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5-hydroxytryptamine receptor agonist

A solvent and tandospirone acid technology, applied in the field of tandospirone compounds, can solve the problems affecting the stability of pharmaceutical preparations, solubility, hygroscopicity, bioavailability, drug quality and clinical efficacy differences, etc., and achieve water solubility. Good effect, improved safety and efficacy, simple preparation process

Active Publication Date: 2017-06-06
SICHUAN CREDIT PHARMA +1
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  • 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

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  • 5-hydroxytryptamine receptor agonist
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  • 5-hydroxytryptamine receptor agonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The preparation of embodiment 1 tandospirone maleate

[0044] Weigh 1 kg of tandospirone and 303 g of maleic acid, add 6L of ethanol, heat to solvent reflux, stir until the reaction is complete, stop heating, naturally cool to room temperature, filter and collect the solid, and dry to obtain 1.30 kg of tandospirone maleate Duspirone, the yield is 99.8%, mass spectrometry shows its ESI m / z: 383 (M + ).

Embodiment 2

[0045] The preparation of embodiment 2 tandospirone maleate

[0046] Tandospirone maleate was prepared according to the method of Example 1, see Table 1 for specific conditions, and the feeding amount of tandospirone was 1 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.

[0047] Table 1, the preparation condition of tandospirone maleate

[0048]

[0049]

[0050] The ratios of mixed solvents in the table are volume ratios.

Embodiment 3

[0051] Example 3 Preparation of Tandospirone Maleate Form II

[0052] Take 200g of tandospirone maleate, add 900mL of acetonitrile and 300mL of water, heat to solvent reflux, stir until completely dissolved, stop heating, naturally cool to room temperature for crystallization, collect crystals by filtration, and dry to obtain 193g of white powdered horseradish. The yield of tandospirone crystalline form II was 96.5%, and its ESI m / z was shown by mass spectrometry: 383 (M + ), the measured melting point is 159.0-160.5°C.

[0053] Adopt Cu Kα radiation, measure the X-ray powder diffraction result of tandospirone maleate crystal form II of the present invention as follows figure 1 The relevant diffraction data are shown in Table 2.

[0054] Table 2. X-powder diffraction results of crystal form II

[0055]

[0056]

[0057] Among them, the main relevant diffraction data of relative intensity I%≥5% are shown in Table 3.

[0058] Table 3, X-ray powder diffraction results o...

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Abstract

The invention provides a 5-hydroxytryptamine receptor agonist. Particularly, provided is a tandospirone maleate compound. The invention also provides a preparation method of the compound, and a pharmaceutical composition containing the compound and a use of the compound. The tandospirone maleate provided by the invention exists in a crystal form, has stable properties and good water solubility, has the bioavailability significantly improved, and provides an effective solving way for improving the safety and effectiveness of drugs; in addition, the compound is simple in preparation technology, high in yield and suitable for industrialized production.

Description

[0001] This application is a divisional application of China's invention patent application No. 201510835073.7, the filing date of which is November 25, 2015, and the title of the invention is a serotonin receptor agonist. technical field [0002] The invention relates to a tandospirone compound, mainly relates to a maleate salt of tandospirone, specifically relates to a crystal form of the compound, a preparation method, a pharmaceutical composition and an application of the compound crystal. Background technique [0003] The chemical name of tandospirone is (3aα,4β,7β,7aα)-hexahydro-2-[4[4-(2-pyrimidinyl)-1-(piperazinyl)-butyl]-4,7 -Methylene-1H-isoindole-1,3(2H)-dione, which belongs to the azaspirone class of drugs, was first developed by Sumitomo Pharmaceutical Co., Ltd., and was approved for marketing in Japan in 1996. Tandospirone is a third-generation anti-anxiety drug, mainly used to treat anxiety or other diseases accompanied by anxiety. Different from traditional ...

Claims

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Application Information

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IPC IPC(8): C07D403/12A61K31/506A61P25/00A61P27/02A61P25/22A61P25/24A61P25/18A61P25/28A61P25/20A61P3/04A61P25/32A61P15/00A61P13/00A61P29/00A61P25/16A61P25/08A61P27/06A61P3/10A61P7/10
CPCC07B2200/13C07D403/12
Inventor 邓丽敏陈刚宿磊蒋春霞鲍文娟邓锐
Owner SICHUAN CREDIT PHARMA
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