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Nizofenone fumarate freeze-dried powder and method of preparing the same

A technology of nizophenone fumarate and freeze-dried powder is applied in the field of medicine, can solve the problems of poor solubility of microcrystalline cellulose, narrow application range, troublesome injection storage, etc., and achieves easy large-scale industrial production and preparation method Simple and easy to do, improve the effect of little solubility

Inactive Publication Date: 2009-06-10
SHANDONG LUOXIN PHARMA GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the tablet needs to go through the gastrointestinal tract when it is taken orally, and the drug effect is poor due to the influence of the first-pass effect
The microcrystalline cellulose used in powder injections has poor solubility in water, and nizophenone fumarate itself has poor solubility in water, and it is easy to produce insoluble matter when used. It is very dangerous to use it as an injection
And its injection is more troublesome to store, and it is easy to decompose and deteriorate.
[0008] At present, most nizophenone fumarate preparations sold in the market are aqueous injections, and there are many inconveniences in the use process: 1. In actual operation, the liquid needs to be pumped many times, and the preparations are easily contaminated by bacteria, resulting in unqualified pyrogens
2. In actual clinical practice, many diseases require reducing the amount of infusion, but water acupuncture cannot solve the problem
3. In the cold season, especially in the north and alpine areas, there are inconveniences in transportation and storage
4. The liquid preparation is damaged, which will easily cause pollution to the packaging
5. The scope of application is narrow
However, the powder injections disclosed in the prior art have adopted unsuitable auxiliary materials

Method used

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  • Nizofenone fumarate freeze-dried powder and method of preparing the same
  • Nizofenone fumarate freeze-dried powder and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Nizophenone Fumarate 5g

[0051] Mannitol 3g

[0052] Tween 80 2g

[0053] Put the main and auxiliary materials into the liquid mixing tank, add 1200m water for injection to dissolve, adjust the pH to 3~4 with hydrochloric acid or sodium hydroxide, then add 0.05% medical activated carbon and stir for 20 minutes to decolorize, then filter to remove carbon, and the filtrate is qualified after pH measurement Add water for injection until the volume of the solution is 2000ml, fine filter with a 0.22μm microporous membrane, subpackage the filtrate, and half-tamp the plug, freeze the subpackaged drug solution to -45°C, keep it frozen for 3 hours, and then evacuate to 1mmHg, the temperature was raised slowly at a constant speed of 3°C / hour to 15°C, and then raised to 45°C at a speed of 6°C / hour, then dried at a constant temperature for 5 hours, capped, packed and put into storage.

Embodiment 2

[0055] Nizophenone Fumarate 5g

[0056] Dextran 2.5g

[0057] Hydroxypropyl beta cyclodextrin 2g

[0058] Put the main and auxiliary materials into the liquid mixing tank, add 1200ml of water for injection to dissolve, adjust the pH to 3-11 with hydrochloric acid or sodium hydroxide, then add 0.05% medical activated carbon and stir for 10 minutes to decolorize, then filter to remove carbon, and the filtrate is qualified after pH measurement Add water for injection until the volume of the solution is 2000ml, fine filter with a 0.22μm microporous membrane, subpackage the filtrate, and half-tamp the plug, freeze the subpackaged drug solution to -60°C, insulate and freeze for 1 hour, and then evacuate to 10mmHg, the temperature was raised slowly at a constant speed of 5°C / hour to 0°C, and then the temperature was raised to 50°C at a speed of 9°C / hour, then dried at a constant temperature for 3 hours, capped, packed and put into storage.

Embodiment 3

[0060] Nizophenone Fumarate 5g

[0061] Dextran 50g

[0062] Poloxamer 2g

[0063] Put the main and auxiliary materials into the liquid mixing tank, add 1200ml of water for injection to dissolve, adjust the pH to 5-7 with hydrochloric acid or sodium hydroxide, then add 0.05% medical activated carbon and stir for 30 minutes to decolorize, then filter to remove carbon, and the filtrate is qualified after pH measurement Add water for injection until the volume of the solution is 2000ml, fine filter with a 0.22μm microporous membrane, subpackage the filtrate, and half-tamp the plug, freeze the subpackaged drug solution to -30°C, keep it frozen for 6 hours, and then evacuate to 0.5mmHg, the temperature was raised slowly at a constant speed of 2°C / hour to 0°C, and then raised to 40°C at a speed of 7°C / hour, and then dried at a constant temperature for 7 hours, capped, packed and put into storage.

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PUM

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Abstract

The invention provides nizofenone fumarate lyophilized powder for injection and a preparation method thereof. The lyophilized powder for injection comprises nizofenone fumarate, excipient, solubilizer and pH regulator. The dose of excipient is 0.1-10 times of that of the nizofenone fumarate, the dose of solubilizer is 0.1-10 times of the nizofenone fumarate, and the pH regulator is used for adjusting the pH value of the nizofenone fumarate before lyophilization to 3-11. The preparation method comprises the following steps of dissolving main raw materials and adjuvants in water, adjusting pH value, adding activated carbon for discoloration, filtering to remove carbon, subpackaging, freezing to -60-(-30) DEG C, keeping the temperature for 1-6 hours, vacuuming to 0.1-10mmHg, increasing the temperature to 0-30 DEG C with rate of 2-5 DEG C / hour, increasing the temperature to 30-50 DEG C with rate of 4-9 DEG C, and drying at constant temperature for 3-7 hours. The method of the invention is simple and easy for industrial production, and the obtained lyophilized powder has good quality, good appearance, and is easy for storage and transportation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a freeze-dried preparation, in particular to a nizophenone fumarate freeze-dried powder and a preparation method thereof. Background technique [0002] Nizofenone fumarate, CAS: 54533-85-6, molecular formula: C 25 h 25 ClN 4 o 7 , molecular weight: 528.88, structural formula: [0003] [0004] This product was researched and developed by Welfide Company of Japan, and it was launched in Japan in 1988. In 1991, it was listed in Korea by Hanall Company. This product is a new type of imidazole ischemic cerebrovascular disease improving drug, which can improve brain function, inhibit the formation of cerebral infarction, improve brain waves after cerebral ischemia and restore pyramidal tract function. Animal experiments also show that this product can significantly prolong the survival time of brain cells under ischemic or hypoxic conditions, thereby improving a series of symp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4164A61K9/19A61K47/30A61P9/10
Inventor 刘保起李明华宋良伟
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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