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A new crystal form of safinamide methanesulfonate and its preparation method

A safinamide mesylate and safinamide technology are applied in the field of safinamide mesylate crystal form C and preparation thereof, and can solve the problems of affecting drug absorption, unsatisfactory formulation dissolution, and poor solubility Ideal and other issues, to achieve the effects of good solubility, high stability, and improved drug safety and effectiveness

Active Publication Date: 2018-04-17
CHENGDU BAIYU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the existing crystalline form of safinamide mesylate has unsatisfactory solubility in water, which not only affects the absorption of drugs in the human body, but is also extremely unfavorable to the development of pharmaceutical preparations, especially water-soluble preparations.
In order to solve the above problems, patent CN105017060 A discloses a crystal form B of safinamide mesylate crystal form, but the dissolution rate of the preparation prepared by this crystal form is not very ideal, and the drug effect cannot be effectively guaranteed

Method used

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  • A new crystal form of safinamide methanesulfonate and its preparation method
  • A new crystal form of safinamide methanesulfonate and its preparation method
  • A new crystal form of safinamide methanesulfonate and its preparation method

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Embodiment 1

[0030] Embodiment 1 Preparation of crystal form of the present invention

[0031] Add 9.0g of safinamide and 27mL of N,N-dimethylformamide to a 100mL three-necked flask in turn, stir and heat up to 60-70°C, stir to dissolve completely, add 3.0g of methanesulfonic acid dropwise, add 54mL of ethyl acetate, Cool down to 10-15°C, stir and crystallize for 2 hours, filter the precipitated solid, and dry under vacuum at 45-50°C to obtain 11 g of white solid with a purity of 99.95% and a yield of 91.7%.

Embodiment 2

[0032] Embodiment 2 Preparation of crystal form of the present invention

[0033] Add 9.0g of safinamide and 27mL of N,N-dimethylformamide to a 100mL three-necked flask in turn, stir to raise the temperature to 60-65°C, stir to dissolve completely, add 3.0g of methanesulfonic acid dropwise, add 54mL of ethyl acetate, Cool down to 10-15°C, stir and crystallize for 2 hours, filter the precipitated solid, and vacuum-dry at 45-50°C to obtain 11.1 g of white solid with a purity of 99.92% and a yield of 92.5%.

Embodiment 3

[0034] Embodiment 3 Preparation of crystal form of the present invention

[0035] Add 9.0g of safinamide and 27mL of N,N-dimethylformamide to a 100mL three-necked flask in turn, stir to raise the temperature to 40-45°C, stir to dissolve completely, add 3.0g of methanesulfonic acid dropwise, add 54mL of ethyl acetate, Cool down to 10-15°C, stir and crystallize for 2 hours, filter the precipitated solid, and dry under vacuum at 45-50°C to obtain 11.3 g of white solid with a purity of 99.91% and a yield of 94.2%.

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Abstract

The invention discloses a new crystal form of safinamide mesylate and a preparation method of the new crystal form. According to the new crystal form, the solubility and the stability of existing products are improved, preparation and utilization of the products are facilitated, and the safety and the effectiveness of a medicine are improved.

Description

technical field [0001] The invention relates to a new crystal form of safinamide mesylate, in particular to crystal form C of safinamide mesylate and a preparation method thereof. Background technique [0002] Safinamide methanesulfonate, the chemical name is (S)-2-[4-(3-fluorobenzyloxy)benzylamino]propionamide methanesulfonate, the English name is (S)-2-[[p -[(m-fluorobenzyl)oxy]benzyl]amino]propionamide monomethanesulfonate, its structural formula is as follows: [0003] [0004] Safinamide mesylate improves the function of dopamine by reversibly inhibiting the reuptake of monoamine oxidase B (MAO-B) and dopamine, inhibits the excessive release of glutamate, and is used for the treatment of Parkinson's disease. [0005] However, the existing crystal form of safinamide mesylate has unsatisfactory solubility in water, which not only affects the absorption of drugs in the human body, but is also extremely unfavorable to the development of pharmaceutical preparations, espe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C237/06C07C231/12C07C309/04C07C303/32A61K31/165
CPCC07B2200/13C07C231/12C07C237/06C07C303/32C07C309/04
Inventor 王波杨应朗张振国甘鹏龚胜威
Owner CHENGDU BAIYU PHARMA CO LTD