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Tandospirone citrate compound

A technology of tandospirone citrate and tandospirone, which is applied in the field of preparation of the compound crystals, can solve the problems of less research on the crystal form of tandospirone citrate, unsatisfactory dissolution rate of preparations, and ineffectiveness. Ensure the effect of medication and other issues, to achieve the effect of ensuring the effect of medication, good dissolution effect, and improving bioavailability and safety

Inactive Publication Date: 2016-10-05
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For example, US4507303, US4818756, JP60087262, CN101362751B, etc. disclose the preparation methods of tandospirone and tandospirone citrate respectively, but there are few studies on the crystal form of tandospirone citrate, and existing The dissolution rate of the preparation made of the tandospirone citrate crystal form is not particularly ideal, and the drug effect cannot be effectively guaranteed

Method used

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  • Tandospirone citrate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of Crystal Form IV of Tandospirone Citrate Compound

[0036] Get 41g citric acid and dissolve in 300mL acetone to make the acetone solution of citric acid. Weigh 80g tandospirone, add a mixed solution of 600mL acetone and 300mL ether, dissolve, add dropwise the prepared acetone citrate solution, heat and stir until the reaction is complete, naturally cool to room temperature and let stand for 6h, suction filter, wash , and dried under reduced pressure to obtain 118.8 g of white powdery tandospirone citrate crystal form IV, with a yield of 99.0%. Mass spectrum showed its ESI m / z: 383.

[0037] The melting point of tandospirone citrate crystal form IV was measured to be 165.5-166.5°C. Using Cu Kα radiation, the X-ray powder diffraction pattern of tandospirone citrate crystal form IV is measured in figure 1 , and its main relevant diffraction data are shown in Table 1 (2θ measurement error is ±0.2).

[0038] Table 1 X-ray powder diffraction data o...

Embodiment 2

[0040] Example 2 Preparation of tandospirone citrate compound crystal form IV

[0041] Get 40.1g of citric acid and dissolve in 250mL of acetone to make the acetone solution of citric acid. Weigh 80g of tandospirone, add 500mL of acetone and 50mL of diethyl ether mixed solution, wait until it is completely dissolved, add dropwise the prepared citric acid acetone solution, stir at 35°C until the reaction is complete, stop heating, and cool to room temperature naturally Stand still for 16 hours, filter with suction, wash, and dry under reduced pressure to obtain 118.6 g of white powdery crystal form IV of tandospirone citrate, with a yield of 98.8%. The structural analysis results and X-ray powder diffraction patterns of the obtained product are not significantly different from those in Example 1.

Embodiment 3

[0042] Example 3 Preparation of Crystal Form IV of Tandospirone Citrate Compound

[0043] Get 60.2g of citric acid and dissolve in 500mL of acetone to make the acetone solution of citric acid. Weigh 80g of tandospirone, add 1900mL of acetone and 400mL of diethyl ether mixed solution, until it is completely dissolved, add the prepared acetone citrate solution dropwise, stir at 40°C until the reaction is complete, stop heating, and cool to room temperature naturally Stand still for 2 hours, filter with suction, wash, and dry under reduced pressure to obtain 118.2 g of tandospirone citrate crystal form IV in the form of white powder, with a yield of 98.5%. The structural analysis results and X-ray powder diffraction patterns of the obtained product are not significantly different from those in Example 1.

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Abstract

The invention provides a tandospirone citrate compound and further provides a preparation method, pharmaceutical composition and application of the tandospirone citrate compound. The tandospirone citrate compound exists in the form of crystals and is stable in property and high in purity, water solubility is obviously improved compared with an existing product, and an effective solving way is provided for improving the bioavailability and safety of medicine. A preparation prepared from the tandospirone citrate compound is good in dissolving effect, the medicine application effect can be guaranteed, and the tandospirone citrate compound is suitable for medicine use. In addition, the compound is simple in preparation process, high in yield and suitable for industrial production.

Description

technical field [0001] The invention relates to a tandospirone citrate 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 formula is as follows. In clinical treatment, the citrate salt of tandospirone (i.e. tandospirone citrate) is often used, and its molecular structural formula 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 bra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12A61K31/506A61P25/22
Inventor 邓丽敏李晓莉李文婕陈刚
Owner SICHUAN CREDIT PHARMA
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