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Liquid pharmaceutical composition containing echinocandin antifungal agent micafungin

A composition and antifungal technology, applied to the compound represented by the formula: , in the field of liquid pharmaceutical compositions for treating and/or preventing fungal infections, can solve the problems of long production cycle, increased risk of drug use, complicated production process and the like

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

[0006] However, the above-mentioned compositions are not ideal, they are all freeze-dried products, the production process is relatively complicated, the energy consumption of the freeze-drying process is high, the production cycle is long, and factors such as the limited freeze-drying area of ​​the freeze-dryer directly affect the production efficiency , which increases the production cost
And in the process of medication, reconstitution is required, which is not only inconvenient to operate, but also increases the risk of medication

Method used

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  • Liquid pharmaceutical composition containing echinocandin antifungal agent micafungin
  • Liquid pharmaceutical composition containing echinocandin antifungal agent micafungin
  • Liquid pharmaceutical composition containing echinocandin antifungal agent micafungin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 3

[0047] Micafungin liquid formulation preparation

[0048] Take 30ml of water, add 75μl of glacial acetic acid, and adjust the pH to 5.5 with 1M sodium hydroxide. Dissolve 12.0 g of trehalose in the buffer solution, then add 1.25 g of micafungin sodium, stir gently to dissolve, add water to 50 mL, and filter with a 0.22 μm membrane. The composition of the composition (Formulation 3) is as follows:

[0049] Micafungin Sodium 25mg / ml

[0050] Trehalose 240mg / ml

[0051] Glacial acetic acid 1.5mg / ml

[0052] NaOH Adjust to pH5.5

[0053] The prepared solution was dispensed into 10mL vials at a rate of 2.5mL / bottle, fully stoppered, and capped. The resulting liquid product was subjected to the same stability investigation as that of Comparative Example 1.

Embodiment 4

[0055] Micafungin liquid formulation preparation

[0056]The preparation process is similar to Example 3, except that in the preparation process, the stabilizing agent is selected between trehalose, sucrose, lactose or maltose, and the pH regulator used is selected between acetate, phosphate or citrate , even do not add any additional pH regulator, thus obtaining different formulations, the composition of each composition formulation is as follows:

[0057]

[0058] The composition of each formulation was also subjected to the stability investigation described in Comparative Example 1.

Embodiment 5

[0060] Micafungin liquid formulation preparation

[0061] After the samples of Comparative Example 1, Comparative Example 2, Example 3 and Example 4 were tested for stability, the active substances were analyzed by HPLC.

[0062] The results of the 4-week stability investigation at 70°C are shown in the table below:

[0063]

[0064] As can be seen from the above table, the liquid formulation using trehalose, sucrose, lactose or maltose or a combination thereof as a stabilizer, and the weight ratio of the stabilizer to micafungin sodium is 100:1-1:20, preferably 20: In the case of 1-1:5, it has good stability. The HPLC analysis chromatogram of formula 1 and 6 is attached Figure 1-4 .

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Abstract

The invention discloses a liquid pharmaceutical composition containing echinocandin antifungal agent micafungin, wherein the pharmaceutical composition containing carbohydrate as a stabilizer. The pharmaceutical composition provided by the invention has good stability.

Description

technical field [0001] The present invention relates to liquid pharmaceutical compositions for the treatment and / or prevention of fungal infections. More specifically, the present invention relates to compounds represented by formula (I): [0002] [0003] Or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable amount of stabilizer, such as monosaccharide, disaccharide or polysaccharide, or a composition thereof, preferably lactose, sucrose, maltose, trehalose or a composition thereof. It is a liquid 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 modificat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K9/00A61K47/26A61P31/10
CPCA61K31/42A61K47/26A61K31/422A61K38/12A61K9/0019A61P31/10
Inventor 洪云海薛颖季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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