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A kind of fos fluconazole freeze-dried powder composition and preparation method thereof

A technology of fosfluconazole and spafluconazole, which is applied in the field of fosfluconazole freeze-dried powder composition and its preparation, can solve the problems of unsatisfactory freeze-drying molding effect, unstable pH value, easy precipitation, etc., and achieve Reduce the production of harmful impurities, easy to carry and transport, and good resolubility

Active Publication Date: 2018-04-27
科贝园(北京)医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the high concentration, it is easy to precipitate during preparation, and the effect of freeze-drying is not ideal
And the pH value is unstable during the freeze-drying process and during the storage process, and the pH tends to decrease with the prolongation of the storage time

Method used

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  • A kind of fos fluconazole freeze-dried powder composition and preparation method thereof
  • A kind of fos fluconazole freeze-dried powder composition and preparation method thereof
  • A kind of fos fluconazole freeze-dried powder composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048]

[0049]

[0050] Preparation process: Take 30% of the prescribed amount of water for injection, add the prescribed amount of fosfluconazole, stir evenly, add sodium hydroxide solution, until the drug is completely dissolved and adjust the pH value of the solution to 9.0, add water to the full amount, add 0.1% of Activated carbon, stirred for 15 minutes, sterilized and filtered with a 0.22 μm microporous membrane, filled in a 5ml vial with a filling volume of 1ml / cartridge, and half stoppered. During the preparation of the liquid medicine, the water temperature should be controlled below 25°C.

[0051] Place the vial in a freeze dryer, and lower the temperature inside the freeze dryer to below -40°C within 2 hours to freeze it quickly. Vacuumize, reduce the atmospheric pressure in the box to 3.5pa within 30 minutes, sublimation drying temperature is -20°C, dry for 10h, program temperature rise to 30°C for drying, the heating rate is not more than 5°C / h, follow the...

Embodiment 2

[0053]

[0054] Preparation process: take 30% of the prescription amount of water for injection, add fosfluconazole of the prescription amount, stir evenly, add sodium hydroxide solution until the drug is completely dissolved and adjust the pH value of the solution to 9.0, add sodium chloride to dissolve, add water to For the full amount, add 0.1% activated carbon, stir for 15 minutes, sterilize and filter with a 0.22 μm microporous membrane, fill in a 5ml vial, the filling volume is 1ml / bottle, and half stoppered. During the preparation of the liquid medicine, the water temperature should be controlled below 25°C.

[0055] Place the vial in a freeze dryer, and lower the temperature inside the freeze dryer to below -45°C within 2 hours to freeze it quickly. Vacuumize to reduce the atmospheric pressure in the box to 4.1 within 30 minutes, sublimation drying temperature is -20°C, dry for 10 hours, program temperature rise to 30°C for drying, temperature rise rate is not more ...

Embodiment 3

[0057]

[0058]

[0059] Preparation process: Take 30% of the prescription amount of water for injection, add sodium hydroxide and fosfluconazole in the prescription amount, stir to dissolve, add citric acid solution, adjust the pH value of the solution to 9.0, add water to the full amount, add 0.1% activated carbon, Stir for 15 minutes, sterilize and filter with a 0.22 μm microporous membrane, fill in a 5ml vial, the filling volume is 1ml / bottle, and half stoppered. During the preparation of the liquid medicine, the water temperature should be controlled below 25°C.

[0060] Place the vial in a freeze dryer, and lower the temperature inside the freeze dryer to below -40°C within 2 hours to freeze it quickly. Vacuumize to reduce the atmospheric pressure in the box to 3.8pa within 30 minutes, sublimation drying temperature is -20°C, dry for 10 hours, program temperature rise to 30°C for drying, temperature rise rate is not more than 5°C / h, follow the program to heat up to...

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Abstract

The invention relates to a fosfluconazole freeze-dried powder composition and a preparation method thereof. Wherein, the composition comprises fosfluconazole and a pH regulator, wherein the pH regulator is selected from sodium hydroxide, sodium citrate, sodium dihydrogen phosphate, disodium hydrogen phosphate, sodium acetate, citric acid, One or more of phosphoric acid, acetic acid, hydrochloric acid. The fosfluconazole freeze-dried powder of the present invention has a simple prescription, is stored in a solid form, is convenient to carry and transport, and can be stored for more than two years at a temperature below 25°C, which can greatly delay the degradation rate of the fosfluconazole and increase the stability. It can reduce the generation of harmful impurities, improve the quality of products, and ensure the safety of patients in medication.

Description

technical field [0001] The invention relates to a fosfluconazole freeze-dried powder composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Fluconazole can inhibit the synthesis of ergosterol in the fungal cell membrane, and exhibit strong antibacterial activity in the yeast-type development phase and hyphae-type development phase of fungi. The global sales of the drug in 2000 were US$1.014 billion, which increased to US$1.066 billion in 2001, a year-on-year increase of 5.13%, ranking 43rd among the world's best-selling drugs. 11.12% billion dollars. Since fluconazole is slightly soluble in water (solubility about 2mg / ml), if a small water injection of 5ml:200mg is made, the solubility must be increased by more than 20 times, which is difficult to achieve in actual production. Therefore, it is necessary to modify the structure of fluconazole to increase its solubility. [0003] Fosfluconazole is a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/675A61P31/10A61K31/4196
Inventor 满艳哲
Owner 科贝园(北京)医药科技有限公司