Caspofungin formulations

A technology of caspofungin and regulator, which is applied in the directions of antifungal agents, medical preparations with non-active ingredients, and pharmaceutical formulas, and can solve the problems of increased risk of embolism and the like

Inactive Publication Date: 2009-08-26
SANDOZ AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such sub-visible particles may, for example, lead to an increased risk of embolism in patients receiving intravenously reconstituted products

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0246] Embodiment 1 (comparison) :

[0247] Preparation of composition 1 comprising caspofungin diacetate and additional amount of acetate buffer according to example 1 of EP 0 904 098 B1

[0248] Table 1:

[0249]

[0250] A liquid formulation of Composition 1 was prepared by dissolving 5 g of mannitol and 7.5 g of sucrose in about 200 ml of water. The pH was then measured and acetic acid was added to a final concentration of 1.5 mg / ml and the pH was adjusted to pH 3.7 with 1 N NaOH. Then 11.7 g of caspofungin diacetate were added, corresponding to 46.6 mg / ml caspofungin diacetate or 42 mg / ml caspofungin calculated as base, and the pH was adjusted to pH 6.0 using 1 N NaOH. Adjust volume to 250ml with water and pass through Millex TM -GV injector-driven with Durapore TM - The solution is filtered with a membrane and a filter device with a diameter of 0.22 μm and filled with 1.25 ml each into 15 ml glass vials. The vials were partially stoppered with lyophilization st...

Embodiment 2 and 3

[0252] Preparation of Composition 2 and Composition 3 comprising caspofungin and an additional pH adjuster, namely acetic acid:

[0253] Table 2:

[0254] components

[0255] Liquid formulations of compositions 2 and 3 were prepared according to Example 1 by dissolving mannitol and sucrose using a 100 ml batch size. Subsequently 46.6 mg / ml caspofungin diacetate was added, corresponding to 42 mg / ml caspofungin base, the pH was measured at 6.59 and adjusted to pH 6.0 or pH 6.5 with 1N acetic acid, respectively. For composition 2, 0.1315 mg / ml acetic acid was added (calculated based on the final volume of the liquid formulation), corresponding to a final molar concentration of 2.19 mmol / l of additional acetic acid or a molar ratio of additional acetic acid to caspofungin of 0.0569 . After adjusting the volume with water, a pH of 6.05 was obtained. For composition 3, 0.0188 mg / ml of acetic acid was added (calculated based on the final volume of the liquid formulation)...

Embodiment 4

[0257] Preparation of composition 4 comprising caspofungin without any additional pH adjuster:

[0258] table 3:

[0259]

[0260] A 200 ml batch size liquid formulation of Composition 4 was prepared by dissolving mannitol and sucrose according to Examples 2 and 3. Then 42 mg / ml caspofungin base, ie 46.6 mg / ml caspofungin diacetate, was added without further pH adjustment. The volume was adjusted with water in a similar manner to Example 1, ie to a final volume of 200 ml, whereby a pH value of 5.96 was obtained, the solution was filtered, filled into vials and lyophilized. Redissolve and / or dilute lyophilized composition 4 in a similar manner to Example 1.

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Abstract

The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable salt of caspofungin as active ingredient being useful for the prevention and/or treatment of fungal infections. Said compositions additionally comprise specific bulking agents and small amounts or no amounts of an additional pH modifier and may be in a liquid or solid form, e.g. may be lyophilized compositions. Said compositions show good stability and reduced amounts of sub-visible particulate matter formed in solutions which are reconstituted from the lyophilized product.

Description

field of invention [0001] The present invention relates to pharmaceutical compositions comprising pharmaceutically active components for the prevention and / or treatment of fungal infections and / or conditions resulting from said infections. More specifically, the present invention relates to compositions, either liquid or solid, such as lyophilized compositions, comprising as active ingredient the compound caspofungin, specific bulking agents and little or no additional pH regulators . Background of the invention [0002] The composition of the present invention comprises as a pharmaceutically active ingredient caspofungin free base which is a compound of formula I: [0003] [0004] It is known to be an effective antifungal and antiprotozoal drug. Caspofungin, an azacyclic hexapeptide compound belonging to the echinocandin family, has a CAS registry number of 162808-62-0 and a CAS name of 1-[(4R,5S)-5-[(2-aminoethyl)amino- N 2 -(10,12-Dimethyl-1-oxotetradecyl-4-hydrox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61P31/10A61K9/19
CPCA61K9/19A61K38/12A61K47/12A61K47/26
Inventor C·韦尔茨G·斯蒂鲍尔A·施马尔达H·延内魏因I·马赫尔J·卢德谢尔
Owner SANDOZ AG
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