Simultaneous Determination of Six Coumarins in Rat Plasma and Metabolites Identification of Bergapten in Vitro and in Vivo

We developed a sensitive, simple and validated HPLC-FL method for simultaneous determination of FEB and DIC in rat plasma. The method requires a relatively small volume of sample, has simple sample preparation and excellent sensitivity.

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Simultaneous determination of vasicine and its major metabolites in rat plasma by UPLC-MS/MS and its application to in vivo pharmacokinetic studies

RSC Advances ◽

10.1039/c5ra12547b ◽

2015 ◽

Vol 5 (95) ◽

pp. 78336-78351 ◽

Cited By ~ 7

Author(s):

Wei Liu ◽

Dandan He ◽

Yudan Zhu ◽

Xuemei Cheng ◽

Hao Xu ◽

...

Keyword(s):

Simultaneous Determination ◽

Pharmacokinetic Study ◽

Rat Plasma ◽

Pharmacokinetic Studies ◽

Butyrylcholinesterase Activity

An UPLC-MS/MS method was developed to simultaneously determinate vasicine and its main metabolites and applied to the pharmacokinetic study. In addition, the anti-butyrylcholinesterase activity of component in plasma was evaluatedin vitro.

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A high throughput flow gradient LC–MS/MS method for simultaneous determination of fingolimod, fampridine and prednisone in rat plasma, application to in vivo perfusion study

Journal of Pharmaceutical and Biomedical Analysis ◽

10.1016/j.jpba.2015.11.042 ◽

2016 ◽

Vol 120 ◽

pp. 10-18 ◽

Cited By ~ 4

Author(s):

A. Suneetha ◽

K. Raja Rajeswari

Keyword(s):

Simultaneous Determination ◽

High Throughput ◽

Rat Plasma ◽

Perfusion Study ◽

Flow Gradient

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A new sensitive HPLC/UV method for simultaneous determination of paclitaxel, sorafenib and omeprazole in standard solutions and spiked plasma: Application to in-vitro and in-vivo evaluation of paclitaxel polymeric nanoformulations

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v20i9.23 ◽

2021 ◽

Vol 20 (9) ◽

pp. 1949-1959

Author(s):

Mirina Sakhi ◽

Abad Khan ◽

Ismail Khan ◽

Zafar Iqbal ◽

Sumaira Irum Khan ◽

...

Keyword(s):

Simultaneous Determination ◽

Chromatographic Method ◽

Pharmacokinetic Studies ◽

Good Resolution ◽

In Vivo Evaluation ◽

Spiked Plasma ◽

Standard Solutions

Purpose: To develop a simple, novel, sensitive and rapid reverse phase high performance liquid chromatographic method for simultaneous determination of paclitaxel, sorafenib and omeprazole in standard solutions and spiked human plasma and its application to the in-vitro and in-vivo evaluation of paclitaxel polymeric nanoparticle formulations.Methods: The method was tested for the assessment of paclitaxel, omeprazole and sorafenib using tamoxifen citrate as internal standard. The analysis was performed at a wavelength of 235 nm using Thermo HS C18 column, 40 °C column oven temperature, acetonitrile and water (70:30 v/v, pH 3.37 adjusted with phosphoric acid) as a mobile phase and at a flow rate of 0.8 ml/min. All analytes were extracted by simple protein precipitation method using acetonitrile. The linearity was assessed in the concentration range of 1 - 2000 ng/mL for paclitaxel, omeprazole and sorafenib.Results: The developed chromatographic method effectively separated omeprazole, paclitaxel, sorafenib and IS with retention time of 3.93, 5.18, 6.43 and 9.93 min, respectively. The chromatograms of the three target compounds and IS showed good resolution and peak separation. The LOD of the method was 1, 5 and. 5 ng/mL while the LOQ was 2, 7.5 and 10 ng/mL, for paclitaxel, sorafenib and omeprazole, respectively.Conclusion: The proposed RP-HPLC–UV method for the assessment of paclitaxel, sorafenib and omeprazole in standard solutions and spiked plasma is simple, economical, sensitive and robust. The method is also suitable for the analysis of paclitaxel in nanoformulations and for its pharmacokinetic studies in an animal model.

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Simultaneous Determination of Bufalin and Its Nine Metabolites in Rat Plasma for Characterization of Metabolic Profiles and Pharmacokinetic Study by LC–MS/MS

Molecules ◽

10.3390/molecules24091662 ◽

2019 ◽

Vol 24 (9) ◽

pp. 1662

Author(s):

Wenlong Wei ◽

Yang Yu ◽

Xia Wang ◽

Linhui Yang ◽

Hang Zhang ◽

...

Keyword(s):

Oral Administration ◽

Simultaneous Determination ◽

Pharmacokinetic Study ◽

Metabolic Pathways ◽

Multiple Reaction Monitoring ◽

Rat Plasma ◽

Limit Of Quantitation

Characterization and determination of metabolites to monitor metabolic pathways play a paramount role in evaluating the efficacy and safety of medicines. However, the separation and quantification of metabolites are rather difficult due to their limited contents in vivo, especially in the case of Chinese medicine, due to its complexity. In this study, an effective and convenient method was developed to simultaneously quantify bufalin and its nine metabolites (semi-quantitation) in rat plasma after an oral administration of 10 mg/kg to rats. The prototype and metabolites that were identified were subsequently quantified using positive electrospray ionization in multiple reaction monitoring (MRM) mode with transitions of m/z 387.4→369.6 and 387.4→351.3 for bufalin, m/z 513.7→145.3 for IS, and 387.4→369.6, 419.2→365.2, and 403.2→349.2 for the main metabolites (3-epi-bufalin, dihydroxylated bufalin, and hydroxylated bufalin, respectively). The method was validated over the calibration curve range of 1.00–100 ng/mL with a limit of quantitation (LOQ) of 1 ng/mL for bufalin. No obvious matrix effect was observed, and the intra- and inter-day precisions, as well as accuracy, were all within the acceptable criteria in this method. Then, this method was successfully applied in metabolic profiling and a pharmacokinetic study of bufalin after an oral administration of 10 mg/kg to rats. The method of simultaneous determination of bufalin and its nine metabolites in rat plasma could be useful for pharmacokinetic–pharmacodynamic relationship research of bufalin, providing experimental evidence for explaining the occurrence of some adverse effects of Venenum Bufonis and its related preparations.

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In Vitro, In Silico, and In Vivo Assessments of Pharmacokinetic Properties of ZM241385

Molecules ◽

10.3390/molecules25051106 ◽

2020 ◽

Vol 25 (5) ◽

pp. 1106 ◽

Cited By ~ 1

Author(s):

Jin-Ju Byeon ◽

Min-Ho Park ◽

Seok-Ho Shin ◽

Yuri Park ◽

Byeong ill Lee ◽

...

Keyword(s):

In Silico ◽

Hepatic Clearance ◽

Brain Regions ◽

Rat Plasma ◽

Pbpk Modeling ◽

Pharmacokinetic Properties ◽

Low Exposure

Parkinson’s disease is one of the most common neurodegenerative diseases. Adenosine regulates the response to other neurotransmitters in the brain regions related to motor function. In the several subtypes of adenosine receptors, especially, adenosine 2A receptors (A2ARs) are involved in neurodegenerative conditions. ZM241385 is one of the selective non-xanthine A2AR antagonists with high affinity in the nanomolar range. This study describes the in vitro and in vivo pharmacokinetic properties of ZM241385 in rats. A liquid chromatography-quadrupole time-of-flight mass spectrometric (LC-qToF MS) method was developed for the determination of ZM241385 in rat plasma. In vivo IV administration studies showed that ZM241385 was rapidly eliminated in rats. However, the result of in vitro metabolic stability studies showed that ZM241385 had moderate clearance, suggesting that there is an extra clearance pathway in addition to hepatic clearance. In addition, in vivo PO administration studies demonstrated that ZM241385 had low exposure in rats. The results of semi-mass balance studies and the in silico PBPK modeling studies suggested that the low bioavailability of ZM241385 after oral administration in rats was due to the metabolism and by liver, kidney, and gut.

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Quantitative bioanalytical LC–MS/MS assay for S130 in rat plasma-application to a pharmacokinetic study

Bioanalysis ◽

10.4155/bio-2019-0101 ◽

2019 ◽

Vol 11 (16) ◽

pp. 1469-1481 ◽

Cited By ~ 3

Author(s):

Yanping Guan ◽

Yuanyuan Fu ◽

Yao Liu ◽

Siyi Wang ◽

Man Zhao ◽

...

Keyword(s):

Rat Plasma ◽

Negative Influence ◽

Selected Reaction Monitoring ◽

Toxicological Evaluation ◽

Colorectal Cancer Cells ◽

The Us ◽

Us Fda

Aim: An innovative Atg4B inhibitor, S130, exhibited a negative influence on colorectal cancer cells in vitro and in vivo. To assist reliable toxicodynamic and pharmacokinetic evaluation, an LC–MS/MS assay of S130 in rat plasma must be necessary. Results: An LC–MS/MS assay for determination of S130 in rat plasma has been first developed and fully verified whose values met the admissible limits as per the US FDA guidelines. Chromatographic separation was achieved by using an isocratic elution after 3 min. MS was conducted under the ESI+ mode fitted with selected reaction monitoring. The calibration curve proved acceptable linearity over 0.50–800 ng/ml. Conclusion: The developed LC–MS/MS assay of S130 in rat plasma is easily applicable in pharmacokinetics study and the further toxicological evaluation.

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Hypocholesterolemic effect of emodin by simultaneous determination of in vitro and in vivo bile salts binding

Fitoterapia ◽

10.1016/j.fitote.2016.03.007 ◽

2016 ◽

Vol 110 ◽

pp. 116-122 ◽

Cited By ~ 9

Author(s):

Jiaoying Wang ◽

Jun Ji ◽

Zijing Song ◽

Wenjun Zhang ◽

Xin He ◽

...

Keyword(s):

Simultaneous Determination ◽

Bile Salts ◽

Hypocholesterolemic Effect

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A Validated HPLC-MS/MS Method for Simultaneous Determination of Militarine and Its Three Metabolites in Rat Plasma: Application to a Pharmacokinetic Study

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2019/2371784 ◽

2019 ◽

Vol 2019 ◽

pp. 1-9 ◽

Cited By ~ 2

Author(s):

Hui-Yuan Sun ◽

Lin Zheng ◽

Zi-Peng Gong ◽

Yue-Ting Li ◽

Chang Yang ◽

...

Keyword(s):

Formic Acid ◽

Simultaneous Determination ◽

Multiple Reaction Monitoring ◽

Area Under The Curve ◽

Internal Standard ◽

Rat Plasma ◽

Relative Standard ◽

Method Accuracy

A rapid, reliable, and sensitive HPLC-electrospray ionization-tandem mass spectrometry (HPLC-MS/MS) method was established and validated for simultaneous determination of militarine and its three metabolites (gastrodin, α-isobutylmalic acid, and gymnoside I) in rat plasma. Plasma was acidified with formic acid, and protein was precipitated with methanol. MS/MS with ESI and multiple reaction monitoring at m/z 725.3→457.3, 457.1→127, 304.3→107.2, 189→129, and 417.1→267.1 was used for determination of militarine, gastrodin, α-isobutylmalic acid, gymnoside I, and puerarin (internal standard), respectively. Chromatographic separation was conducted using an ACE UltraCore SuperC18 (2.1 × 100 mm, 2.5 μm) column with gradient mobile phase (0.1% formic acid in water and acetonitrile). The lower limits of quantitation for militarine, gastrodin, α-isobutylmalic acid, and gymnoside I were 1.02, 2.96, 1.64, and 0.3 ng/mL, respectively. The relative standard deviations of intra- and interday measurements were less than 15%, and the method accuracy ranged from 87.4% to 112.5%. The extraction recovery was 83.52%-105.34%, and no matrix effect was observed. The three metabolites (gastrodin, α-isobutylmalic acid, and gymnoside I) were synchronously detected at 0.83 h, suggesting that militarine was rapidly transformed to gastrodin, α-isobutylmalic acid, and gymnoside I. Moreover, the area under the curve (AUC) and Cmax of militarine were significantly lower than those of gastrodin and α-isobutylmalic acid, showing that militarine was largely metabolized to gastrodin and α-isobutylmalic acid in vivo. The studies on pharmacokinetics of militarine and its three metabolites were of great use for facilitating the clinical application of militarine and were also highly meaningful for the potential development of militarine.

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Liquid Chromatographic Method for the Simultaneous Determination of Eprosartan and Hydrochlorothiazide in Tablets and Human Plasma

Journal of AOAC International ◽

10.1093/jaoac/94.3.823 ◽

2011 ◽

Vol 94 (3) ◽

pp. 823-832 ◽

Cited By ~ 1

Author(s):

Fathalla Belal ◽

Amina M El-Brashy ◽

Nahed El-Enany ◽

Manar M Tolba

Keyword(s):

Simultaneous Determination ◽

Human Plasma ◽

Mobile Phase ◽

Hplc Method ◽

Rp Hplc ◽

Liquid Chromatographic Method ◽

Liquid Chromatographic

Abstract A new, specific, and sensitive RP-HPLC method was developed for the simultaneous determination of eprosartan (EPR) and hydrochlorothiazide (HCT). Good chromatographic separation was achieved using a 250 × 4.6 mm id, 5 μm particle size Symmetry® C18 column. The mobile phase acetonitrile–0.1 M phosphate buffer (35 + 65, v/v), pH 4.5, was pumped at a flow rate of 1 mL/min, with UV detection at 275 nm. The method showed good linearity in the ranges of 0.5–50 and 0.1–10 μg/mL, with LOD of 0.06 and 0.02 μg/mL and LOQ of 0.20 and 0.08 μg/mL for EPR and HCT, respectively. The proposed method was successfully applied for the analysis of the studied drugs in their synthetic mixture and co-formulated tablets. The method was further extended to the in vitro and in vivo determination of the two drugs in spiked and real human plasma. Interference likely to be encountered from the co-administered drugs was studied.

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