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Resolution agent of palonosetron hydrochloride optical isomer and separation and detection method

A technology of optical isomers and palonosetron, which is applied in the field of pharmaceutical analysis, can solve problems such as unsatisfactory, high cost, and low cost of ordinary chromatographic columns, and achieve the effects of saving consumables, reducing application costs, and effectively separating

Active Publication Date: 2017-11-07
康龙化成(南京)临床医学研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] First, the separation degree needs to be improved: the separation degree of palonosetron hydrochloride and RS isomer is 2.6, the separation degree of RS isomer and SR isomer is 1.2, and the separation degree of SR isomer and RR isomer 1.0, the separation degree of RS isomer and SR isomer, and the separation degree of SR isomer and RR isomer are less than 1.5, which is not ideal;
[0008] Second, the cost is high: one of the above-mentioned chiral chromatographic columns is at least 10,000 yuan, and the service life of the chiral chromatographic column is short. After a project is completed, the cost of the optical chromatographic column will be more than 100,000 to 200,000 yuan, which increases the cost of research and development
However, the cost of ordinary chromatographic columns is very low. A domestic ordinary reversed-phase high-performance liquid chromatography column only costs one or two thousand yuan. A project consumes 20 chromatographic columns, and the cost of the chromatographic column is only 30,000-40,000.

Method used

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  • Resolution agent of palonosetron hydrochloride optical isomer and separation and detection method
  • Resolution agent of palonosetron hydrochloride optical isomer and separation and detection method
  • Resolution agent of palonosetron hydrochloride optical isomer and separation and detection method

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Experimental program
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Effect test

Embodiment 1

[0035] The determination of optical isomers in the palonosetron hydrochloride of embodiment 1

[0036] 1. Experimental materials

[0037] Shimadzu LC-20A high performance liquid chromatography;

[0038] CPA225D electronic balance (Beijing Sartorius Instrument System Co., Ltd.);

[0039] Chromatographic column: ZORBAX SB-C18 column (Agilent);

[0040] Palonosetron hydrochloride raw materials were purchased from Qilu Pharmaceutical Co., Ltd. Palonosetron hydrochloride, RR, SR, and RS reference substances were purchased from Kunming Jida Pharmaceutical Co., Ltd. The chemical structure is as follows: figure 1 shown;

[0041] Methanol, isopropanol, and oxalic acid are all chromatographically pure, water is deionized water, and other reagents are analytically pure.

[0042] 2. Experimental methods and results

[0043] 1. Solution preparation

[0044]Resolution determination solution: Weigh 10 mg each of the RS isomer reference substance, SR isomer reference substance, and RR i...

Embodiment 2

[0069] Embodiment 2 comparative example, using common methanol-water elution

[0070] 1. Solution preparation

[0071] Resolution determination solution: Weigh 10 mg each of the RS isomer reference substance, SR isomer reference substance, and RR isomer reference substance, weigh them accurately, add methanol to dissolve and dilute to 10 mL, and shake well. Accurately weigh 50mg of palonosetron hydrochloride, put it in a 50mL measuring bottle, then accurately measure 1mL of the above-mentioned isomer solutions respectively and put them in the same 50mL measuring bottle, add methanol to dissolve and dilute to the scale, shake well to get .

[0072] Test solution: Accurately weigh 50mg of palonosetron hydrochloride, put it in a 50mL measuring bottle, add methanol to dissolve and dilute to the mark, shake well, and you get it.

[0073] 2. Chromatographic conditions

[0074] Chromatographic column: Agilent ZORBAX SB-C18 chromatographic column (250mm×4.6mm, 5μm);

[0075] Mobil...

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Abstract

The invention discloses a resolution agent of a palonosetron hydrochloride optical isomer and a separation and detection method. The palonosetron hydrochloride optical isomer is prepared from palonosetron hydrochloride as well as an RS isomer, an RR isomer and an SR isomer of the palonosetron hydrochloride; liquid chromatography is adopted, a stationary phase of the liquid chromatography is octadecyl silane bonded silica gel, a mobile phase is methyl alcohol-water, and isoamyl alcohol and oxalic acid which are in effective concentrations are added; the volume percentage concentration of isopropanol in the mobile phase is 0.4 to 0.8 percent, the mass volume concentration of the oxalic acid is 0.4 to 0.6 percent, and the isopropanol and the oxalic acid are added in methyl alcohol or water or a mixed solvent of the methyl alcohol and water. By adopting the separation and detection method provided by the invention, effective separation of the palonosetron hydrochloride optical isomer can be realized on a common C18 chromatographic column, the application cost is remarkably reduced, and the cost of a large of supplies of the chromatographic column can be saved.

Description

technical field [0001] The invention belongs to the field of drug analysis and relates to the separation and detection of chiral isomers, in particular to a separation reagent and a separation and detection method for palonosetron hydrochloride optical isomers. Background technique [0002] Palonosetron hydrochloride is a highly efficient and highly selective 5-HT3 receptor antagonist developed by MGI Pharma and Helsinn Healthcare in Switzerland. It was first approved for marketing in the United States in July 2003 and is used clinically for radiotherapy and chemotherapy. Acute and delayed nausea and vomiting. It has attracted much attention because of its high curative effect, low toxicity and side effects, long half-life, and small dosage (Palonosetron for the prevention of chemotherapy-induced nausea and vomiting: approval and efficacy, Cancer Manag Res, 2009). [0003] There are 2 chiral carbons in the structure of palonosetron hydrochloride, which can produce 4 isomers...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N30/02
CPCG01N30/02
Inventor 陈云陈昊王斌
Owner 康龙化成(南京)临床医学研究有限公司
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