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L-tartaric acid tandospirone compound

A technology of tandospirone and tartaric acid, which is applied in the amorphous field, can solve the problems of drug quality and clinical efficacy differences, affect the stability of drug preparations, solubility, hygroscopicity, bioavailability, etc., achieve good water solubility, improve biological Utilization and safety, the effect of simple preparation process

Inactive Publication Date: 2017-01-25
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

[0046] The preparation of embodiment 1 L-tandospirone tartrate

[0047] Weigh 2kg of tandospirone and 0.79kg of L-tartaric acid, add 10L of isopropanol, heat up to 90°C, wait until 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 L-tandospirone tartrate, the yield is 99.5%, mass spectrometry shows its ESI m / z: 383 (M + ).

Embodiment 2

[0048] The preparation of embodiment 2 L-tandospirone tartrate

[0049] 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.

[0050] Table 1L - Preparation of Tandospirone Tartrate

[0051]

[0052]

[0053] Note: The proportions of mixed solvents in the table are volume ratios.

Embodiment 3

[0054] Example 3 Preparation of Amorphous L-Tartrate Tandospirone Compound

[0055] Weigh 200g of tandospirone L-tartrate, add 1000mL of ethanol, heat up to 80°C, wait for complete dissolution, continue to stir for 30min, then stop heating, naturally cool to room temperature for 2 hours, then place at -5±5°C for 4 hours , the supernatant was discarded, and the resulting white precipitate was concentrated under reduced pressure and dried to obtain 195g white powder amorphous L-tandospirone tartrate, the yield was 97.5%, and its ESI m / z was shown by mass spectrometry: 383 (M + ), and its melting point was measured to be 92.5-97.0°C.

[0056] Adopt DX-2700 type X-ray powder diffractometer to analyze sample crystal phase, Cu Kα radiation, record the X-ray powder diffraction pattern of amorphous L-tartrate tandospirone see figure 1 , which has no characteristic peaks in X-ray powder diffraction.

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Abstract

The invention provides an L-tartaric acid tandospirone compound. The invention further provides a preparation method, a pharmaceutical composition and application of the compound. The L-tartaric acid tandospirone compound provided by the invention exists in a crystal form, and is characterized in that the compound exists in an amorphous form and has no characteristic peaks in an X-ray powder diffraction pattern. The L-tartaric acid tandospirone compound provided by the invention has very good water solubility and stability and provides the possibility of improving the bioavailability and the safety of medicines; furthermore, the compound has a simple prepapration process and high yield and is suitable for industrial production.

Description

[0001] This application is a divisional application of China's invention patent application No. 201410249687.2. The filing date of this application is June 6, 2014. The invention name is an L-tandospirone tartrate compound. technical field [0002] The invention relates to an L-tandospirone compound of tartrate, in particular to the amorphous form of the compound, as well as the preparation method, pharmaceutical composition and application of the compound. Background technique [0003] 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: [0004] [0005] 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 ...

Claims

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Application Information

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