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A kind of esomeprazole freeze-dried powder injection and preparation method thereof

A technology for esomeprazole and freeze-dried powder injection is applied in the field of esomeprazole freeze-dried powder for injection and preparation thereof, and can solve the problems of difficulty in guaranteeing clarity, difficult and difficult to reconstitute esomeprazole and the like , to avoid damaging free radical reaction, not easy to rupture, and the effect of stable foam structure

Active Publication Date: 2016-11-30
WUHAN PUSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The product obtained by this method is low in related substances, and there is no significant increase in related substances in the storage process, and there is no obvious decrease in content, but the freeze-drying time is as long as more than 20 hours, and esomeprazole itself is difficult to dissolve in water, and after freeze-drying into blocks It is more difficult to reconstitute, and the clarity after reconstitution is difficult to guarantee

Method used

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  • A kind of esomeprazole freeze-dried powder injection and preparation method thereof
  • A kind of esomeprazole freeze-dried powder injection and preparation method thereof
  • A kind of esomeprazole freeze-dried powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] formula:

[0026]

[0027] Preparation:

[0028] ①Preparation of liquid medicine: Weigh parts of esomeprazole and dissolve it in three quarters of water for injection, stir at 25°C until clarified to obtain liquid A; weigh parts of sucrose, Pluronic- F68, gelatin, arginine and glycerin were added to medicinal solution A, mixed and stirred evenly, adjusted to pH 4 with 25mM phosphate buffer solution of pH 7.2, and supplemented with water for injection to the full amount to obtain medicinal solution B;

[0029] ②Vacuum foaming: Put the liquid medicine B in a vacuum stirring tank, the output frequency of the vacuum pump is 35Hz, manually adjust the vacuum degree to 50Pa, and start stirring after 3 minutes of stabilization, and pass inert gas N while stirring 2 , the incoming flow rate is 0.8m 3 / h, the time is 20 minutes, the stirring speed is 1800 rpm, the stirring is accelerated until foaming, the manual regulating valve is closed, the vacuum in the tank is rapidly ...

Embodiment 2

[0033] formula:

[0034]

[0035] Preparation:

[0036] ①Preparation of medicinal solution: Weigh parts of esomeprazole and dissolve it in 3 / 4 of water for injection, stir at 25°C until clarified to obtain medicinal solution A; weigh parts of lactose and sorbitol , ovalbumin, methionine and glycerin are added to the medicinal solution A, mixed and stirred evenly, the pH is adjusted to 7 with sodium phosphate, and water for injection is added to the full amount to obtain the medicinal solution B;

[0037] ②Vacuum foaming: Put the liquid medicine B in a vacuum stirring tank, the output frequency of the vacuum pump is 35Hz, manually adjust the vacuum degree to 50Pa, and start stirring after 4 minutes of stabilization, while stirring, pass inert gas CO 2 , the incoming flow rate is 1m 3 / h, the time is 30 minutes, the stirring speed is 2000 rpm, the stirring is accelerated until foaming, the manual regulating valve is closed, the vacuum degree in the tank is rapidly reduced to...

Embodiment 3

[0041]

[0042]

[0043] Preparation:

[0044] ①Preparation of liquid medicine: Weigh parts of esomeprazole and dissolve it in 3 / 4 of water for injection, stir at 25°C until clarified to obtain liquid A; weigh parts of mannose, wood Add sugar alcohol, collagen, ethylenediaminetetraacetic acid and glycerin to liquid A, mix and stir evenly, adjust the pH to 10 with ammonium bicarbonate, add water for injection to the full amount, and obtain liquid B;

[0045] ②Vacuum foaming: Put the drug solution B in a vacuum stirring tank, the output frequency of the vacuum pump is 35Hz, manually adjust the vacuum degree to 50Pa, and start stirring after 5 minutes of stabilization, and pass inert gas CH while stirring 4 , the incoming flow rate is 1.2m 3 / h, the time is 40 minutes, the stirring speed is 2200 rpm, the stirring is accelerated until foaming, the manual regulating valve is closed, the vacuum in the tank is rapidly reduced to below 10Pa, and the temperature is reduced to 5°...

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Abstract

The invention discloses a freeze-dried esomeprazole powder injection and a preparation method thereof. The main agent esomeprazole, auxiliary agents including protective agents, stabilizers and excipients, pH regulators and water for injection are prepared according to The weight ratio of 1:0.45~0.65:0.25~0.5:50 is prepared and placed in a stirring tank, and the inert gas is introduced to accelerate the stirring until foaming in a vacuum state, and then filtered, divided, pretreated, and freeze-dried to obtain Esso Meprazole freeze-dried powder finished product. In the preparation process of the present invention, by adopting vacuum foaming technology, the moisture in the liquid medicine is greatly reduced, the freeze-drying time of the liquid medicine is only 50% of the existing technology, and the specific surface area of ​​the material after foaming is significantly increased , the properties of the drug have been significantly improved, and the finished product for powder injection has a bulky volume, is not easy to agglomerate, has good resolubility, and high clarity. It not only has advantages in heat resistance, but also maintains the pharmacological activity of the drug after injection. Bioavailability is greatly improved.

Description

technical field [0001] The invention belongs to a pharmaceutical preparation, in particular to a freeze-dried esomeprazole powder injection and a preparation method thereof. Background technique [0002] Esomeprazole is the S-isomer of omeprazole, which is the first isomer proton pump inhibitor available for clinical intravenous administration in the world, and has a stronger effect. Its mechanism of action is protonation under acidifying conditions, transforming into a compound sulfenamide that inhibits H+ / K+-ATPase activity, and rapidly combines with the sulfhydryl group of cysteine ​​on H+ / K+-ATPase to form a disulfide bond. Thereby inactivating the enzyme, specifically inhibiting the H+ / K+-ATPase activity in gastric parietal cells, thereby inhibiting gastric acid secretion. Esomeprazole is a proton pump inhibitor, which has a stronger and longer-lasting ability to suppress gastric acid than others, and the individual differences in metabolism and side effects of esomepr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/4439A61K47/36A61K47/42A61K47/26A61K47/32A61P1/04
Inventor 刘昔平徐林华刘浏陈杰枫梅媛王萍程波陈晨
Owner WUHAN PUSHENG PHARMA
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