Vonoprazan fumarate new crystal form and preparation method thereof

Abstract

The invention discloses a vonoprazan fumarate new crystal form and a preparation method thereof. The preparation method comprises the following step: taking ethyl acetate, methanol and purified water as a mixed crystallizing solvent to obtain the vonoprazan fumarate new crystal form; and in a powder X-ray diffraction map of the vonoprazan fumarate new crystal form, characteristic peaks exist in positions where diffraction angles 2 theta are 12.18+ / - 0.5, 13.43+ / - 0.5, 22.35+ / - 0.5, 37.06+ / - 0.5 and 38.25+ / - 0.5. The vonoprazan fumarate new crystal form is good in stability; addition of medicine impurities can be avoided effectively; high costs caused by storage are reduced; and an effective guarantee is provided for safety of products and clinical effects.

Description

[0001] field of invention

[0002] The invention relates to the technical field of medicine, in particular to a new crystal form of vonoprazan fumarate and a preparation method thereof. Background technique

[0003] Vonoprazan fumarate (TAK-438), chemical name 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrol-3-yl ]-N-methylmethylamine monofumarate is a new type of potassium ion channel blocker developed by Takeda Pharmaceutical Company of Japan. It was launched in Japan in 2015 and is used for the treatment of non-erosive gastroesophageal reflux disease, Duodenal ulcer, gastric ulcer, erosive esophagitis, etc. The chemical structural formula is shown in (1).

[0004]

[0005] Vonoprazan fumarate inhibits basal gastric acid secretion in a concentration-dependent manner, ID 50 The value is 1.26 mg / kg. In animal experiments compared with lansoprazole, vonoprazan fumarate has a stronger inhibitory effect on gastric acid secretion, a faster increase in the pH value of...

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