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Echinocandin antifungal agent caspofungin containing medicinal composition, a preparation method and application thereof

A composition and antifungal technology, which is applied in the direction of antifungal agents, medical preparations with non-active ingredients, pharmaceutical formulations, etc., and can solve problems such as not providing stability

Active Publication Date: 2012-06-13
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The freeze-dried composition of Example 4 with the best stability performance was tested for 12 weeks at 2-8° C., and the relative peak area of ​​caspofungin % at 0 o’clock and 12 weeks was about 99.55% and about 99.50% respectively. %, but does not provide data reflecting the stability of the composition at higher temperatures

Method used

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  • Echinocandin antifungal agent caspofungin containing medicinal composition, a preparation method and application thereof
  • Echinocandin antifungal agent caspofungin containing medicinal composition, a preparation method and application thereof
  • Echinocandin antifungal agent caspofungin containing medicinal composition, a preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0088] Caspofungin formulation preparation

[0089] The preparation process is as follows: first dissolve the stabilizer sucrose 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, set the volume to a certain volume, and then Lyophilization was carried out.

[0090] Different formulations are obtained by varying the concentration of caspofungin and / or the concentration of sucrose, and the pH or concentration of the pH adjuster. The composition of each formulation of the composition before lyophilization is as follows:

[0091]

[0092]

[0093] After each formulation was freeze-dried, the same stability investigation as described in Comparative Example 1 was carried out.

Embodiment 3

[0095] Caspofungin formulation stability

[0096] After the samples of Comparative Example 1 and Example 2 were tested for stability, the active substances were analyzed by HPLC.

[0097] The results of the 40°C stability test are shown in the table below:

[0098]

[0099] The results of the stability test at 30°C are shown in the table below:

[0100]

[0101] The results of the stability test at 2-8°C are shown in the table below:

[0102]

[0103]

[0104] By comparing the above stability test data, it can be seen that each formulation is very stable at 2-8°C, and the content of caspofungin does not decrease significantly after 12 weeks and 24 weeks. The 2-8°C stability data provided by the present invention is carried out on the basis of the raw material medicine produced by our company, wherein the raw material medicine contains process impurities such as RRT0.95 (relative retention time is 0.95), which has a high degree of stability in stability. There wi...

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Abstract

The invention discloses an echinocandin antifungal agent caspofungin containing medicinal composition, which contains cane sugar used as an excipient. The medicinal composition provide by the invention has good stability.

Description

technical field [0001] The present invention relates to pharmaceutical compositions for the treatment and / or prevention of fungal infections. More specifically, the present invention relates to compounds of formula I: [0002] [0003] Or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable amount of excipient sucrose. It is a lyophilized composition. Background technique [0004] Echinocandin, also known as echinocandin, is a new type of antifungal drug, belonging to the acetylhexacyclic group, and is a glucan synthase inhibitor, which non-competitively inhibits the -β(1,3) of the fungal cell wall -D-glucan synthesis to play a bactericidal effect. Dextran is a fungal cell wall polysaccharide and an important component of the cell wall, which can maintain the integrity of the cell wall and stabilize its osmotic pressure. [0005] Caspofungin (caspofungin) (Caseis, Merck & Co.) is the first listed product of echinocandin antifungal drugs, and i...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61K9/19A61K47/26A61P31/10
Inventor 洪云海薛颖季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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