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

Tandospirone oxalate compound

A technology of tandospirone and its compound, which is applied in the field of crystal preparation of the compound, can solve problems affecting the stability of pharmaceutical preparations, solubility, hygroscopicity, bioavailability, drug quality, and differences in clinical drug efficacy, etc.

Inactive Publication Date: 2015-12-23
SICHUAN CREDIT PHARMA
View PDF10 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And different crystal forms may have different colors, melting points, stability, apparent solubility, dissolution rate, etc. These properties will directly affect the stability, solubility, hygroscopicity, bioavailability, etc. of pharmaceutical preparations, and resulting in differences in drug quality and clinical efficacy

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 oxalate compound
  • Tandospirone oxalate compound
  • Tandospirone oxalate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] The preparation of embodiment 1 tandospirone oxalate

[0122] Weigh 0.66kg of oxalic acid and dissolve it in 2L of isopropanol to form an isopropanol solution of oxalic acid. Weigh 2kg of tandospirone, add 10L of isopropanol, heat up to 90°C, after the solution is clear, add the prepared isopropanol oxalate solution, continue to stir until the reaction is complete, stop heating, naturally cool to room temperature for 2 hour, suction filtration, washing, drying, namely get 2.42kg tandospirone oxalate, yield is 98.0%, mass spectrum shows its ESIm / z: 383 (M + ).

Embodiment 2

[0123] The preparation of embodiment 2 tandospirone oxalate

[0124] Tandospirone oxalate was prepared according to the method of Example 1, see Table 1 for specific conditions, and the feeding amount of tandospirone was 2 kg. There is no significant difference between the structural analysis results of the product obtained under each condition and the structural analysis results of Example 1.

[0125] The preparation of table 1 tandospirone oxalate

[0126]

[0127]

[0128] Note: The proportions of mixed solvents in the table are volume ratios.

Embodiment 3

[0129] Example 3 Preparation of tandospirone oxalate compound crystal form I

[0130] Weigh 200g of tandospirone oxalate, add 1000mL of isopropanol, heat up to 90°C, wait for complete dissolution, continue stirring for 30min, then stop heating, naturally cool to room temperature for 2 hours, filter with suction, wash, and dry to obtain 197g White powder tandospirone oxalate crystal form I, the yield is 98.5%, mass spectrum shows its ESIm / z: 383 (M + ), and its melting point was measured to be 162.0-163.0°C.

[0131] Using DX-2700 X-ray powder diffractometer to analyze the crystal phase of the sample, and CuKα radiation, the X-ray powder diffraction pattern of tandospirone oxalate crystal form I is obtained. figure 1 , and its main relevant diffraction data are shown in Table 2 (2θ measurement error is ±0.2).

[0132] Table 2 X-ray powder diffraction data of tandospirone oxalate crystal form Ⅰ

[0133]

[0134]

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 tandospirone oxalate compound. The invention also provides a preparation method of the tandospirone oxalate compound, a pharmaceutical composition containing the compound and a use of the compound. The tandospirone oxalate compound provided by the invention exists in a form of crystals, has stable properties and good solubility in water, and provides an effective solution way for improving the drug bioavailability and safety; and in addition, the preparation process of the compound is simple, high in yield, and suitable for industrialized production.

Description

technical field [0001] The invention relates to a tandospirone oxalate compound, in particular to the crystal form of the compound, as well as the preparation method, pharmaceutical composition and application of the compound crystal. Background technique [0002] Tandospirone belongs to the azaspirone class of drugs, the chemical name is (3aα,4β,7β,7aα)-hexahydro-2-[4[4-(2-pyrimidinyl)-1-(piperazinyl)- Butyl]-4,7-methylene-1H-isoindole-1,3(2H)-dione, the molecular structure is as follows: [0003] [0004] Tandospirone was first developed by Sumitomo Pharmaceutical Co., Ltd., and was approved for marketing in Japan in 1996. It is a serotonin receptor agonist and belongs to the third generation of anxiolytic drugs, mainly used for the treatment of anxiety or other diseases accompanied by anxiety state. In the brain, it can be concentrated in the emotional center of the hippocampus, septum, interpeduncular nucleus, amygdala and other brain limbic systems and 5-HT in the ...

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 Applications(China)
IPC IPC(8): C07D403/12C07C55/06C07C51/41A61K31/506A61P25/22A61P25/24A61P25/20A61P25/18A61P25/00A61P25/28A61P27/02A61P27/06A61P3/10A61P9/10
CPCC07B2200/13C07D403/12
Inventor 傅霖邓丽敏陈刚
Owner SICHUAN CREDIT PHARMA
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