Development and validation of a high throughput LC–MS/MS method for simultaneous quantitation of pioglitazone and telmisartan in rat plasma and its application to a pharmacokinetic study

Sengupta, Pinaki; Chatterjee, Bappaditya; Mandal, Uttam Kumar; Gorain, Bapi; Pal, Tapan Kumar

doi:10.1016/j.jpha.2017.05.004

Cited by 31 publications

(23 citation statements)

References 25 publications

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“…The acceptance criteria for accuracy study were ±15% of nominal concentration (Mahmood, Sengupta, Mandal, Chatterjee, & Taher, ). For LLOQ, the acceptable limit of deviation was set at ±20% (Sengupta, Chatterjee, Mandal, Gorain, & Pal, ).…”

Section: Methodsmentioning

confidence: 99%

Drug development and bioanalytical method validation for a novel anticancer molecule, 4‐(dimethylamino)‐2‐(p‐tolylamino) thiazole‐5‐carbonitrile

Biswas

Shard

Patel

et al. 2018

Drug Development Research

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Hit, Lead & Candidate Discovery The thiazole ring system represents a significant building block that exists in many biologically active natural products and clinically successful anticancer drugs. Modifications of the thiazole core have been a proven and highly effective method in improving anticancer potency. We designed a novel thiazole‐based molecule, 4‐(dimethylamino)‐2‐(p‐tolylamino) thiazole‐5‐carbonitrile, which showed potent in vitro anticancer effect against targeted Bcl‐2 Jurkat cell‐line quantified using 3‐(4, 5‐dimethythiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide (MTT) assay. Physicochemical parameters (pKa, LogP, LogD) of the molecule have also been evaluated as a part of the drug development process. Moreover, a rapid Reverse phase‐high performance liquid chromatography (RP‐HPLC) bioanalytical method has been developed to quantitate the molecule in human plasma. The method has been validated following the United States Food and Drug Administration bioanalytical method validation guideline. The stability studies showed no significant instability of the analyte in respective stability conditions (6 hr autosampler, 8 hr bench top, 30 days long‐term, and 3 freeze–thaw cycles). The molecule was found to be stable for 3 hr in human plasma. The molecule was shown to have high plasma protein binding affinity. It showed favorable pKa (11), Log P (3.01), Log D (2.96), and plasma protein binding (90%) values toward its further exploitation as a lead anticancer candidate molecule. The developed bioanalytical method can be used for quantifying the molecule in different pharmacokinetic, toxicokinetic, or other clinical trial samples involving human plasma during development process or in routine bioavailability and bioequivalence study after its regulatory approval.

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Section: Methodsmentioning

confidence: 99%

Drug development and bioanalytical method validation for a novel anticancer molecule, 4‐(dimethylamino)‐2‐(p‐tolylamino) thiazole‐5‐carbonitrile

Biswas

Shard

Patel

et al. 2018

Drug Development Research

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“…Selectivity of the developed method was determined after injecting the blank plasma samples taken separately from six different rats. The chromatographic nature of blank was compared with the lower limit of quantitation (LLOQ) samples for detecting the presence of any co‐eluting peaks at the retention time of the three analytes (ABP, LCZ and PRN) and IS (Sengupta, Chatterjee, Mandal, Gorain, & Pal, ; US Department of Health and Human Services, US Food and Drug Administration and Center for Veterinary Medicine, ).…”

Section: Methodsmentioning

confidence: 99%

Simultaneous bioanalysis and pharmacokinetic interaction study of acebrophylline, levocetirizine and pranlukast in Sprague–Dawley rats

Lohar

Sharma

Sahu

et al. 2019

Biomedical Chromatography

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The combination of acebrophylline (ABP), levocetirizine (LCZ) and pranlukast (PRN) is used to treat allergic rhinitis, asthma, hay-fever and other conditions where patients experience difficulty in breathing. This study was carried out with the aim of developing and validating a reverse-phase high-performance liquid chromatographic bioanalytical method to simultaneously quantitate ABP, LCZ and PRN in rat plasma.The objective also includes determination of the pharmacokinetic interaction of these three drugs after administration via the oral route after individual and combination treatment in rat. Optimum resolution between the analytes was observed with a C 18 Kinetex column (250 mm × 4.6 mm × 5 μm). The chromatography was performed in a gradient elution mode with a 1 mL/min flow rate. The calibration curves were linear over the concentration range of 100-1600 ng/mL. The intra-and inter-day precision and accuracy were found to be within acceptable limits as specified in US Food and Drug Administration guideline for bioanalytical method validation. The analytes were stable on the bench-top (8 h), after three freeze-thaw cycles, in the autosampler (8 h) and as a dry extract (−80°C for 48 h). The statistical results of the pharmacokinetic study in Sprague-Dawley rats showed a significant change in pharmacokinetic parameters for PRN upon co-administration of the three drugs.

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“…Acceptance limit for average value was +15% of the theoretical concentration except at LLOQ, where it should be within +20%. 20,23…”

Section: Chromatographic Conditionsmentioning

confidence: 99%

Development and Validation of a Simultaneous Bioanalytical Method for Methotrexate, Sulfasalazine and Hydroxychloroquine in Rat Plasma following Single Step Protein Precipitation Technique

Reddy¹,

Sahu²,

Sharma³

et al. 2020

IJPER

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Background: Triple therapy of methotrexate, sulfasalazine and hydroxychloroquine is widely used in the treatment of rheumatoid arthritis. Different studies reported the superior efficacy of combination of these three drugs in the improvement of this disease state. However, there is still a lot of scopes remains for preclinical study of this combination in future. Establishment of bioanalytical method is essential for quantitating these analytes in the samples from such types of studies. Therefore, in this study, we aim to develop a simultaneous method for quantification of methotrexate, sulfasalazine and hydroxychloroquine in rat plasma through a single run. Materials and Methods: The method includes a simple single step protein precipitation technique for extraction of all the three analytes from rat plasma with more than 84% recovery. The method was validated according to the USFDA guideline for a calibration range of 0.50-10μg/mL. Results: Overall, the method showed acceptable accuracy (92.14-116.12%) and precision (%coefficient of variation; 0.79-11.94%) at lower limit of quantification and three quality control levels. Analytes were found to be stable in all the tested stability study conditions. Conclusion: We have established a simultaneous bioanalytical method for methotrexate, sulfasalazine and hydroxychloroquine in rat plasma. Applicability of the method has been established through an oral pharmacokinetic study of the combination in rat.

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Development and validation of a high throughput LC–MS/MS method for simultaneous quantitation of pioglitazone and telmisartan in rat plasma and its application to a pharmacokinetic study

Cited by 31 publications

References 25 publications

Drug development and bioanalytical method validation for a novel anticancer molecule, 4‐(dimethylamino)‐2‐(p‐tolylamino) thiazole‐5‐carbonitrile

Drug development and bioanalytical method validation for a novel anticancer molecule, 4‐(dimethylamino)‐2‐(p‐tolylamino) thiazole‐5‐carbonitrile

Simultaneous bioanalysis and pharmacokinetic interaction study of acebrophylline, levocetirizine and pranlukast in Sprague–Dawley rats

Development and Validation of a Simultaneous Bioanalytical Method for Methotrexate, Sulfasalazine and Hydroxychloroquine in Rat Plasma following Single Step Protein Precipitation Technique

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