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Levopantoprazole sodium freeze-dried powder composition for injection and preparation method thereof

A technology for pantoprazole sodium and injection, which is applied in the field of medicine and can solve the problems of the stability of the preparation, the failure to completely isolate activated carbon, and the increase in the degree of degradation, etc., and achieve the effect of reducing irritation and reducing the introduction of insoluble particles

Active Publication Date: 2021-02-09
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In the previous patent literature, there have been many reports on S-pantoprazole sodium freeze-dried powder injection, but the influence of the interaction between the drug and activated carbon on the preparation has not been considered.
The stability of S-pantoprazole sodium solution is highly dependent on the pH value, and the degree of degradation increases with the decrease of the pH value; activated carbon sometimes appears "sol" or desorption in alkaline solution, which makes the solution in the opposite direction. The increase of impurities affects the quality of the preparation; light has a great impact on the stability of the preparation, but no measures have been taken to protect it.
[0011] Chinese patent CN102000034B is a kind of S-pantoprazole sodium composition and preparation method thereof for injection, because S-pantoprazole sodium itself is an alkaline medicine, so the pH value of the preparation solution of medicine is higher (9.8-10.5 ); although this invention carries out simple pretreatment to gac, experiment does not completely isolate gac and contact with S-pantoprazole sodium, desorption still can occur in gac
[0012] Chinese patent CN 103536563A freeze-dried powder injection of S-pantoprazole sodium composition for injection, the preparation process of the invention is very complicated, which is not conducive to the industrial production of the product; the auxiliary material chitosan nanoparticles used in the prescription process results in poor resolubility of the product , and the safety needs to be evaluated
This invention does not solve the problem of activated carbon desorption under alkaline conditions, and the problem of the influence of light on the stability of the preparation, and no solution is given

Method used

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  • Levopantoprazole sodium freeze-dried powder composition for injection and preparation method thereof
  • Levopantoprazole sodium freeze-dried powder composition for injection and preparation method thereof
  • Levopantoprazole sodium freeze-dried powder composition for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] S-pantoprazole sodium 200g

[0029] Sulfobutyl-β-cyclodextrin 400g

[0030] Water for injection 20L

[0031] Weigh 400 g of sulfobutyl-β-cyclodextrin and place it in a preparation tank, add 15 L of water for injection cooled to below 20 ° C, and stir to dissolve; then add the active ingredient S-pantoprazole sodium into it, and stir for 15~ After 20 minutes, add water for injection below 20°C to 20L, and stir for 5 minutes. Use a 0.22 μm polyethersulfone filter element for sterilization and filtration, divide the medicinal solution into vials, half-fill with rubber stoppers, each bottle contains 2 ml, and freeze-dry it.

Embodiment 2

[0033] S-pantoprazole sodium 200g

[0034] Glucosyl-β-cyclodextrin 800g

[0035] Water for injection 20L

[0036] Weigh 800 g of glucosyl-β-cyclodextrin and place it in a preparation tank, add 15 L of water for injection cooled to below 20 ° C, and stir to dissolve; then add the active ingredient S-pantoprazole sodium into it, and stir for 15~ After 20 minutes, add water for injection below 20°C to 20L, and stir for 5 minutes. Use a 0.22 μm polyethersulfone filter element for sterilization and filtration, divide the medicinal solution into vials, half-fill with rubber stoppers, each bottle contains 2 ml, and freeze-dry it.

Embodiment 3

[0038] S-pantoprazole sodium 200g

[0039] Hydroxypropyl-β-cyclodextrin 1200g

[0040] Water for injection 20L

[0041] Weigh 1200 g of hydroxypropyl-β-cyclodextrin and place it in a preparation tank, add 15 L of water for injection cooled to below 20 ° C, and stir to dissolve; then add the active ingredient S-pantoprazole sodium into it, and stir for 15~ After 20 minutes, add water for injection below 20°C to 20L, and stir for 5 minutes. Use a 0.22 μm polyethersulfone filter element for sterilization and filtration, divide the medicinal solution into vials, half-fill with rubber stoppers, each bottle contains 2 ml, and freeze-dry it.

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Abstract

The invention relates to a sterile freeze-dried powder for inhibiting the racemization of levopantoprazole sodium and a preparation process thereof. Using β-cyclodextrin and its derivatives, the active ingredient L-pantoprazole sodium is incorporated into its molecular "hole" structure to prevent its racemization to ensure the efficacy and safety of the product. The product of the present invention is stored for 24 months with less than 0.3% of R configuration isomers; the number of insoluble particles is significantly reduced through the optimization of the preparation process; the preparation process of the present invention is simple and feasible, and is suitable for industrial scale production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a freeze-dried powder composition of levopantoprazole sodium for injection and a preparation method thereof. Background technique [0002] Gastric ulcer is one of the common and frequently-occurring diseases in our country. Its occurrence is mainly related to the imbalance between the damage factors of the gastroduodenal mucosa and the defense and repair factors of the mucosa itself. Helicobacter pylori (H. pylori) infection, non-steroidal anti-inflammatory drugs (NSAIDs such as aspirin), and abnormal gastric acid secretion are common causes of ulcers. Typical ulcer pain is chronic, periodic, and rhythmic. [0003] In the stomach cavity, gastric acid and pepsin are important digestive substances in gastric juice. Stomach acid is a strong acidic substance and is highly erosive; pepsin has the effect of hydrolyzing proteins and can destroy the proteins on the stomach wall. However, in th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/40A61K31/4439A61P1/04
Inventor 张贵民吕永超
Owner SHANDONG NEWTIME PHARMA