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Rabeprazole sodium crystal compound and preparing method thereof

A technology for rabeprazole sodium and crystalline compounds, applied in the field of rabeprazole sodium crystalline compounds and their preparation, can solve the problems of low binding strength, difference in solubility of crystalline drugs, large free energy per unit surface and the like, and achieve quality assurance , good stability effect

Active Publication Date: 2012-07-18
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compounds with different crystal structures are in different energy states due to the difference in molecular arrangement order. Generally, amorphous drugs have greater potential energy, and the bonding strength between particles is smaller than that of crystal forms. The total unit surface free The energy is large, and the surface between the particles is easy to hydrate, resulting in a difference in solubility from that of crystalline drugs

Method used

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  • Rabeprazole sodium crystal compound and preparing method thereof
  • Rabeprazole sodium crystal compound and preparing method thereof
  • Rabeprazole sodium crystal compound and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] [Example 1] Preparation of Rabeprazole Sodium Crystal Compound

[0038] 1) Add 60 g of the raw material drug rabeprazole sodium to 300 ml of water, stir and dissolve to obtain an aqueous solution of rabeprazole sodium;

[0039] 2) Add 480ml of a mixed solution of tetrahydrofuran and methanol (the volume ratio of tetrahydrofuran to methanol is 3:1) to the above aqueous solution of rabeprazole sodium under stirring at a speed of 300r / min. The activated carbon is kept decolorized at 25°C and filtered. Get filtrate

[0040] 3) The filtrate was dropped into 1440 ml of acetonitrile, cooled to 5° C., crystals were precipitated, filtered, and dried in vacuum to obtain 54.1 g of white rabeprazole sodium crystalline compound.

[0041] The melting point of the crystalline compound is 162-163°C detected by capillary method.

[0042] Using the PE 2400II elemental analyzer from Perkin-Elmer, USA, the elemental analysis (%) is: actual measured value (calculated value), C: 56.68 (56.68), H: 5.2...

Embodiment 2-9

[0046]

[0047] The melting point of the crystalline compound obtained in Examples 2-9 was detected by capillary method to be 162-163° C., and elemental analysis was performed with the PE2400II elemental analyzer of Perkin-Elmer Company, USA. The result was similar to that of Example 1.

[0048] At the same time, the crystalline compounds of Examples 2-9 were measured by powder X-ray diffraction measurement, and the X-ray powder diffraction pattern represented by the diffraction angle of 2θ±0.2° was similar to that of Example 1.

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Abstract

The invention relates to a rabeprazole sodium crystal compound and a preparing method thereof. The crystal compound is determined by a powder X-ray diffraction determining method, and an X-ray powder diffraction spectrum represented by 2 theta + / - 0.2 degree diffraction angles shows characteristic diffraction peaks at the positions of 5.8 degrees, 7.5 degrees, 12.1 degrees, 12.8 degrees, 13.3 degrees, 15.6 degrees, 16.7 degrees, 18.3 degrees, 20.4 degrees, 25.7 degrees, 26.8 degrees and 31.5 degrees. The preparing method comprises the following steps of: 1) adding rabeprazole sodium serving as a crude drug in water, stirring and dissolving to obtain a rabeprazole sodium water solution; 2) adding a mixed solution of tetrahydrofuran and methanol into the rabeprazole sodium water solution, conducting heat-insulation decoloration at the temperature of 25-35 DEG C by active carbon and filtering to obtain filtrate; and 3) dropping the filtrate into acetonitrile, cooling, crystallizing, filtering and drying in vacuum, thus obtaining the rabeprazole sodium crystal compound. The crystal compound has good stability and strong inhibitory action on Helicobacter pylori.

Description

Technical field [0001] The invention relates to a rabeprazole sodium crystal compound and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Rabeprazole sodium, its chemical name is: 2-{[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methanesulfinyl}-1H-benzimidazole sodium , Molecular formula: C 18 H 20 N 3 NaO 3 S, molecular weight: 381.43, structural formula: [0003] [0004] Rabeprazole sodium is a benzimidazole compound. It is a second-generation proton pump inhibitor that specifically inhibits parietal cells H + , K + -ATPase system to block the last step of gastric acid secretion. The effect is dose-dependent, and can inhibit both basal gastric acid secretion and gastric acid secretion under stimulation. This product is for cholic acid and histamine H 2 The receptor has no resistance. [0005] The salt formation of rabeprazole sodium, patent literature reports all use rabeprazole and sodium hydroxide aqueous solution reac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 郭中明李明华张明法
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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