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Caspofungin preparation with low impurity content and preparation method and application thereof

一种杂质、含量的技术，应用在治疗和/或预防真菌感染的药用组合物领域，能够解决患者安全性隐患、降解杂质未进行有效的严格控制、不现实等问题

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

[0010] Impurities in active pharmaceutical ingredients such as those in caspofungin are undesirable and may even pose safety concerns for patients
However, it is unrealistic to completely remove these impurities, so reducing the limit of these impurities is a key focus of drug formulation developers
[0011] Yet each disclosed pharmaceutical composition is not the most ideal formula, and they have not carried out effective strict control to the RRT1.35 degradation impurity of caspofungin

Method used

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  • Caspofungin preparation with low impurity content and preparation method and application thereof
  • Caspofungin preparation with low impurity content and preparation method and application thereof
  • Caspofungin preparation with low impurity content and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0136] Caspofungin HPLC analysis method:

[0137] High performance liquid chromatography: WATERS 2695-2998

[0138] Analytical column: YMC-Pack ODS-A column, specification: 250×4.6mm, S-5um, 1.2nm

[0139] Column temperature: 35°C

[0140] Detection wavelength: 220nm

[0141] Mobile phase: A: 0.1% perchloric acid (analytical pure, Shanghai Jinlu Chemical Co., Ltd.) and 0.075% sodium chloride (analytical pure, Sinopharm Chemical Reagent Co., Ltd.) solution (get perchloric acid 1.0ml and chlorine Sodium chloride 0.75g, add water to dissolve and dilute to 1000ml);

[0142] B: Acetonitrile (HPLC grade, TEDIA).

[0143] The gradient conditions are shown in the table below:

[0144] time (minutes)

A％

B％

initial

65.5

34.5

14.5

65.5

34.5

[0145] 35

50

50

45

35

65

50

20

80

52

20

80

53

65.5

34.5

66 ...

Embodiment 1

[0184] Preparation of caspofungin pharmaceutical composition

[0185] The preparation process is as follows: first dissolve the carbohydrate protecting agent and glycine (or other amino acids) 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, Dilute to a certain volume, and then lyophilize the solution obtained above.

[0186] Different formulations can be obtained by changing the concentration of caspofungin and / or the concentration of carbohydrate protecting agent and / or glycine (or other amino acids), and the pH or concentration of pH regulator. The composition of each formulation of the composition before lyophilization is as follows:

[0187]

[0188]

[0189]

[0190] Each freeze-drying procedure is as follows:

[0191] Freeze-drying procedure A:

[0192] a. The shelf temperature drops to -40°C at a rate of 1°C / min;

[0193] b. The shelf temperature is mai...

Embodiment 2

[0255] Get 0.75g sorbitol, 0.5g mannitol, dissolve in 20ml of water, then add 1.05g of caspofungin base, then add sodium dihydrogen phosphate, until its final constant volume concentration is 20mM, and adjust the pH to 6.0, add water to make up to 25mL final volume. Then through a 0.22 μm membrane filter, the composition of the composition (formulation 22) before freeze-drying is as follows:

[0256]

[0257] Fill vials at 1.25ml / bottle and lyophilize.

[0258] The freeze-dried products were placed at 40°C for stability inspection, and samples were taken for HPLC analysis after 8 weeks and 24 weeks, respectively, and stability inspections were carried out at 25°C, 65% RH and 2-8°C, and respectively Samples were taken after 24 weeks for HPLC analysis (including data at time 0).

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Abstract

The invention discloses a caspofungin medicinal composition with low impurity content, and discloses a method for preparing the caspofungin medicinal composition with low impurity content. The caspofungin medicinal composition provided by the invention has high stability.

Description

technical field [0001] The invention relates to a pharmaceutical composition for treating and / or preventing fungal infection, and also relates to a preparation method of the pharmaceutical composition. Background technique [0002] Echinocandin, also known as echinocandin, is a new type of antifungal drug, belonging to the acetylhexacyclic class, and is a drug composition for inhibiting glucan synthase, which non-competitively inhibits the -β(1 , 3) The synthesis of -D-glucan plays 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. [0003] Caspofungin (caspofungin) is the first product of echinocandin antifungal drugs, and its structure is as formula I, [0004] [0005] It has broad-spectrum antifungal activity, and has good antifungal activity against Candida albicans, non-Candida albicans and fungi of the genus Aspergill...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K47/18A61K47/26A61K47/36A61P3/10A61K38/08
CPCA61K47/18A61K38/08A61K47/42A61K9/19A61K47/26A61K38/12C07K7/56A61K31/10A61K47/36A61P31/04A61P31/10A61P3/10
Inventor 洪云海薛颖沙丽新季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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