Fosfluconazole freeze-drying preparation composition and preparing method thereof

A technology of fosfluconazole and freeze-dried preparations, applied in freeze-dried transportation, antifungal agents, pharmaceutical formulations, etc., can solve the problems of unfavorable promotion and application, increased cost, inconvenient storage, etc., and achieve strong resolubility and good stability performance, the effect of improving practicality

Inactive Publication Date: 2017-01-04
合肥美利康医药技术股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, fosfluconazole is only an injection solution with poor stability, and can only be stored at 2-8°C with a validity period of 1 year. If stored under this condition, its cost will increase greatly, and it is not convenient for hospitals or patients to store, which is not conducive to Its promotion and application in clinical

Method used

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  • Fosfluconazole freeze-drying preparation composition and preparing method thereof
  • Fosfluconazole freeze-drying preparation composition and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] A kind of fosfluconazole freeze-dried preparation composition, comprising fosfluconazole, molar ratio is the composition of absolute ethanol and acetone of 1:1, the composition of lactic acid and sodium hydroxide, povidone K30, glucose and Composition of mannitol, glycine.

[0019] The mass percentage of fosfluconazole and filler is 1:2.6.

[0020] The mass percentage of excipient, stabilizer and povidone K30 is 1.8:0.9:1.1.

[0021] The preparation method of fos fluconazole freeze-dried preparation composition, the preparation steps are as follows:

[0022] 1) Add fosfluconazole and the filler to water for injection 8 times the weight of the filler, stir and blend, add the composition of absolute ethanol and acetone dropwise during the stirring process, and then add 2 times the weight of the filler Water for injection in parts by weight, stirred evenly, and then adding a pH regulator to adjust the pH to 8.3 to obtain an aqueous solution of forsifluconazole;

[0023]...

Embodiment 2

[0026] A fosfluconazole freeze-dried preparation composition, comprising forsfluconazole, a composition of dehydrated alcohol and acetone with a molar ratio of 2:1, a composition of tartaric acid and sodium hydroxide, povidone K30, glucose, Composition of tryptophan and phenylalanine.

[0027] The mass percentage of fosfluconazole and filler is 1:2.5.

[0028] The mass percentage of excipient, stabilizer and povidone K30 is 2:0.8:1.2.

[0029] The preparation method of fos fluconazole freeze-dried preparation composition, the preparation steps are as follows:

[0030] 1) Add fosfluconazole and the filler to water for injection 8 times the weight of the filler, stir and blend, add the composition of absolute ethanol and acetone dropwise during the stirring process, and then add 2 times the weight of the filler Water for injection in parts by weight, stirred evenly and then adding a pH regulator to adjust the pH to 8.5 to obtain an aqueous solution of fluconazole fores;

[00...

Embodiment 3

[0034] A composition of fosfluconazole freeze-dried formulations, comprising the composition of fosfluconazole, molar ratio of absolute ethanol and acetone of 2.5:1, phosphate buffer, povidone K30, sorbitol and mannitol , aspartic acid.

[0035] The mass percentage of fosfluconazole and filler is 1:3.2.

[0036] The mass percentage of excipient, stabilizer and povidone K30 is 1.6:0.9:1.2.

[0037] The preparation method of fos fluconazole freeze-dried preparation composition, the preparation steps are as follows:

[0038] 1) Add fosfluconazole and the filler to water for injection 8 times the weight of the filler, stir and blend, add the composition of absolute ethanol and acetone dropwise during the stirring process, and then add 2 times the weight of the filler Water for injection in parts by weight, stirred evenly and then adding a pH regulator to adjust the pH to 8.2 to obtain an aqueous solution of fluconazole fores;

[0039] 2) filter and sterilize the fosfluconazole ...

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Abstract

The invention provides a fosfluconazole freeze-drying preparation composition and a preparing method thereof. The fosfluconazole freeze-drying preparation composition is prepared from fosfluconazole, a filling agent and a pH regulator, wherein the mass ratio of fosfluconazole to the filling agent is 1:(2.5-3.5), the filling agent is composed of an excipient, a stabilizer and povidone K30, and the excipient is one or a composition of two or more of glucose, glucan, trehalose, sucrose, gelatin, sorbitol and mannitol. By preparing fosfluconazole into the freeze-drying preparation with good stability, the degradation rate is greatly inhibited, the freeze-drying preparation can be stored for 3 years or longer in the normal-temperature state, and the practicability of fosfluconazole is improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a freeze-dried preparation composition of fosfluconazole and a preparation method thereof. Background technique [0002] Fosfluconazole (fosfluconazole, formula I) is a monophosphate prodrug of fluconazole (formula IV), which converts the tertiary alcohol in fluconazole into a phosphate ester, not only does not introduce a chiral center, but also increases water solubility , thereby overcoming the long-standing defect of fluconazole infusion volume caused by low water solubility. After intravenous administration, it is hydrolyzed into fluconazole under the action of phosphatase in the body to exert pharmacological effects. Fos fluconazole was developed by the Central Research Institute of Huiduan Corporation of the United States and was launched in Japan on January 15, 2004. It is used for the treatment of deep infections caused by Candida and cryptococcus, s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/675A61K47/32A61P31/10
CPCA61K31/675A61K9/19A61K47/32
Inventor 赵冬生方从彬方存杰孙明哲孙延标徐奎
Owner 合肥美利康医药技术股份有限公司
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