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Lafutidine crystal compound
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A lafutidine compound technology, applied in the field of lafutidine crystal compounds, can solve problems such as polymorphism
Active Publication Date: 2015-03-11
YOUCARE PHARMA GROUP
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Lafutidine may also have polymorphism
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Embodiment 1
[0031] Embodiment 1, the preparation of lafutidine crystal form compound
[0032] 1) Take 50g of crude lafutidine, add a mixed solvent of N,N-dimethylformamide / methanol, dissolve to obtain a solution, wherein the ratio of crude lafutidine to mixed solvent is 1g:12ml, mixed solvent The volume ratio of N,N-dimethylformamide to methanol is 3.5:1;
[0033] 2) Add 0.10 g of activated carbon to the solution obtained in step 1), stir for adsorption, filter for decarbonization and sterilization to obtain a clear solution, and reflux at 72°C for 3 hours;
[0034] 3) Then lower the temperature to 65°C, keep the temperature and add distilled water at 65°C dropwise under stirring at a rate of 28r / min, wherein the volume ratio of distilled water to the mixed solvent in step 1) is 5:1;
[0035] 4) Continue to keep stirring at 65° C. for 25 minutes at the above rate after dropping, then stop stirring, let stand and cool down to room temperature naturally, filter, wash with distilled water, ...
Embodiment 2-9
[0037] [Example 2-9] According to the parameters shown in Table 1, the lafutidine crystal compound was prepared
[0038] The following are embodiments 2-9 of the present invention, and the operation steps are the same as in embodiment 1, and the concrete process parameters are shown in Table 1:
[0039] Table 1, Embodiment 2-9
[0040]
[0041] The X-ray powder diffraction pattern obtained by measuring the lafutidine crystal form compound obtained in Examples 2-9 using Cu-Kα rays is similar to that in Example 1.
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Abstract
The invention belongs to the technical field of a medicine, and particularly relates to a lafutidine crystal compound shown in a formula (I). An X-ray powder diffraction spectrum obtained by using a Cu-K alpha ray is shown in a figure 1. The lafutidine crystal compound provided by the invention is a novel lafutidine crystal compound different from that in the prior art, the novel lafutidine crystal compound has improved solubility in water while the preparation prepared by adopting the novel lafutidine crystal compound disclosed by the invention has good bioavailability in comparison with the prior art.
Description
technical field [0001] The invention belongs to the technical field of medicines, in particular to a lafutidine crystal compound. Background technique [0002] Lafutidine is a new generation of long-acting, powerful H 2 Receptor antagonists, developed by Japanese Fuji and Dapeng pharmaceutical companies, were first launched in Japan in April 2000, and are mainly used for the treatment of gastric and duodenal ulcers and other related symptoms. Lafutidine is an off-white crystalline powder with a slight odor. The melting point is 96-99°C. Soluble in acetic acid, slightly soluble in methanol, slightly soluble in ethanol, very slightly soluble in ether, almost insoluble in water. Studies have shown that lafutidine can sustainably inhibit the basal secretion and nocturnal secretion of human gastric acid and pepsin, and the secretion caused by stimulating factors such as tetrapeptide gastrin, and effectively resist gastric mucosal damage caused by various gastric stimulating fa...
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