Simultaneous quantification of carvedilol and its metabolites in rat plasma by ultra performance liquid chromatography tandem mass spectrometry and pharmacokinetic application

Li, Junwei; Wang, Li; Wang, Shuanghu; Chen, Mengchun; Gu, Er-min; Hu, Guoxin; Ge, Ren‐Shan

doi:10.1016/j.jchromb.2014.10.037

Cited by 13 publications

(5 citation statements)

References 36 publications

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“…Compared with the outstanding identification ability of TOF‐MS for unknown metabolites, TQ‐MS coupled with UHPLC is extremely suitable for detecting the known metabolites at trace level in complex biological samples since its high sensitivity, especially when using the most sensitive scan type MRM. Surprisingly, in this study, UHPLC–TQ‐MS used to identify the unknown metabolites of ( R )‐bambuterol got a fairly good result with eight metabolites identified.…”

Section: Resultsmentioning

confidence: 99%

“…At present, UHPLC–MS/MS is a powerful tool for the study of drug metabolism due to the benefits of structure identification and the superior sensitivity and specificity . The triple quadrupole mass spectrometer (TQ‐MS) with multiple reaction monitoring (MRM) mode is well known for its super sensitivity, which is extremely suitable for detecting the expected metabolites at trace levels in complex biological samples . On the other hand, Q‐TOF‐MS coupled with an automated MS E mode, on account of pronounced advantage of high resolution and superior selectivity, is an accurate and reliable tool for the rapid identification of expected or unexpected drug metabolites .…”

Section: Introductionmentioning

confidence: 99%

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In vivo metabolism study of (R)‐bambuterol in humans using ultra high performance liquid chromatography with tandem mass spectrometry

Zhou

Zhang

Zhao

et al. 2016

J of Separation Science

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(R)-Bambuterol, a selective β2-adrenoceptor agonist, has been approved as a new drug for the treatment of asthma and chronic obstructive pulmonary disease by the China Food and Drug Administration and is currently under phase I clinical trials. In this study, a combined method based on ultra high performance liquid chromatography with triple quadrupole mass spectrometry and ultra high performance liquid chromatography with quadrupole time-of-flight mass spectrometry was employed for the identification of the major metabolites of (R)-bambuterol in human plasma and urine after an oral dose of 10 mg. The metabolites were separated by gradient elution program and different sample preparation methods were compared. Totally, 12 metabolites of (R)-bambuterol were identified, including four metabolites in plasma and all 12 metabolites in urine. Among these, four metabolites are reported for the first time. The possible metabolic pathways of (R)-bambuterol were subsequently proposed. The results indicated that (R)-bambuterol was metabolized via hydrolysis, demethylation, oxygenation, glucuronidation, and sulfation pathways in vivo. This study revealed that this combined method was accurate and sensitive to identify the possible metabolites and to better understand the metabolism of (R)-bambuterol in vivo.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

In vivo metabolism study of (R)‐bambuterol in humans using ultra high performance liquid chromatography with tandem mass spectrometry

Zhou

Zhang

Zhao

et al. 2016

J of Separation Science

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“…This makes it usefull for the treatment of hypertension and angina pectoris [2,3]. However, preliminary data suggest that it is a strong β-adrenergic antagonist but a weak vasodilator [4].…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of carvedilol-loaded solid lipid nanoparticles for targeted drug delivery

Kipriye¹,

Şenel²,

Yenilmez³

2017

Trop. J. Pharm Res

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“…A literature survey revealed several methods for the quantitation of MET either alone (Ben-Hander, Makahleh, Saad, & Saleh, 2013;Hsieh, Galviz, & Hwa, 2009;Michel, Gaunt, Arnason, & El-Aneed, 2015;Nielsen, Christensen, & Brosen, 2014;Zhang et al, 2012) or with other antidiabetic drugs ( AbuRuz, Millership, & McElnay, 2005;Attimarad, Nair, & Aldhubaib, 2015;Ben-Hander, Makahleh, Saad, Saleh, & Cheng, 2015;Li, Deng, Qin, Yu, & Li, 2013;Mistri, Jangid, & Shrivastav, 2007; Mohamed, Mohamed, Ahmed, & Mohamed, 2015;Sharma et al, 2013;Siddiqui et al, 2013;Zhang et al, 2015;Zhong, Bi, Zhou, Chen, & Huang, 2005), in various biological matrices including human plasma (AbuRuz et al, 2005;Attimarad et al, 2015;Ben-Hander et al, 2013Li et al, 2013;Mistri et al, 2007;Nielsen et al, 2014;Zhang et al, 2015;Zhong et al, 2005), human urine (Ben-Hander et al, 2013, human serum (Siddiqui et al, 2013), rat plasma (Sharma et al, 2013;Zhang et al, 2012), dog serum (Michel et al, 2015), mouse plasma (Hsieh et al, 2009) and rabbit plasma (Mohamed et al, 2015).…”

mentioning

confidence: 99%

LC–MS/MS analysis of metformin, saxagliptin and 5‐hydroxy saxagliptin in human plasma and its pharmacokinetic study with a fixed‐dose formulation in healthy Indian subjects

Shah

Sanyal

et al. 2016

Biomedical Chromatography

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A specific and rapid liquid chromatography-tandem mass spectrometry method is proposed for the simultaneous determination of metformin (MET), saxagliptin (SAXA) and its active metabolite, 5-hydroxy saxagliptin (5-OH SAXA) in human plasma. Sample preparation was accomplished from 50 μL plasma sample by solid-phase extraction using sodium dodecyl sulfate as an ion-pair reagent. Reversed-phase chromatographic resolution of analytes was possible within 3.5 min on ACE 5CN (150 × 4.6 mm, 5 μm) column using acetonitrile and10.0 mm ammonium formate buffer, pH 5.0 (80:20, v/v) as the mobile phase. Triple quadrupole mass spectrometric detection was performed using electrospray ionization in the positive ionization mode. The calibration curves showed good linearity (r ≥ 0.9992) over the established concentration range with limit of quantification of 1.50, 0.10 and 0.20 ng/mL for MET, SAXA and 5-OH SAXA respectively. The extraction recoveries obtained from spiked plasma samples were highly consistent for MET (75.12-77.84%), SAXA (85.90-87.84%) and 5-OH SAXA (80.32-82.69%) across quality controls. The validated method was successfully applied to a bioequivalence study with a fixed-dose formulation consisting of 5 mg SAXA and 500 mg MET in 18 healthy subjects. The reproducibility of the assay was demonstrated by reanalysis of 87 incurred samples.

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Simultaneous quantification of carvedilol and its metabolites in rat plasma by ultra performance liquid chromatography tandem mass spectrometry and pharmacokinetic application

Cited by 13 publications

References 36 publications

In vivo metabolism study of (R)‐bambuterol in humans using ultra high performance liquid chromatography with tandem mass spectrometry

In vivo metabolism study of (R)‐bambuterol in humans using ultra high performance liquid chromatography with tandem mass spectrometry

Preparation and evaluation of carvedilol-loaded solid lipid nanoparticles for targeted drug delivery

LC–MS/MS analysis of metformin, saxagliptin and 5‐hydroxy saxagliptin in human plasma and its pharmacokinetic study with a fixed‐dose formulation in healthy Indian subjects

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