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Fosfluconazole lyophilized preparation composition stable at normal temperature and preparation method thereof

A technology of fosfluconazole and freeze-dried preparations, applied in freeze-dried transportation, antifungal agents, powder transportation, etc., can solve problems such as poor stability, increased production costs, unfavorable storage for hospitals and patients, and achieve improved stability , Conducive to the effect of convenient production, storage and portability

Inactive Publication Date: 2014-06-25
ANHUI PIOM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Fosfluconazole listed in Japan abroad is only an injection solution with poor stability, so it is required to store it at 2-8°C in the instructions of the marketed product, and the validity period is one year. Storage under this condition will inevitably increase production costs, and it is not conducive to hospitals. and patient storage

Method used

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  • Fosfluconazole lyophilized preparation composition stable at normal temperature and preparation method thereof
  • Fosfluconazole lyophilized preparation composition stable at normal temperature and preparation method thereof
  • Fosfluconazole lyophilized preparation composition stable at normal temperature and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Prescription:

[0029]

[0030] Preparation Process:

[0031] Take about 90% of the total amount of water for injection, control the water temperature between 20°C and 25°C, add 302.7g of injection-grade arginine and 504.5g of fosfluconazole, which are accurately weighed, stir well until they are completely dissolved, and measure the pH value. At this time, the pH value is 8.9, add water for injection to the full amount, add 0.1% activated carbon for needles, stir for 30 minutes at 20 ° C ~ 25 ° C, filter with a 0.22 μm microporous membrane to sterilize, and divide the solution into 10 ml vials , the volume of each bottle is 5ml.

[0032] The prepared cillin bottle filled with fosfluconazole is put into the freeze-drying box, and then the temperature in the freeze-drying machine is reduced to below -45°C within 2 hours to make it freeze rapidly. Vacuumize and make the atmospheric pressure in the box reach 2.66pa within 30 minutes. Dry according to the temperature...

Embodiment 2

[0034] Prescription:

[0035]

[0036] Preparation Process:

[0037] Take about 90% of the total amount of water for injection in the prescription. The water temperature is controlled at 20°C to 25°C. Add 152.4g of injection-grade arginine and 252.3g of fosfluconazole, which are precisely weighed, and stir until they are completely dissolved. Measure the pH value. At this time, the pH value is 9.0, add water for injection to the full amount, add 0.1% activated carbon for needles, stir for 30 minutes at 20°C to 25°C, filter with a 0.22μm microporous filter membrane, and pack the solution into 7ml vials , the volume of each bottle is 2.5ml.

[0038] Put the prepared cillin bottle filled with fosfluconazole into the freeze-drying box, and then reduce the temperature inside the freeze-drying machine to below -45°C within 2 hours to make it freeze quickly. Vacuumize and make the atmospheric pressure in the box reach 2.66pa within 30 minutes. Dry according to the temperature ...

Embodiment 3

[0040] Prescription:

[0041]

[0042] Preparation Process:

[0043] Take about 90% of the total amount of water for injection, and control the water temperature at 20°C to 25°C, add 302.7g of injection-grade arginine, 504.5g of fosfluconazole and 1009g of injection-grade mannitol, and stir well until completely dissolved , measure the pH value, at this time the pH value is 9.1, add water for injection to the full amount, add 0.1% activated carbon for needles, stir for 30 minutes at 20 ° C ~ 25 ° C, sterilize and filter the solution with a 0.22 μm microporous membrane, and pack the solution in 10 ml specifications In the vials, the volume of each bottle is 5ml.

[0044]The prepared cillin bottle filled with fosfluconazole is put into the freeze-drying box, and then the temperature in the freeze-drying machine is reduced to below -45°C within 2 hours to make it freeze rapidly. Vacuumize and make the atmospheric pressure in the box reach 2.66pa within 30 minutes. Dry acco...

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Abstract

The invention provides a fosfluconazole lyophilized preparation composition stable at normal temperature and a preparation method thereof. The lyophilized preparation comprises fosfluconazole, a lyophilization excipient and a pH value regulating agent in a weight ratio of 5:10:3. The lyophilized preparation can be used for overcoming the defect of low-temperature preservation of an injection, and the preparation composition is more stable, cannot lose efficacy when being preserved for more than 2 years at normal temperature, and is favorable to preservation of hospitals and patients.

Description

1. Technical field [0001] The invention relates to the field of pharmaceutical preparations, and specifically designs a freeze-dried preparation composition of fosfluconazole stable at room temperature and a preparation method thereof. 2. Background technology [0002] Fos fluconazole injection was developed by Pfizer and launched in Japan in 2003 under the trade name Prodif. Fluconazole injection is a large infusion solution, and its production cost is relatively high. Fluconazole injection is an intravenous drip, which is time-consuming and inconvenient for patients. Fluconazole is slightly soluble in water, with a solubility of about 2mg / ml. If it is made into a 5ml: 200mg small water injection, the solubility must be increased by about 20 times, which is difficult to achieve in actual production. Fosfluconazole is a successful case of increasing solubility through structural modification. Fosfluconazole is the monophosphate of fluconazole, which is hydrolyzed in the b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4196A61K47/10A61K47/18A61K47/26A61P31/10
Inventor 徐奎陈正晧魏伟
Owner ANHUI PIOM PHARMA
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