Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Tandospirone hydrochloride crystal form I and preparation method thereof

A technology of tandospirone hydrochloride and tandospirone, which is applied in the field of tandospirone hydrochloride crystal form I 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: 2015-10-21
SICHUAN CREDIT CHEMWERTH PHARMACEUTICAL CO LTD
View PDF8 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Tandospirone hydrochloride crystal form I and preparation method thereof
  • Tandospirone hydrochloride crystal form I and preparation method thereof
  • Tandospirone hydrochloride crystal form I and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
melting pointaaaaaaaaaa
melting pointaaaaaaaaaa
Login to View More

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 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com