Brivaracetam crystal as well as preparation method and application thereof

A brivaracetam and crystal technology, which is applied to brivaracetam crystals and their preparation and application fields, can solve problems such as difficulty in overcoming weight deviation and tableting obstacles, and achieve the improvement of powder flow performance and sieving performance, and the reduction of Small proportion, not easy to fine particle effect

Pending Publication Date: 2020-11-17
ZHEJIANG JINGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the above two reasons, it is difficult for Brivaracetam to overcome tableting obstacles such as weight deviation and mold sticking in mass production

Method used

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  • Brivaracetam crystal as well as preparation method and application thereof
  • Brivaracetam crystal as well as preparation method and application thereof
  • Brivaracetam crystal as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Add 1000g of brivaracetam into 650ml of acetone, heat to 50°C and stir until dissolved, then cool down at 1-2°C / min for crystallization, after cooling down to 5-15°C, filter with suction, and drum the wet product at 40°C Air-dried to obtain brivaracetam crystals.

[0116] Observe the crystal form after suction filtration and drying with a microscope, as shown in Figure 14 As shown, the length: width ratio is in the range of 1:1 to 2:1, and the width: height ratio is in the range of 1:1 to 2:1.

[0117] The powder X-ray diffraction pattern of formed buvaracetam crystal is as follows figure 2 As shown, its powder X-ray diffraction data are shown in Table 7. The powder X-ray diffraction data shows that it is consistent with the crystal form of Comparative Example 1 and Comparative Example 2, and is consistent with the single crystal diffraction simulation at room temperature Figure 1 Sincerely. Its DSC diagram is as follows image 3 As shown, it shows that the melt...

Embodiment 2

[0122] Add 6000g of brivaracetam into 4000ml of acetone, heat to 50°C and stir until dissolved, then cool down at 1-2°C / min for crystallization, after cooling down to 5-15°C, filter with suction, and drum the wet product at 40°C Air-dried to obtain brivaracetam crystals.

[0123] Observe the crystal form after suction filtration and drying with a microscope, as shown in Figure 15 As shown, the length: width ratio is in the range of 1:1 to 2:1, and the width: height ratio is in the range of 1:1 to 2:1.

Embodiment 3

[0125] Add 1000g of brivaracetam into 1500ml of acetone, heat to 50°C and stir until dissolved, then cool down at 1-2°C / min for crystallization, after cooling down to 5-15°C, filter with suction, and drum the wet product at 40°C Air-dried to obtain brivaracetam crystals.

[0126] Observe the crystal form after suction filtration and drying with a microscope, as shown in Figure 16 As shown, the length: width ratio is in the range of 1:1 to 2:1, and the width: height ratio is in the range of 1:1 to 2:1.

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Abstract

The invention discloses a brivaracetam crystal as well as a preparation method and application thereof. A ratio of the length to the width of the crystal is about 1: 1 to about 3: 1, and a ratio of the width to the height of the crystal is about 1: 1 to about 3: 1. The brivaracetam crystal provided by the invention has crystal habit different from the crystal habit of conventional brivaracetam crystals, reduces the 001 crystal face with remarkable thermal expansion, is not easy to break and good in flowability, has remarkable advantages in operations such as sieving, mixing and the like in a preparation process, and can also remarkably reduce tabletting obstacles such as sticking and mass deviation. According to the preparation method of the brivaracetam crystal, the pure brivaracetam crystal form can be obtained, the brivaracetam crystal is uniformly separated out in the crystallization process, stirring is smooth, substance purification is facilitated, and the preparation method is suitable for industrial production.

Description

technical field [0001] The invention relates to a buvaracetam crystal, a preparation method and application thereof. Background technique [0002] Brivaracetam (or Briracetam), chemical name is (S)-2-[(4R)-2-oxo-4-propylpyrrolidin-1-yl)butanamide, its structure is as follows I show. [0003] [0004] Belgian UCB Company disclosed this compound (No. 159) and its preparation method in the patent WO2001 / 062726A2 for the treatment of neurological diseases such as epilepsy. The compound 159 is marketed under the drug name of "Briviact". [0005] Patent WO2001 / 062726 pointed out that two solid forms of 159 were observed, revealing that there were two crystal forms of brivaracetam. Herein, form A is referred to as crystal form I, and form B is referred to as crystal form II. The identification of the two crystal forms of Buvaracetam can be realized by powder X-ray diffraction method, wherein Couvrat et al. pointed out that the crystal form I is a thermodynamically stable anhyd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/27A61K31/4015A61P25/08
CPCC07D207/27A61K31/4015A61P25/08C07B2200/13
Inventor 周新波朱建荣沈宇飞黄生军王凯源唐飞宇
Owner ZHEJIANG JINGXIN PHARMA
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