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

A technology of lansoprazole and lyophilized powder, applied in the field of biomedicine, can solve the problems of high risk of clinical application, threat to patient medication safety, calcium deficiency, etc., and achieves accelerated dissolution rate, water sublimation, and good redissolving performance. Effect

Active Publication Date: 2018-08-31
JINAN KANGHE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of lansoprazole, it is easy to produce visible foreign matter and insoluble particles after freeze-drying and reconstitution. Especially when it is compatible with clinical infusion, there will be a large number of fine particles. After entering the blood, it can cause embolism, form phlebitis, Granuloma, allergic reaction, etc., the risk of clinical application is relatively high, which poses a great threat to the safety of medication for patients
[0008] At present, a large amount of research has been carried out to solve the problems of visible foreign matter and insoluble particles after reconstitution of lansoprazole freeze-dried powder injection, such as in terms of formula components: patents CN101057846 and CN1810244 disclose the use of meglumine as a cosolvent to increase Lansoprazole water-soluble method, but problems such as the stability of solution and resolubility are not solved; CN101129368 and CN101874789A are by adding polyethylene glycol, although can solve the problem of solubility and resolubility, hemolysis phenomenon easily occurs, also Its stability problem is not really solved; in CN101756898A, components such as emulsifier, carrier material, antioxidant and excipient are added to make freeze-dried powder in order to increase the water solubility of the drug. This technology increases the clinical use due to adding too many auxiliary materials risk; CN101829065B uses disodium edetate as a stabilizer, but disodium edetate will complex with calcium ions after injection into the blood, resulting in bone calcium loss and the risk of calcium deficiency
[0009] In terms of the preparation process of lansoprazole freeze-dried powder, the current research mainly includes: CN201110144489.6, CN200810122761.9 and CN201010198253.6 adopt the pre-freezing process of direct cooling, which is easy to cause crystallization and product redissolution visible foreign matter or insoluble particles
[0010] At present, the formula and process of lansoprazole freeze-dried powder do not solve the problems of visible foreign matter and insoluble particles after product reconstitution, which leads to the appearance of a large number of fine particles during clinical infusion compatibility, which can cause embolism after entering the blood , form phlebitis, granuloma, allergic reaction, etc., the risk of clinical application is relatively high, which poses a great threat to the safety of patients' medication

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] prescription

[0028] Element

Dosage

Lansoprazole

20g

Hydroxyethyl starch

40g

Acetamide

10g

sodium hydroxide

Adjust the pH to 10.5

Water for Injection

Add to 3000ml

[0029] Preparation:

[0030] (1) Dosing: inject 2700ml water for injection into the dosing tank, cool to 30°C, add 40g hydroxyethyl starch, add 10g acetamide and stir to dissolve, add 20g lansoprazole, stir to make lansoprazole dissolve, Adjust the pH to 10.5 with sodium hydroxide, add water to 3000ml, add 0.1% (w / v) activated carbon to the liquid medicine, stir at room temperature for 20 minutes, filter for decarbonization, and filter the filtrate through a 0.22 μm filter membrane to sterilize;

[0031] (2) Filling and half stoppering;

[0032] (3) Freeze-drying: Pre-freezing adopts the method of repeated heating and cooling, which is characterized in that the temperature is reduced to -45 °C at a cooling rate of 1 °C / min, kept for 1 h...

Embodiment 2

[0035] prescription

[0036] Element

Dosage

Lansoprazole

30g

Hydroxyethyl starch

50g

Acetamide

20g

sodium hydroxide

Adjust the pH to 11.0

Water for Injection

Add to 3000ml

[0037] Preparation:

[0038] (1) Dosing: inject 2700ml water for injection into the dosing tank, cool to 0°C, add 50g hydroxyethyl starch, add 20g acetamide and stir to dissolve, add 30g lansoprazole, stir to make lansoprazole dissolve, Adjust the pH to 11.0 with sodium hydroxide, add water to 3000ml, add 0.1% (w / v) activated carbon to the liquid medicine, stir at room temperature for 20 minutes, filter and decarbonize, and filter the filtrate through a 0.22 μm filter membrane to sterilize;

[0039] (2) Filling and half stoppering;

[0040] (3) Freeze-drying: Pre-freezing adopts the method of repeated heating and cooling, which is characterized in that the cooling rate is 1.5 °C / min down to -45 °C, kept for 2 hours, and then raised to -...

Embodiment 3

[0043] prescription

[0044]

[0045]

[0046] Preparation:

[0047](1) Dosing: inject 2700ml water for injection into the dosing tank, cool to 15°C, add 60g hydroxyethyl starch, add 30g acetamide and stir to dissolve, add 40g lansoprazole, stir to make lansoprazole dissolve, Use sodium hydroxide to adjust the pH to 10.7, add water to 3000ml, add 0.1% (w / v) activated carbon to the liquid medicine, stir at room temperature for 20 minutes, filter for decarbonization, and filter the filtrate through a 0.22 μm membrane filter to sterilize;

[0048] (2) Filling and half stoppering;

[0049] (3) Freeze-drying: Pre-freezing adopts the method of repeated temperature rise and fall pre-freeze, which is characterized in that the temperature rise and fall rate is reduced to -45°C at a cooling rate of 1.2°C / min, kept for 1.5h, and then raised at a heating rate of 2°C / min. Heat at -25°C for 1.5h, then cool down to -40°C at a cooling rate of 1.2°C / min, and hold for 2h; sublimate and ...

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Abstract

The present invention relates to a kind of lyophilized powder of lansoprazole for injection and preparation method thereof, this lyophilized powder comprises lansoprazole, hydroxyethyl starch, acetamide, sodium hydroxide and water for injection, wherein lansoprazole: Hydroxyethyl starch: the weight ratio of acetamide is 2~4: 4~6: 1~3; Lansoprazole and hydroxyethyl starch, acetamide can form good eutectic compound; The preparation method of this lyophilized powder The medium pre-freezing method adopts the method of repeated heating and cooling; the freeze-dried powder produced by this technical scheme has good shape, good resolubility, and excellent compatibility with infusion in clinical use, and there is no visible foreign matter and insoluble particles.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a lansoprazole freeze-dried powder for injection and a preparation method thereof. Background technique [0002] Lansoprazole is the second-generation proton pump inhibitor developed by Japan's Takeda Pharmaceutical Co., Ltd. It was first launched in Japan in 1991 and passed the US FDA certification in 1995. Its global sales in 2000 were 3.694 billion U.S. dollars, ranking it in the world Sixth, it is the second largest product in the anti-ulcer drug market in the same year. [0003] The chemical name of the drug is 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl-1H-benzimidazole], Molecular formula is C 16 h 14 f 3 N 3 o 2 S, the molecular weight is 369.36. The structural formula is: [0004] [0005] Lansoprazole has good acid suppression effect, long-lasting action and strong specificity. When it is distributed in the acidic environment of gastric pariet...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/36A61K47/18A61K31/4439A61P1/04A61P31/04
CPCA61K9/0019A61K9/19A61K31/4439A61K47/18A61K47/36
Inventor 张颖徐宇超李鹏何花杨春芬
Owner JINAN KANGHE MEDICAL TECH
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