Method for determining concentration of loxoprofen and trans-hydroxyl matrix thereof in plasma

Abstract

The invention discloses a method for determining concentration of loxoprofen and trans-hydroxyl matrix thereof in plasma, which includes the steps pf preparation of reserve solution, preparation of working solution, preparation of standard curve and quality control sample, sample pretreatment method and LC-MS / MS analysis.The method establishes a simple, rapid, durable, high-sensitivity and good-selectivity LC-MS / MS method for simultaneously determining concentration of loxoprofen and the active metabolite trans-OH thereof in EDTA-K2 anticoagulated human plasma, which can be used for simultaneous quantitative analysis of loxoprofen and trans-OH loxoprofen in EDTA-K2 anticoagulated human plasma. Compared with fluorescence method and ultraviolet detection method, the method provided by the invention is more sensitive, whereby the quantitative lower limit of loxoprofen is reduced from 0.31 mg / mL and 0.20 mg / mL to 0.050 mg / mL, and the quantitative lower limit of the trans-OH loxoprofen is reduced to from 0.31 mg / mL and 0.20 mg / mL 0.010 mg / mL, and meanwhile, the analysis time is greatly shortened from 25 min and 30 min to 3.5 min.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a method for measuring the concentration of loxoprofen and its trans hydroxyl form in blood plasma. Background technique [0002] Loxoprofen sodium is a non-steroidal anti-inflammatory analgesic, which has significant analgesic, anti-inflammatory and antipyretic effects, especially has a strong analgesic effect. As a new type of non-steroidal anti-inflammatory drug, Loxoprofen The difference between profen sodium and other drugs is that the drug is a prodrug, which has no activity itself, and becomes active after being rapidly converted into trans-OH body by the liver, so it can reduce the damage to the gastrointestinal tract. [0003] At present, the studies of drug pharmacokinetics and bioequivalence are all evaluated by measuring the pharmacokinetic parameters of the drug. Therefore, the determination of the concentration of loxoprofen and its active metabolite trans-OH in...

AI Technical Summary

Problems solved by technology

[0003] At present, the studies of drug pharmacokinetics and bioequivalence are all evaluated by measuring the pharmacokinetic parameters of the drug. Therefore, the determination of the concentration of loxoprofen and its active metabolite trans-OH in plasma is very important for loxoprofen. The development of new drugs for fen sodium is extremely important. In addition to the trans-OH, the metabolites of loxoprofen also have a cis-OH body. The two metabolites are enantiomers. Separate them by chromatography and mass spectrometry; in addition, the concentrations of loxoprofen and trans-OH forms in human plasma vary greatly, and there are few bioanalytical methods for simultaneously quantifying the concentrations of loxoprofen and trans-OH forms in human plasma According to reports, at present, the quantitative analysis method that can simultaneously determine the plasma concentration of loxoprofen and its active metabolite trans-OH is mainly based on HPLC method, and LC-MS / MS method has not been reported.

[0004] So far, there are two HPLC methods that can simultaneously measure the concentration of loxoprofen and its active metabolite trans-OH in plasma, namely fluorescence method and ultraviolet detection method. Although these two methods have achieved the separation of cis-OH However, the pretreatment process is very complicated, and the sensitivity is low, the linear range is narrow, and the analysis time is long, which cannot meet the needs of rapid analysis of large batches of samples.

Images