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Lansoprazole compound and pharmaceutical composition thereof

A technology for lansoprazole and compounds, which is applied in the field of lansoprazole compounds and pharmaceutical compositions thereof, can solve the problems of poor stability of lansoprazole, increased cost, difficult preparation application and the like

Active Publication Date: 2013-08-21
湖北美林药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Lansoprazole has poor stability and is difficult to dissolve in water. It needs to be dissolved under high pH value conditions, making it difficult to use in preparations. The prior art of this problem generally solves this problem from preparation technology, and often technology requires extremely strict and complex, uses more raw materials, such as in the preparation technology of lansoprazole for injection, in order to keep the stability and stability of lansoprazole Insoluble microparticles meet the requirements, and the prior art generally adopts a large variety of raw materials, such as Chinese application: CN201210115887.X relates to a lansoprazole pharmaceutical composition for injection, containing lansoprazole: 3 parts by weight, poloxa Mu 188: 5-15 parts by weight, mannitol: 10 parts by weight; or it is necessary to maintain a high pH value in the preparation process. The highest pH reaches 12.5; also as mentioned in the Chinese application CN101313895B, use the method of separating out part of the lansoprazole crystals first, then filter, fill, and freeze-dry, which solves the problem of resolubility, but this patent method needs to be filtered to remove part The crystallization of lansoprazole has caused a lot of waste and increased costs. These technologies have limited the use of lansoprazole in preparations, and some studies have tried to solve this problem from crystal structure research, such as the Chinese application CN102180866A and Chinese application CN102558154A, although the stability and solubility of the lansoprazole compound obtained by it are improved, but the improvement is limited

Method used

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  • Lansoprazole compound and pharmaceutical composition thereof
  • Lansoprazole compound and pharmaceutical composition thereof
  • Lansoprazole compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] The preparation of embodiment 1 Lansoprazole compound

[0070] 60 DEG C, under the stirring speed of 100 rev / mins, lansoprazole is dissolved in the mixed solution of methanol and ethanol that volume ratio is 7:1 by weight ratio 1:12; 1.5% activated carbon, stirred at 150 rpm for 25 minutes, filtered to remove carbon, and filtered the filtrate through a 0.22 μm filter membrane to obtain solution I; lower the temperature to 30°C, and pour into solution I while stirring at a stirring speed of 100 rpm Slowly and uniformly drop a mixed solution of water and ether whose volume ratio is 7:1, which is 10 times the weight of the mixed solution of methanol and ethanol, at a rate of 70mL / min; at the same time, the temperature is lowered to 10°C at a constant rate of 1.5°C / min. , stop stirring, cool down to 2°C at a constant rate of 0.1°C / min, let stand for crystal growth for 10 hours, and filter to obtain a filter cake; use 3 times the weight of the filter cake with a mixed soluti...

Embodiment 2

[0071] The preparation of embodiment 2 Lansoprazole compound

[0072] 65 DEG C, under the stirring speed of 150 revs / min, lansoprazole is dissolved in the mixed solution of methanol and ethanol that volume ratio is 7:1 by weight ratio 1:15; 1.5% activated carbon, stirred at 200 rpm for 25 minutes, filtered to remove carbon, and filtered the filtrate through a 0.22 μm filter membrane to obtain solution I; cooled to 34 ° C, at a stirring speed of 150 rpm, poured into solution I while stirring At a rate of 90mL / min, slowly and uniformly drop a mixed solution of water and ether whose volume ratio is 7:1, which is 12 times the weight of the mixed solution of methanol and ethanol; at the same time, the temperature is lowered to 14°C at a constant rate of 1.5°C / min. , stop stirring, cool down to 4°C at a constant rate of 0.2°C / min, let stand for crystal growth for 10 hours, and filter to obtain a filter cake; use 3 times the weight of the filter cake with a mixed solution of water an...

Embodiment 3

[0074] Example 3 Preparation of Lansoprazole Compound Pharmaceutical Composition (lyophilized powder injection)

[0075] Prescription: (Specification: 30mg / bottle)

[0076] Lansoprazole Compound 30g

[0077] Mannitol 150g

[0078] Appropriate amount of sodium hydroxide

[0079] Make 1000 pieces

[0080] The preparation method is as follows:

[0081] 1) Add 30g of lansoprazole compound into 1500g of water for injection at 55-60°C, stir and disperse evenly, adjust the pH value to 11.20 with sodium hydroxide, stir to completely dissolve lansoprazole, and add 150g of mannitol Add water for injection and stir to dissolve, add 500g of water for injection, and stir evenly;

[0082] 2) Add 0.15% activated carbon to step 1), stir for 20 minutes, filter to decarbonize, filter and sterilize with a 0.22 μm filter membrane to obtain the filtrate;

[0083] 3) Freeze-drying:

[0084] ① Pre-freezing: put the filtrate in step 2) into a half-packed freezer and pl...

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Abstract

The invention relates to a lansoprazole compound and a pharmaceutical composition thereof. The lansoprazole compound is a crystal. The characteristic peaks measured by X-ray powder diffraction are shown as 3.6, 4.8, 10.9, 14.0, 15.4, 16.9, 22.6, 24.7, 28.5, 32.1, 35.2, 36.7 and 39.3 at 2theta+ / -0.2 degrees. The medical composition preparation comprises the lansoprazole compound. The preparation is in form of freeze-dried powder injections, troches, capsules, enteric-coated tablets or enteric-coated capsules. The lansoprazole compound prepared by the invention has better solubleness and stability. The lansoprazole pharmaceutical composition prepared by using the lansoprazole compound provided by the invention as the effective component is good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a lansoprazole compound and a pharmaceutical composition thereof. Background technique [0002] Lansoprazole chemical name: 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl-1H-benzimidazole ]. Lansoprazole is a proton pump inhibitor, a new type of drug that inhibits gastric acid secretion. After the drug is distributed in the acidic environment of the parietal cells of the gastric mucosa, it is transformed into active metabolites. This metabolite binds to the sulfhydryl group of H+, K+-ATPase present at the site of acid generation, and inhibits acid secretion by inhibiting the activity of H+, K+-ATPase. It is clinically used in the treatment of duodenal ulcer, gastric ulcer, reflux esophagitis, and Zollinger-Ellison syndrome (gastrinoma), with remarkable curative effect and inhibitory effect on Helicobacter pylori. [0003] Lansoprazole introduces fluorine i...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61P1/04A61P31/04
Inventor 曾艺胡成忠
Owner 湖北美林药业有限公司
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