing 5-HT 1A Autoreceptors play an anti-anxiety effect. [0003] Since Tandospirone acts on 5-HT 1A It is highly selective when used as a receptor, so it has high drug safety, basically no adverse reactions such as sedation, sleep induction, convulsions, etc., and no muscle relaxation and dependence effects. Moreover, it is compared with the original drug Azas...

Claims

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Application Information

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Patent Type & Authority Patents(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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