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Lansoprazole compound

A technology of lansoprazole hydrate and dexlansoprazole, which is applied in the field of dexlansoprazole compound and its preparation, can solve the problem of high total amount of impurities, large number of impurities of dexlansoprazole, and low optical purity And other issues

Active Publication Date: 2011-11-09
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In the research process, repeat the method of above-mentioned patent document, obtain the impurity number of dexlansoprazole more, total amount of impurity is higher, optical purity is low

Method used

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  • Lansoprazole compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051]In the 1000ml reaction flask equipped with stirring, thermometer and condenser, add 80 grams of dexlansoprazole and 400ml of isopropanol-acetic acid-water=5-6:1-2:3-4 in the mixed solution, Stirring was started, heated to 70°C-72°C, filtered while hot, naturally cooled to room temperature, and kept warm for 5 hours, crystals were precipitated, filtered, and dried indoors to obtain 72.7 grams of white crystals. Determined by Karl Fischer method, it contains 10.88% (weight percent) of water. Purity 99.95% (HPLC normalization method), optical purity 99.99% ee.

[0052] Elemental Analysis Results:

[0053] Measured value (calculated value), C:46.28(46.37),H:4.60(4.62),N:10.20(10.14),

[0054] S: 7.79 (7.74), F: 13.81 (13.75).

[0055] 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 ° ;

[0056] The infrared spectrum of the crystal...

Embodiment 2

[0058] Capsules containing two hemihydrates of dexlansoprazole

[0059] Prescription: 60 grams of dexlansoprazole two hemihydrates, 5 ml of propylene glycol, and 150 grams of starch, made into 1000 capsules.

[0060] Process: Moisten two hemihydrates of dexlansoprazole and starch with 15% propylene glycol aqueous solution, mix well, sieve and granulate, dry at 60°C, granulate, and fill capsules.

Embodiment 3

[0062] Tablets containing two hemihydrates of dexlansoprazole

[0063] Prescription: 30 grams of dexlansoprazole two hemihydrates, 200 grams of lactose, 30 grams of PEG-4000, 11 grams of magnesium stearate, 27 grams of povidone K30, 50 grams of croscarmellose sodium, Appropriate amount of distilled water, made into 1000 tablets.

[0064] Process: Grind PEG-4000 and two hemihydrates of dexlansoprazole together, pass through 80-mesh sieve, mix with other materials, make soft material with distilled water, make granules with 16-mesh sieve, put in a drying box at 40-45 Dry at ℃, granulate with a 16-mesh sieve, add magnesium stearate to the dry granules, mix evenly, and compress into tablets.

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a dexlansoprazole compound and a preparation method thereof. The compound comprises 2.5 crystal water molecules, and has the advantages that: the chemical purity is 99.95 percent, the highest content of impurities is less than 0.1 percent, the optical purity is 99.99 percent ee, and the stability is high. The invention also relates to application of a composition of the compound in preparation of medicines for treating stomach burning caused by non-erosive gastro-oesophageal reflux and erosive esophagitis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a dexlansoprazole compound and a preparation method thereof. The invention also relates to the use of the hydrate composition to manufacture and treat stomach burning sensation and erosive gastroesophageal reflux caused by non-erosive gastroesophageal reflux. Esophagitis drug application. Background technique [0002] Lansoprazole is the second proton pump inhibitor on the market after omeprazole. Due to the introduction of fluorine, its properties are different from omeprazole, its thermodynamic and oxidation stability are increased, and its biological activity is greatly improved. It is used to treat gastric ulcer, duodenal ulcer and reflux esophagitis, and to eradicate Helicobacter pylori. [0003] Lansoprazole has a chiral central sulfur atom and therefore has two optical isomers. Studies have shown that the (R)-configuration of lansoprazole is significantly m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04
Inventor 严洁黄欣
Owner TIANJIN HANKANG PHARMA BIOTECH
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