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L-tandospirone tartrate 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: 2016-01-06
SICHUAN CREDIT PHARMA
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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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] The preparation of embodiment 1L-tandospirone tartrate

[0070] Weigh 2kg of tandospirone and 0.79kg of L-tartaric acid, add 10L of isopropanol, heat up to 90°C, after the solution is clear, continue to stir until the reaction is complete, stop heating, and concentrate to dryness under reduced pressure to obtain 2.77kg of L- Tandospirone tartrate, the yield is 99.5%, mass spectrometry shows its ESIm / z: 383 (M + ).

Embodiment 2

[0071] The preparation of embodiment 2L-tandospirone tartrate

[0072] L-tandospirone tartrate 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.

[0073] Table 1L - Preparation of Tandospirone Tartrate

[0074]

[0075] Note: The proportions of mixed solvents in the table are volume ratios.

Embodiment 3

[0076] Example 3L- Preparation of tandospirone tartrate compound crystal form I

[0077] Weigh 200gL-tandospirone tartrate, add 600mL isopropanol, heat up to 90°C, wait for complete dissolution, continue stirring for 30min, then stop heating, naturally cool to room temperature for 12 hours, filter with suction, wash, and dry to obtain 191g of white crystalline form I of tandospirone L-tartrate, the yield is 95.5%, mass spectrum shows its ESIm / z: 383 (M + ), the measured melting point is 146.5-149.0°C.

[0078] Adopt DX-2700 type X-ray powder diffractometer to analyze sample crystal phase, CuKα radiation, record the X-ray powder diffraction pattern of L-tandospirone tartrate crystal form I as follows figure 1 As shown, the main relevant diffraction data are shown in Table 2 (2θ measurement error is ±0.2).

[0079] Table 2L- X-ray powder diffraction data of tandospirone tartrate crystal form Ⅰ

[0080]

[0081]

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Abstract

The invention provides an L-tandospirone tartrate compound. The invention also provides a preparation method for the compound, a pharmaceutical composition and application. The L-tandospirone tartrate compound provided by the invention exists in a crystal form, has excellent water-solubility and stability, and provides possibility to improve bioavailability and safety of medicines; in addition, the compound provided by the invention has the advantages of simple preparation process, high yield, and applicability to industrial production.

Description

technical field [0001] The invention relates to an L-tandospirone compound of tartrate, in particular to a crystal form of the compound, a preparation method, a pharmaceutical composition and an application of the compound crystal. Background technique [0002] Tandospirone belongs to the class of azaspirone 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 sut...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12C07C59/255C07C51/41A61K31/506A61P25/22A61P25/24A61P25/18A61P25/28A61P27/06A61P27/02A61P25/20A61P25/00
CPCC07B2200/13C07D403/12
Inventor 傅霖邓丽敏陈刚
Owner SICHUAN CREDIT PHARMA
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