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More stable nitrogen heterocyclic peptide preparation

A technology for injection preparations and excipients, which is applied in the field of azacyclohexyl peptide preparations, can solve problems such as harsh and unstable storage conditions, and hidden safety hazards for patients in drug circulation, and achieve the effect of increased stability, facilitating circulation and use

Inactive Publication Date: 2011-08-31
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of its instability, the storage conditions are harsh, which brings hidden dangers to drug circulation and patient safety.

Method used

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  • More stable nitrogen heterocyclic peptide preparation
  • More stable nitrogen heterocyclic peptide preparation
  • More stable nitrogen heterocyclic peptide preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Table 1-1 embodiment 1 composition formula

[0017] components

Dosage

Caspofungin

42mg / ml

Sorbitol

30mg / ml

Mannitol

20mg / ml

Sodium dihydrogen phosphate

20mM

sodium hydroxide

Appropriate amount, adjusted to pH 6.6

[0018] Its preparation process is as follows: in 2500ml beaker, add 75g sorbitol, 50g mannitol, 1750ml water, add caspofungin, be 42mg / ml to its final constant volume concentration, add sodium dihydrogen phosphate to its concentration and be 20mM, And the pH was adjusted to 6.6 with 1 N NaOH. Add water for injection to volume. Before filtering, add 12.5g of activated carbon to the injection, absorb pyrogen for 30 minutes under stirring, decarbonize and filter. The filtrate was filtered through a 0.22 μm titanium rod filter, and then sterilized and filtered through a 0.22 μm microporous membrane. Each bottle is filled into a 10ml glass vial with an amount of 1.25ml, freeze-dried, sto...

Embodiment 2- Embodiment 10

[0059] Embodiment 2-embodiment 10 formula is as follows

[0060]

[0061]

[0062]

[0063] The preparation process of embodiment 2-embodiment 10 is basically the same as that of embodiment 1, all are to add all excipients in 2500ml beaker earlier, 1750ml water, add caspofungin to its final constant volume concentration and be 42mg / ml , add buffer salt to its concentration, and adjust the pH to 6.6 with 1N NaOH, add water for injection to volume. Wherein in embodiment 10, benzyl alcohol and sodium thiosulfate are added after adding excipient. Before filtering, add 12.5g of activated carbon to the injection, absorb pyrogen for 30 minutes under stirring, decarbonize and filter. The filtrate was filtered through a 0.22 μm titanium rod filter, and then sterilized and filtered through a 0.22 μm microporous membrane. Each bottle is filled into a 10ml glass vial with an amount of 1.75ml, freeze-dried, stoppered, and capped to obtain caspofungin for injection. The lyophili...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations and provides a caspofungin injection preparation composition. The caspofungin injection preparation composition comprises 5 to 250 mg / ml of caspofungin or pharmaceutically available salt of the caspofungin, 5 to 150 mg / ml of excipient, 10 to 250 mM of buffer solution and an appropriate amount of sodium hydroxide or hydrochloric acid of which the pH value is regulated to be between 3.0 and 8.0, wherein the buffer solution is sulphate, citrate, phosphate, lactate or a mixture of the sulphate, the citrate, the phosphate and the lactate. The caspofungin injection preparation can be stored at room temperature, so that the stability is obviously improved, and the circulation and use of medicaments are facilitated.

Description

technical field [0001] The invention relates to an antifungal preparation, in particular to a more stable azacyclohexyl peptide preparation. Background technique [0002] Caspofungin, whose structural formula is shown in (I), has been widely used in the preparation of antifungal preparations for treatment or prevention. US Patent No. 5,552,521 discloses its preparation method. The compound itself is very unstable and prone to hydrolysis, dimerization or oxidation. [0003] [0004] Previously, tartaric acid was used as a buffer and caspofungin was made into a lyophilized formulation to maintain stability, but caspofungin was easily degraded in it. [0005] The Chinese patent with authorized notification number CN1132624C discloses a caspofungin injection preparation composition using acetate as a buffer, which has higher stability and fewer degradation products than that using tartaric acid as a buffer. According to the patent of the commercially available caspofungin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K38/16A61K47/10A61K47/12A61K47/26A61P31/10
Inventor 姚志勇支钦李新宇张健存
Owner SHENZHEN JYMED TECH
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