Related Experiment Video

Updated: Dec 20, 2025

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
08:38

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Published on: November 8, 2015

17.3K

Simultaneous determination of canrenone, digoxin and tolvaptan by UHPLC-MS/MS: application in heart failure patients

Peng Guo1, Qiucheng Liang2, Juntao Zheng1

  • 1Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou City, Guangdong Province 510006, PR China.

Bioanalysis
|May 30, 2020
PubMed

Insights

A new UHPLC-MS/MS method accurately measures canrenone, digoxin, and tolvaptan in human plasma. This assay supports crucial drug-drug interaction studies for heart failure patients on combined medications.

Area of Science:

  • Pharmacology
  • Analytical Chemistry
  • Clinical Pharmacology

Background:

  • Heart failure patients often receive multiple medications, including digoxin and diuretics like spironolactone and tolvaptan.
  • Understanding drug-drug interactions (DDIs) is critical for optimizing treatment efficacy and patient safety in this population.
  • Simultaneous quantification of these drugs and their metabolites is essential for DDI studies.

Purpose of the Study:

  • To develop and validate a rapid Ultra-High-Performance Liquid Chromatography-tandem Mass Spectrometry (UHPLC-MS/MS) assay.
  • To enable simultaneous determination of canrenone (spironolactone's active metabolite), digoxin, and tolvaptan in human plasma.
  • To support research into drug-drug interactions involving these commonly co-prescribed medications.

Main Methods:

  • Established a UHPLC-MS/MS method for simultaneous analysis of canrenone, digoxin, and tolvaptan.
  • Achieved chromatographic separation using a 4-minute isocratic elution.
  • Performed mass analysis via positive electrospray ionization; validated per CFDA guidelines.

Main Results:

  • Successfully developed and validated a UHPLC-MS/MS method for simultaneous quantification.
  • Established linear calibration curves ranging from 1.0-400.0 ng/ml for canrenone and tolvaptan, and 0.1-40.0 ng/ml for digoxin.
  • The method demonstrated feasibility for detecting drug concentrations in human plasma.

Conclusions:

  • The developed UHPLC-MS/MS method is suitable for simultaneous determination of canrenone, digoxin, and tolvaptan.
  • This assay provides a valuable tool for pharmacokinetic and drug-drug interaction studies in heart failure patients.
  • The method's efficiency supports clinical research and therapeutic drug monitoring.

Keywords:
UHPLC–MS/MScanrenonedigoxindrug–drug interactionsheart failuretolvaptan

More Related Videos

Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice08:57

Sample Extraction and Simultaneous Chromatographic Quantitation of Doxorubicin and Mitomycin C Following Drug Combination Delivery in Nanoparticles to Tumor-bearing Mice

Published on: October 5, 2017

11.3K
Optimized LC-MS/MS Method for the High-throughput Analysis of Clinical Samples of Ivacaftor, Its Major Metabolites, and Lumacaftor in Biological Fluids of Cystic Fibrosis Patients06:14

Optimized LC-MS/MS Method for the High-throughput Analysis of Clinical Samples of Ivacaftor, Its Major Metabolites, and Lumacaftor in Biological Fluids of Cystic Fibrosis Patients

Published on: October 15, 2017

8.6K

Related Concept Videos

Determination of Multiple Dosing Parameters: Steady-State, Minimum and Maximum Concentrations01:15

Determination of Multiple Dosing Parameters: Steady-State, Minimum and Maximum Concentrations

Gentamicin, an aminoglycoside antibiotic, is commonly administered via intermittent intravenous infusion to treat severe infections. An intermittent one-hour infusion of gentamicin, administered at eight-hour intervals, allows for precise control of plasma drug concentrations, minimizing toxicity while ensuring therapeutic efficacy. Pharmacokinetic principles govern the dynamics of plasma concentrations and can be mathematically described using specific equations.The plasma drug concentration...
160
Determination of Renal Drug Clearance: Graphical and Midpoint Methods01:07

Determination of Renal Drug Clearance: Graphical and Midpoint Methods

Renal clearance, a crucial parameter in pharmacokinetics, can be determined using two different methods: the graphical method and the midpoint method. These methods provide insights into the rate of drug excretion by the kidneys and aid in assessing renal function.
The graphical method involves plotting the rate of drug excretion in urine against the plasma drug concentration. By analyzing the graph, the clearance can be calculated and obtained. Drugs rapidly excreted by the kidneys exhibit a...
321
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
801
Heart Failure Drugs: Inotropic Agents01:26

Heart Failure Drugs: Inotropic Agents

Positive inotropic agents are commonly used as the first line of treatment for heart failure. One such agent is digoxin, derived from the genus Digitalis, which has been known for centuries but effectively utilized since 1785. However, these cardiac glycosides can have potentially toxic effects due to their mechanism of action, which involves inhibiting Na+/K+-ATPase and increasing contractility. Digoxin is absorbed orally and distributed in various tissues, including the CNS. It has a long...
1.1K
Heart Failure Drugs: Diuretics01:22

Heart Failure Drugs: Diuretics

Heart failure and kidney perfusion are interconnected in a complex way. Reduced renal perfusion and venous congestion are two significant factors that contribute to renal dysfunction in heart failure. The kidneys, primarily responsible for fluid balance in the body, are adversely affected due to compromised cardiac output and increased venous pressure. In response to reduced renal perfusion, the kidneys activate neurohumoral mechanisms to restore balance. However, these mechanisms can be...
726
Heart Failure IV: Classification and Diagnostic Evaluation01:30

Heart Failure IV: Classification and Diagnostic Evaluation

Heart failure can be classified in various ways, with the most common classifications based on physical activity limitations, disease progression, severity, and treatment strategies.The Functional Classification of Heart Failure divides patients into four categories based on physical activity limitation due to symptom burden.Class I: Patients in this class have cardiac disease but no physical activity limitations. Ordinary activities like walking, climbing stairs, or routine tasks do not cause...
225