Lansoprazole sodium submicron emulsion freeze-drying preparation

A technology of lansoprazole sodium and freeze-dried preparations, which is applied in the field of submicron emulsion freeze-dried preparations of lansoprazole sodium and its preparation, and can solve problems such as difficult industrial scale-up production, easy destruction, and reduced production reproducibility , to achieve the effect of reducing drug side effects, ensuring product quality, and product quality stability

Inactive Publication Date: 2009-09-30
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Lansoprazole sodium is unstable under acidic conditions, is easily destroyed in gastric acid, is slowly absorbed orally after being made into tablets or capsules, and has low bioavailability, so it needs to be made into injections, but because Lansoprazole The stability of the azole solution is very poor, and it cannot be sterilized by high temperature, and only the freeze-drying method can be used to prepare injections
However, during the development, it was found that the lansoprazole freeze-dried powder injection prepared by the common preparation method was reconstituted with obvious foreign matter, and the insoluble particles were unqualified
[0006] The disclosed lansoprazole sodium freeze-dried powder injection of CN1810224A adopts meglumine as stabilizer, but only contains a basic group in the meglumine structure, although certain buffering effect is arranged, but not strong enough, to make lansoprazole The medicinal solution prepared by injection will precipitate and crystallize after being placed at room temperature f...

Method used

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  • Lansoprazole sodium submicron emulsion freeze-drying preparation
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  • Lansoprazole sodium submicron emulsion freeze-drying preparation

Examples

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Effect test

Embodiment 1

[0049] Example 1 Preparation of Lansoprazole Sodium Submicroemulsion Freeze-dried Preparation

[0050] Formula: Lansoprazole 15g

[0051] Sodium hydroxide 2g

[0052] Polyacrylate 75g

[0053] Poloxamer 188 100g

[0054] Trehalose 120g

[0055] Povidone K15 30g

[0056] Preparation Process

[0057] (1) 15g lansoprazole and 2g sodium hydroxide are dissolved in 500ml water, 75g polyacrylate is dissolved in 200ml acetone, the two are mixed and stirred for 15min, and the rotating speed is 800r / min to make W / O type emulsion;

[0058] (2) Dissolve 120g trehalose and 30g povidone K15 in 1000ml water, add the solution to the above-mentioned W / O emulsion, stir at room temperature for 30min, and rotate at 200r / min to make a W / O / W double emulsion;

[0059] (3) Add the above-mentioned W / O / W type double emulsion into the aqueous solution of 100g poloxamer 188, stir at room temperature for 60min, rotate at a speed of 500r / min, evaporate acetone under redu...

Embodiment 2

[0091] The preparation of embodiment 2 lansoprazole sodium submicron emulsion preparation

[0092] Formula: Lansoprazole 30g

[0093] Sodium hydroxide 3.5g

[0094] Polylactic acid 180g

[0095] Tween 80 60g

[0096] Glucose 180g

[0097] Povidone K30 18g

[0098] Preparation Process

[0099] (1) Dissolve 30g of lansoprazole and 3.5g of sodium hydroxide in 1000ml of water, dissolve 180g of polylactic acid in 500ml of isopropanol, mix and stir for 30min at a speed of 200r / min to make a W / O emulsion ;

[0100] (2) Dissolve 18g of povidone K30 and 180g of glucose in 500ml of water, add the solution to the above-mentioned W / O emulsion, stir at room temperature for 40min, and rotate at 800r / min to make a W / O / W type double emulsion;

[0101] (3) Add the above-mentioned W / O / W type double emulsion into the aqueous solution of 60g Tween 80, stir at room temperature for 30min, rotate at a speed of 200r / min, evaporate isopropanol under reduced pressur...

Embodiment 3

[0104] The preparation of embodiment 3 lansoprazole sodium submicron emulsion preparation

[0105] Formula: Lansoprazole 30g

[0106] Sodium hydroxide 3.8g

[0107] Polylactic / glycolic acid copolymer 150g

[0108] Lecithin 90g

[0109] Maltose 100g

[0110] Dextran 40 40g

[0111] Preparation Process

[0112] (1) 30g lansoprazole and 3.8g sodium hydroxide were dissolved in 1000ml water, 150g polylactic acid / glycolic acid copolymer was dissolved in 800ml dichloromethane, the two were mixed and stirred for 20min, and the rotating speed was 500r / min to prepare W / O type emulsion;

[0113] (2) Dissolve 40g of dextran 40 and 100g of maltose in 500ml of water, add the solution to the above-mentioned W / O type emulsion, stir at room temperature for 35min, and rotate at 400r / min to make W / O / W type double emulsion;

[0114] (3) Add the above-mentioned W / O / W type double emulsion into the aqueous solution of 90g lecithin, stir at room temperature for 40...

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Abstract

The invention provides a method for preparing Lansoprazole sodium submicron emulsion freeze-drying preparation and the product thereof. The method includes the following steps: (1) Lansoprazole and sodium hydroxide are dissolved together in water, biodegradable polymer is dissolved in and mixed and stirred with organic solvent to form W/O type emulsion; (2) stabilizing agent and apodemal agent are dissolved in water, and the obtained solution is added to the W/O type emulsion to be stirred to form W/O/W type emulsion; and (3) the W/O type emulsion is added to the emulsifying agent aqueous solution and stirred into the same at room temperature, and the submicron emulsion freeze-drying preparation is obtained after the operations of pressure reduction for organic solvent evaporation, eccentric separation, water rinsing, freezing and drying are performed.

Description

technical field [0001] The invention relates to a submicron emulsion preparation of lansoprazole sodium, in particular to a submicroemulsion freeze-dried preparation of lansoprazole sodium and a preparation method thereof. Background technique [0002] Lansoprazole sodium, its chemical name is: 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]-sulfinyl] -1H-benzimidazole sodium salt, molecular formula C 16 h 13 f 3 N 3 NaO 2 S, molecular weight 391.34, structural formula: [0003] [0004] It is a new type of drug that inhibits gastric acid secretion. It acts on the H+-K+-ATPase of gastric parietal cells, so that the H+ of parietal cells cannot be transported to the stomach, so that the amount of gastric acid in gastric juice is greatly reduced. It is clinically used for ten The treatment of duodenal ulcer, gastric ulcer, reflux esophagitis, and Zollinger-Ellison syndrome (gastrinoma) has remarkable curative effect, and has inhibitory effect on Helicobacter ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/4439A61K47/42A61K47/36A61K47/34A61K47/32A61P1/04
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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