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Rabeprazole sodium compound

A technology of rabeprazole sodium and hydrate, which is applied in digestive system, organic chemistry, drug combination and other directions, can solve the problems of difficult product purification, high impurities, moisture absorption and weight gain, etc.

Active Publication Date: 2014-05-07
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] It is difficult to purify the product of the above-mentioned rabeprazole method. Rabeprazole is made into its sodium salt, which can effectively reduce impurities and purify the product, but the impurities are still relatively high, and there is also a certain amount of moisture absorption and weight gain.

Method used

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  • Rabeprazole sodium compound
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  • Rabeprazole sodium compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] In a 5l reaction kettle equipped with stirring, thermometer, and condenser, add 240 grams of rabeprazole sodium, 970.0ml isopropanol, 16.5ml piperidine, and 980.0ml water, start stirring, heat to dissolve, and the filtrate is naturally cooled to 30°C-32°C, then let it stand for 4 hours, precipitated crystals, filtered, and dried indoors to obtain 230.6 grams of white crystals of rabeprazole sodium sesquihydrate, with a melting point of 122.3°C-123.2°C. The content is 99.76%, and the single impurity is less than 0.06%. Determined by Karl Fischer method, it contains 6.57% (weight percent) of water.

[0056] The X-ray diffraction pattern of the crystal is shown in figure 1 . Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50 ° .

[0057] Microparticles or microspheres are prepared by combining the compounds of the present invention with a pharmaceutically acceptable solid or liquid carrier, and optio...

Embodiment 2

[0059] Tablets containing rabeprazole sodium sesquihydrate

[0060] Prescription: Rabeprazole sodium sesquihydrate 10.7g, microcrystalline cellulose 12g, pregelatinized starch 16g, sodium starch glycolate 5g, lactose 210g, PEG-4000 25g, magnesium stearate 6g , 30 grams of povidone K30, 33 grams of croscarmellose sodium, appropriate amount of distilled water, made into 10,000 tablets.

[0061] Process:

[0062] Preparation of tablet core: according to the determined prescription, the main ingredient and auxiliary materials are mixed uniformly, granulated, and the granules are ventilated and dried below 40°C, granulated with a 16 mesh sieve, added magnesium stearate and remaining starch, and compressed into tablets to obtain final product .

[0063] Isolation layer coating: add talcum powder to 5% polyvinylpyrrolidone (PVP) absolute ethanol solution, stir evenly, and prepare a 20% suspension as the isolation layer coating solution. Coating is carried out in a fluidized bed, a...

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to a rabeprazole sodium sesquihydrate and a preparation method thereof. The rabeprazole sodium sesquihydrate prepared by the invention contains a hemicrystalline water, and has the advantages that the rabeprazole sodium sesquihydrate is high in purity and stability, and the phenomena of weight increasing due to moisture absorption even under a high-humidity condition are not obvious; the gastric acid secretion inhibition effect of the rabeprazole sodium sesquihydrate is improved by about 20 percent. The invention further relates to application of a composition comprising the sesquihydrate to treat digestive system diseases such as duodenal ulcers, gastric ulcers and reflux esophagitis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to rabeprazole sodium hydrate and a preparation method thereof. The invention also relates to the use of the hydrate composition to treat duodenal ulcer, gastric ulcer, reflux esophagitis and other digestive diseases. Application to systemic diseases. Background technique [0002] With the progress of society and the quickening pace of life, the incidence of digestive system diseases is also increasing year by year. According to statistics, the incidence of digestive system diseases in the world accounts for 10%-12% of the human incidence; the incidence of digestive system diseases in cities and towns in China reaches 11.43%, of which excessive gastric acid secretion is an important cause of digestive system diseases, H2 receptor antagonists and proton pump inhibitors are the two most commonly used drugs for the treatment of acid-related digestive diseases, they both inc...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61P1/04
CPCC07B2200/13C07D401/12
Inventor 严洁李轩
Owner TIANJIN HANRUI PHARMA
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