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Pharmaceutical composition containing echinocandin antifungal agent micafungin, its preparation method and application

一种组合物、抗真菌的技术，应用在式表示的化合物：领域

Active Publication Date: 2012-08-01
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of these two pharmaceutical compositions is not optimal

Method used

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  • Pharmaceutical composition containing echinocandin antifungal agent micafungin, its preparation method and application
  • Pharmaceutical composition containing echinocandin antifungal agent micafungin, its preparation method and application
  • Pharmaceutical composition containing echinocandin antifungal agent micafungin, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 3

[0041] Preparation of micafungin formulations

[0042] The preparation process is as follows: first dissolve the stabilizer trehalose in water or in a solution containing an optional pH regulator, then add the compound of formula I or its pharmaceutically acceptable salt to dissolve it, and set the volume to a certain volume, The solution obtained was then freeze-dried.

[0043] Different formulations can be obtained by changing the concentration of micafungin sodium and / or the concentration of trehalose, and the pH of the pH regulator. The composition of each formulation of the composition before lyophilization is as follows:

[0044]

[0045]

[0046] After each formulation was freeze-dried, the same stability investigation as described in Comparative Example 1 was carried out.

Embodiment 4

[0048] Comparison of Stability of Micafungin Preparations

[0049] After the samples of Comparative Example 1, Comparative Example 2 and Example 3 were tested for stability, the active substances were analyzed by HPLC. The analytical column used was YMC-Pack ODS-A column, specification: 250×4.6mm, S-5um , 1.2nm, column temperature: 35°C, detection at 210nm, mobile phase: hexanonitrile-phosphate buffer (pH3.0) [take 16.56g of sodium dihydrogen phosphate and 7.73g of sodium perchlorate, add water to dissolve and dilute to 1000ml , adjust the pH to 3.0 with dilute phosphoric acid (1→10)] (45:70). The content of micafungin was calculated by the external standard method.

[0050] The results of the 4-week stability investigation at 70°C are shown in the table below:

[0051]

[0052] As can be seen from the above table, the formula using trehalose as a stabilizer, especially when the weight ratio of trehalose to micafungin sodium is 100:1-1:20, preferably 20:1-1:5, obviously ...

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Abstract

The invention discloses a pharmaceutical composition containing an annular polypeptide compound micafungin of formula (I), or its salt and trehalose as a stabilizer. The pharmaceutical composition provided by the invention has good stability.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for treating and / or preventing infectious diseases. More specifically, the present invention relates to compounds represented by formula (I): [0002] [0003] or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable stabilizer, such as a pharmaceutical composition of trehalose. It is a lyophilized composition. Background technique [0004] The compound represented by formula (I) is a cyclic polypeptide compound, namely micafungin. Micafungin Sodium (Micafungin Sodium, also known as FK463, trade name: Mycamine, Japan Fujisawa Company) is the second echinocandin antifungal drug approved by the FDA after caspofungin, and its structure is as shown in formula III , derived from the fermentation product of Coleophoma empedrit by chemical modification. It was first launched in Japan in 2002, and was approved by FDA in May 2005 in the United States. Its clinical tria...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K9/19A61K47/26A61P31/10
CPCA61K38/12A61K47/26A61K31/422A61K9/19A61K9/0019A61P31/10
Inventor 洪云海薛颖季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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