Research in Pharmaceutical Sciences

ORIGINAL ARTICLE
Year
: 2022  |  Volume : 17  |  Issue : 3  |  Page : 231--241

A simple LC-MS/MS method for pharmacokinetic study of carvedilol and 4/-hydroxyphenyl carvedilol at a low dose


Wanna Eiamart1, Nantaporn Prompila2, Yaowatree Jumroen1, Nonlanee Sayankuldilok1, Pajaree Chariyavilaskul4, Supeecha Wittayalertpanya2 
1 Chula Pharmacokinetic Research Center, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand, 10330, Thailand
2 Chula Pharmacokinetic Research Center; Clinical Pharmacokinetic and Pharmacogenomic Research Unit, Department of Pharmacology, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand, 10330, Thailand

Correspondence Address:
Supeecha Wittayalertpanya
Chula Pharmacokinetic Research Center; Clinical Pharmacokinetic and Pharmacogenomic Research Unit, Department of Pharmacology, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand
Thailand

Background and purpose: The study was aimed at validating a simple, rapid, and low-cost LC-MS/MS method for carvedilol and 4/-hydroxyphenyl carvedilol assay in human plasma. The validated method was applied to investigate the pharmacokinetics after a low dose of 6.25 mg. carvedilol. Experimental approach: In this study, the plasma was extracted by liquid-liquid extraction and evaporated the organic layer to dryness, then both analytes in the residue were reconstituted and detected by LC- MS/MS. The method was validated following the guideline on bioanalytical method validation. Thirty-one healthy volunteers participated in the pharmacokinetic study. After 10 h of fasting, each volunteer received one tablet of 6.25 mg carvedilol orally. Blood samples were collected at 16 prescheduled time points. The plasma samples were analyzed for pharmacokinetics. Findings/Results: The method was linear over a range of 0.050-50.049 ng/mL for carvedilol and 0.050-10.017 ng/mL for 4/-hydroxyphenyl carvedilol. Crucial validated results reached the requirements of selectivity, accuracy, precision, and stability. Pharmacokinetics of carvedilol and 4/-hydroxyphenyl carvedilol were evaluated which showed Cmax at 21.26 ± 9.23 and 2.42 ± 2.07 ng/mL; AUC0-t 66.95 ± 29.45 and 5.93 ± 3.51 ng.h/mL; AUC0-inf 68.54 ± 30.11 and 6.78 ± 3.49 ng.h/mL; and T1/2 6.30 ± 1.95 and 6.31 ± 6.45 h, respectively. Conclusion and implications: The validated method was able to detect and quantify both analytes in plasma samples and can be applied to the pharmacokinetic study of carvedilol and 4/-hydroxyphenyl carvedilol after receiving carvedilol at 6.25 mg orally.


How to cite this article:
Eiamart W, Prompila N, Jumroen Y, Sayankuldilok N, Chariyavilaskul P, Wittayalertpanya S. A simple LC-MS/MS method for pharmacokinetic study of carvedilol and 4/-hydroxyphenyl carvedilol at a low dose.Res Pharma Sci 2022;17:231-241


How to cite this URL:
Eiamart W, Prompila N, Jumroen Y, Sayankuldilok N, Chariyavilaskul P, Wittayalertpanya S. A simple LC-MS/MS method for pharmacokinetic study of carvedilol and 4/-hydroxyphenyl carvedilol at a low dose. Res Pharma Sci [serial online] 2022 [cited 2022 Jul 2 ];17:231-241
Available from: https://www.rpsjournal.net/article.asp?issn=1735-5362;year=2022;volume=17;issue=3;spage=231;epage=241;aulast=Eiamart;type=0