Method for determination of concentration of 5, 6-dihydro-7,8-dimethyl-4,5-dioxy-4-H-pyranoquinoline-2-carboxylic acid in plasma

A pyranquinoline and dimethyl technology, which is applied in the field of drug analysis, can solve the problem that the determination method is not reported in literature and the like, and achieve the effects of simple pretreatment method, high sensitivity and rapid method.

Inactive Publication Date: 2017-02-15
THE SECOND HOSPITAL AFFILIATED TO SUZHOU UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature report on the determination method of the active metabolite MY-1250 in plasma after oral administration of repimilast tablets or granules

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for determination of concentration of 5, 6-dihydro-7,8-dimethyl-4,5-dioxy-4-H-pyranoquinoline-2-carboxylic acid in plasma
  • Method for determination of concentration of 5, 6-dihydro-7,8-dimethyl-4,5-dioxy-4-H-pyranoquinoline-2-carboxylic acid in plasma
  • Method for determination of concentration of 5, 6-dihydro-7,8-dimethyl-4,5-dioxy-4-H-pyranoquinoline-2-carboxylic acid in plasma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Determination of MY-1250 concentration in human plasma.

[0028] 1. Experimental materials and instruments

[0029] MY-1250 reference substance: provided by Henan Furentang Pharmaceutical Co., Ltd., batch number: 20140501D; levetiracetam reference substance: provided by Zhejiang Huahai Pharmaceutical Co., Ltd., batch number: 201308-2; test water: ultrapure water Methanol: chromatographically pure (Merck Company); ammonia water, ammonium acetate: analytically pure (Sinopharm Chemical Reagent Co., Ltd.); hydrochloric acid: analytically pure (Shanghai Lingfeng Chemical Reagent Co., Ltd.).

[0030] API 4000 LC / MS / MS coupled instrument (Applied Biosystems, USA), chromatographic workstation: Analyst 1.6; Mettler XS 105DU electronic balance (Swiss Mettler company); Eppendorf Centrifuge 5424R high-speed low-temperature centrifuge (German Eppendorf company ); KDC-2042 low-speed refrigerated centrifuge (Anhui Zhongke Zhongjia Scientific Instrument Co., Ltd.); Millipor...

Embodiment 2

[0052] Example 2: Determination of MY-1250 concentration in human plasma

[0053] Referring to Example 1, 5 healthy female subjects took 150 mg of Repimilast Tablets on an empty stomach, and took them with 250 mL of warm water; 4 hours after the administration, 3 mL of peripheral venous blood was collected, injected into a heparin tube, and centrifuged (4000 r min -1 , 5min), draw 600μL of subject’s plasma sample, add 12μL of hydrochloric acid solution (5mol·L -1 ), vortexed to prepare plasma. The treatment and measurement conditions of the drug-containing plasma samples were the same, and the results showed that the MY-1250 contents in the plasma of 5 healthy female subjects after oral administration of 150 mg of Repimilast Tablets on an empty stomach were 50.24, 52.71, 41.2, 26.12, and 43.45 ng·mL, respectively. -1 .

Embodiment 3

[0054] Example 3: Determination of MY-1250 Concentration in Human Plasma

[0055] Referring to Example 1, 5 healthy male subjects took 50 mg / bag × 3 bags of Repimilast Granules on an empty stomach, and took it with 250 mL of warm water; 2 hours after administration, 3 mL of peripheral venous blood was collected, injected into a heparin tube, and centrifuged (4000 r min -1 , 5min), draw 600μL of subject’s plasma sample, add 12μL of hydrochloric acid solution (5mol·L -1 ), vortexed to prepare plasma. The treatment and measurement conditions of the drug-containing plasma samples were the same, and the results showed that the contents of MY-1250 in the plasma of 5 healthy male subjects after oral administration of 150 mg of Repimilast Granules on an empty stomach were 49.26, 107.6, 56.76, 100.7, and 124.5 ng mL respectively. -1 .

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses a method for determination of concentration of 5, 6-dihydro-7,8-dimethyl-4,5-dioxy-4-H-pyranoquinoline-2-carboxylic acid in plasma, the method uses a liquid chromatography-mass spectrometry system for the determination, and the method is as follows: first taking a to-be-tested plasma sample, adding a certain amount of an inorganic acid for acidification, adding an organic solvent into the acidified plasma sample to precipitate proteins, centrifuging at a high speed, taking supernatant to add a certain amount of deionized water for even mixing, separating by a chromatographic column, and detecting with a mass spectrometry detector. The method is rapid, accurate, high-sensitivity, simple in operation, and suitable for the determination of the concentration of the 5, 6-dihydro-7,8-dimethyl-4,5-dioxy-4-H-pyranoquinoline-2-carboxylic acid in the plasma.

Description

technical field [0001] The invention belongs to the technical field of drug analysis, and relates to an analysis and determination method for drugs in vivo, in particular to a method for determining 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4-hydro-pyridine in blood plasma Quinoline-2-carboxylic acid concentration method. Background technique [0002] Repimilast is an anti-allergic drug, which can be rapidly degreased into the active metabolite 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4-hydro-pyranoquinoline in the body -2-Carboxylic acid (also known as MY-1250), exerts anti-asthma effect by inhibiting the release of chemical mediators such as histamine, allergic slow-response substances, and platelet activating factor through MY-1250. Oral administration of repimilast to patients with bronchial asthma can inhibit the decline in lung function and skin allergic reactions caused by antigens, and it is mainly used clinically for the prevention and treatment of bronchial asthma. At present...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): G01N30/02
CPCG01N30/02
Inventor 王蒙张全英黄明宗顺麟周文佳
Owner THE SECOND HOSPITAL AFFILIATED TO SUZHOU UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap