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Stable bepotastine besilate crystal and preparation method thereof

A technology of besylate benzenesulfonate and benzenesulfonic acid, which is applied in the field of preparation of the new crystals, can solve problems such as the instability of raw materials, achieve superior stability, good fluidity and compressibility, and facilitate preparations

Active Publication Date: 2014-10-29
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, it is not a fundamental solution to solve the problem of instability of raw materials by optimizing the formulation

Method used

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  • Stable bepotastine besilate crystal and preparation method thereof
  • Stable bepotastine besilate crystal and preparation method thereof
  • Stable bepotastine besilate crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] The preparation of embodiment 1 bepotastine besilate crystal

[0059] Take 20 g of bepotastine besilate obtained in Comparative Example 1, add 40 g of ethanol, heat to dissolve, filter, cool the filtrate to 0-5°C, keep crystallization at this temperature until no solid precipitates, filter, wash, and dry , to obtain 14.4g of sandy crystals.

[0060] The X-powder diffraction data of gained crystal are shown in Table 1, and the diffraction pattern sees figure 1 .

[0061] The X-powder diffraction data of table 1 embodiment 1 gained bepotastine besilate crystals

[0062] 2θ angle

d value

2θ angle

d value

9.297

9.50534

28.372

3.14314

9.996

8.84159

28.863

3.09081

12.671

6.98074

31.094

2.87393

14.495

6.10585

32.581

2.74612

17.696

5.00791

33.820

2.64825

18.368

4.82635

35.871

2.50138

19.591

4.52773

36.779

2.44172

[00...

Embodiment 2

[0066] The preparation of embodiment 2 bepotastine besilate crystals

[0067] Take 200 g of bepotastine besilate obtained in Comparative Example 1, add 1500 g of isopropanol, heat to dissolve, cool the solution to 16-22° C., and keep at this temperature for crystallization. After no solid was precipitated, it was filtered, washed, and dried to obtain 162.0 g of sandy crystals.

[0068] The X-powder diffraction data are shown in Table 2, and the diffraction pattern is shown in Figure 4 .

[0069] The X-powder diffraction data of table 2 embodiment 2 gained bepotastine besylate crystals

[0070] 2θ angle

[0071] 2θ angle

Embodiment 3

[0072] The preparation of embodiment 3 bepotastine besilate crystals

[0073] Take 10 g of bepotastine besilate obtained in Comparative Example 1, add 100 g of n-propanol, heat to dissolve, cool the solution to 20-30° C., and keep at this temperature for crystallization. After no solid was precipitated, it was filtered, washed, and dried to obtain 7.8 g of sandy crystals.

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Abstract

The invention discloses a stable bepotastine besilate crystal in novel crystal form through a recrystallization method. The obtained bepotastine besilate crystal is confirmed through X-ray powder diffraction and infrared spectrum. Stability contrast experiments prove that the provided bepotastine besilate crystal has extremely high stability, and both bulk drug and preparation of the bepotastine besilate crystal have stability obviously better than that of existing bepotastine besilate crystals.

Description

technical field [0001] The invention relates to a new crystal of the drug bepotastine besilate, and also relates to a preparation method and application of the new crystal. Background technique [0002] Bepotastine besilate is the benzenesulfonate of bepotastine, a drug with antihistamine activity, which can be used in the treatment of allergic diseases such as rhinitis, as well as eczema, dermatitis, prurigo, itchy skin, urticaria and other skin diseases. [0003] Bepotastine besilate is a crystal at room temperature. There is a chiral carbon in the molecule of bepotastine besilate compound, and the chiral compound with pharmaceutical activity is the S configuration. However, the bepotastine besylate crystal prepared by the method in the prior art has poor stability and is prone to produce R-isomer impurities, thereby affecting the curative effect of the drug. [0004] [0005] Bepotastine Besilate [0006] CN1098262C is a patent for the preparation of bepotastine be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07C309/29C07C303/44A61K31/4545A61P37/08A61P17/00
CPCC07D401/12
Inventor 张波赵舟邹长忠毛启良
Owner CHONGQING HUAPONT PHARMA
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