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Detection method of chiral isomers in carfilzomib

A detection method and carfilzomib technology, applied in the field of medicine, can solve problems such as hidden safety hazards of patients, affecting the quality of carfilzomib, affecting the pharmacological activity of carfilzomib, etc., and achieving high specificity, separation and durability. Good results with high detection sensitivity

Active Publication Date: 2020-10-13
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Carfilzomib contains 5 chiral centers, with 1 enantiomer and 30 diastereoisomers. Different chiral isomers may have large differences in pharmacological activity and toxicity. Carfilzomib Rice may contain so many chiral isomers, if its content cannot be strictly controlled, it will affect the quality of carfilzomib, which in turn may affect the pharmacological activity of carfilzomib, bringing safety hazards to patients

Method used

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  • Detection method of chiral isomers in carfilzomib
  • Detection method of chiral isomers in carfilzomib
  • Detection method of chiral isomers in carfilzomib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 system suitability test

[0040] Instrument and chromatographic conditions:

[0041] High performance liquid chromatography Waters e2695 type (including e2489 detector and Empower chromatography workstation)

[0042] Chromatographic column: cellulose-tris(4-chloro-3-methylphenylcarbamate) bonded silica gel as filler (CHIRALCELOX-H, 4.6mm×250mm, 5μm)

[0043] Mobile phase: n-hexane-isopropanol-ethanol (89:5:6).

[0044] Flow rate: 1.0ml / min.

[0045] Detection wavelength: 220nm.

[0046] Column temperature: 40°C.

[0047] Running time: 20 minutes.

[0048] Diluent: mobile phase

[0049] Experimental steps:

[0050] Weigh an appropriate amount of carfilzomib, enantiomer, diastereoisomer F, and diastereoisomer G reference substance, dissolve and dilute with diluent to make each 1ml containing enantiomer and a solution of 0.01 mg of each diastereoisomer and 1.0 mg of carfilzomib, shake well, filter, and use it as a system suitability solution. In additio...

Embodiment 2

[0056] Embodiment 2 The influence of mobile phase ratio on separation effect

[0057] Instrument and chromatographic conditions:

[0058] Only adjust the ratio of mobile phase n-hexane-isopropanol-ethanol (see Table 2 for details), and refer to Example 1 for other conditions.

[0059] Experimental steps:

[0060] Under the conditions of different mobile phase n-hexane-isopropanol-ethanol ratios (please see Table 2 for details), the system suitability solution was analyzed by high performance liquid chromatography respectively, and the influence of the mobile phase ratio on the separation effect of each component was investigated. The results See Table 2 for details.

[0061] Table 2 The influence of mobile phase ratio on separation effect

[0062]

[0063]

[0064] The results show that as the polarity of the mobile phase changes within the above range, the resolution and tailing factor do not change much, the column efficiency increases, and the overall separation ef...

Embodiment 3

[0065] The influence of embodiment 3 flow velocity on separation effect

[0066] Instrument and chromatographic conditions:

[0067] Only adjust the mobile phase flow rate (please refer to Table 3 for details), and refer to Example 1 for other conditions.

[0068] Experimental steps:

[0069] Under the conditions of different flow rates (see Table 3 for details), HPLC analysis was performed on the system suitability solution respectively, and the influence of mobile phase flow rate on the separation effect of each component was investigated. The results are shown in Table 3.

[0070] Table 3 The influence of flow rate on separation effect

[0071]

[0072] The results showed that in the flow rate range of 0.9-1.1ml / min, the column efficiency decreased, the tailing factor changed little, the resolution changed little, and the overall separation effect was still good, which indicated that the method had good durability.

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Abstract

The invention relates to a normal-phase high-performance liquid chromatography detection method for detecting three chiral isomers (enantiomers, diastereoisomers F and G) in carfilzomib. Liquid chromatography adopts a chromatographic column with cellulose-tris(4-chloro-3-methylphenylcarbamate) bonded silica gel as filler; mobile phase is n-hexane-isopropanol-ethanol, n-hexane The volume ratio of ‑isopropanol‑ethanol is (87~91):(6~4):(7~5). This detection method has high sensitivity, good specificity, high accuracy and good durability, and can effectively control card Fezomi quality.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a normal-phase high-performance liquid chromatography detection method for detecting three chiral isomers in carfilzomib. Background technique [0002] Carfilzomib (Carfilzomib) is a second-generation proteasome inhibitor administered intravenously. Immunomodulators), and there is evidence that the refractory multiple myeloma with disease progression within 60 days after the completion of the last treatment was approved by the FDA on July 20, 2012. The trade name is Kyprolis, and its chemical structure is as follows: Shown: [0003] [0004] At present, the analytical method for detecting chiral isomers of carfilzomib has not been reported in the literature. [0005] Carfilzomib contains 5 chiral centers, with 1 enantiomer and 30 diastereoisomers. Different chiral isomers may have large differences in pharmacological activity and toxicity. Carfilzomib Rice may ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): G01N30/02
CPCG01N30/02G01N2030/027
Inventor 李海霞何丽娟张红芬郭文敏刘娜刘静媛白培锋
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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