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R-lansoprazole for injection and preparation method thereof

A technology of dexlansoprazole and lansoprazole salt, applied in the field of dexlansoprazole for injection and its preparation, can solve the problem of reducing drug onset speed and bioavailability, instability of dexlansoprazole, etc. problems, to achieve the effect of improving bioavailability, increasing sublimation efficiency, and plump appearance

Inactive Publication Date: 2010-06-02
YANGZIJIANG PHARMA GROUP SHANGHAI HAINI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thereby dexlansoprazole is unstable in partial acidic diluent, after making oral preparation, drug absorption needs to go through drug disintegration release process, and cause dexlansoprazole to destroy and decompose because of gastric acid in the stomach, and reduce drug effect. speed of action and bioavailability

Method used

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  • R-lansoprazole for injection and preparation method thereof
  • R-lansoprazole for injection and preparation method thereof
  • R-lansoprazole for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The formulation of the preparation composition of dexlansoprazole for injection is as follows:

[0053] Active ingredient (21.43%) Dexlansoprazole 60g

[0054] Excipient (78.57%) Meglumine 20g

[0055] Mannitol 200g

[0056] pH adjuster (sodium hydroxide) pH10~12

[0057] Antioxidant (0%) None

[0058] Add dexlansoprazole, meglumine and mannitol into the dosing tank, add 2500ml of water for injection and stir until fully dissolved, add sodium hydroxide to adjust the pH to 10-12, add water for injection to 3000ml, and add to the prepared medicine solution Add 0.01% (W / V, g / 100ml) active carbon for medicinal purposes, stir at room temperature for 45 minutes, filter and decarbonize, then fine filter the filtrate with a 0.22 μm microporous filter membrane, measure the pH value and content of the filtrate, and pack it into 1000 bottle, half stoppered, cool down the subpackaged drug solution to -52°C at a rate of 0.8°C / min, keep it in a freezer for ...

Embodiment 2

[0060] The formulation of the preparation composition of dexlansoprazole for injection is as follows:

[0061] Active ingredient (30%) Dexlansoprazole 30g

[0062] Excipient (70%) Meglumine 10g

[0063] Mannitol 60g

[0064] pH adjuster (sodium hydroxide) adjust pH10~12

[0065] Antioxidant (0%): None

[0066] Add dexlansoprazole, meglumine and mannitol into the dosing tank, add 2500ml of water for injection and stir until fully dissolved, add sodium hydroxide to adjust the pH to 10-12, add water for injection to 3000ml, and add to the prepared medicine solution Add 0.5% (W / V, g / 100ml) medicinal activated carbon to the mixture, stir at room temperature for 15 minutes, filter and decarbonize, then fine filter the filtrate with a 0.22 μm microporous membrane filter, measure the pH value and content of the filtrate, and pack it into 1000 bottle, half stoppered, cool down the subpackaged medicinal solution to -40°C at a rate of 1.5°C / min, keep warm and fr...

Embodiment 3

[0068] The formulation of the preparation composition of dexlansoprazole for injection is as follows:

[0069] Active ingredient (12.45%) Dexlansoprazole 15g

[0070] Excipient (87.14%) Meglumine 5g

[0071] Dextran 100g

[0072] pH adjuster (sodium hydroxide) adjust pH8.5~11

[0073] Antioxidant (0.41%) sodium metabisulfite 0.5g

[0074] Add dexlansoprazole, meglumine, dextran and sodium metabisulfite into the dosing tank, add 1200ml of water for injection and stir until fully dissolved, add sodium hydroxide to adjust the pH to 8.5-11, add water for injection to 1500ml, and add to the dosing tank Add 1.0% (W / V, g / 100ml) medicinal activated carbon to the good medicinal liquid, stir at room temperature for 25 minutes, filter and decarbonize, then fine filter the filtrate with a 0.22 μm microporous filter membrane, measure the pH value and content of the filtrate, Divide into 1000 bottles, half-stoppered, cool the subpackaged medicinal solution to -52°...

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Abstract

The invention provides an r-lansoprazole for injection and a preparation method thereof. The medicament comprises active components of r-lansoprazole, or r-lansoprazole salt or r-lansoprazole water crystal as well as an excipient, a pH regulator and an antioxidizer. The preparation method comprises the following steps of: dissolving raw and auxiliary materials in water; adjusting the pH value; adding active carbon to decolor; filtering with a filter membrane; sub-packaging; freezing and drying to obtain the r-lansoprazole. The medicament is clinically used for treating gastric ulcer, duodenal ulcer, erosive gastro-esophageal reflux disease, helicobacter pylori, zollinger-ellison syndrome, and the like, can prevent the orally taken r-lansoprazole from being damaged in gastric acid and reach the aims of fast onset and improving the bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a proton pump inhibitor drug and a preparation method thereof, more specifically, dexlansoprazole for injection and a preparation method thereof. Background technique [0002] The chemical structure of dexlansoprazole is: [0003] [0004] Chemical name: (+)-2-[(R)-[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl] -1H-benzimidazole [0005] Dexlansoprazole is another optically pure proton pump inhibitor (proton pump inhibitors, PPIs) anti-ulcer drug developed after Esomeprazole (Esomeprazole). Oral preparations were launched by Japan's Takeda Pharmaceutical Factory in early 2009. This product belongs to the drug that replaces benzimidazoles and inhibits gastric acid secretion. It is an optically pure drug of racemic lansoprazole. It acts on the H + / K + -ATPase. H + It cannot be transported to the stomach, so that the amount of gastric acid in the gastric j...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61K9/19A61P1/04
Inventor 唐开勇谢雨礼郭晓静甘益民周庆武李玲玲安日明
Owner YANGZIJIANG PHARMA GROUP SHANGHAI HAINI PHARMA
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