Key result
Administration of a single 150 mg dose of dabigatran etexilate mesylate in healthy subjects allowed for complete pharmacokinetic characterization using newly validated bioanalytical methods.
Why the study?
Bioanalytical limitations previously prevented evaluation of dabigatran etexilate pharmacokinetics, prompting the development of validated methods to completely evaluate its pharmacokinetics.
What are the pharmacokinetics of dabigatran etexilate, total dabigatran, and unconjugated dabigatran following a single 150 mg oral dose in healthy subjects?
What are the pharmacokinetics of dabigatran etexilate, total dabigatran, and unconjugated dabigatran following a single 150 mg oral dose in healthy subjects?
Validated bioanalytical methods allow for complete characterization of dabigatran etexilate pharmacokinetics, which can impact drug development and generic formulation evaluation.
No immediate clinical implications; leaves open extension of dabigatran PK data to patients.
PURPOSE: Due to bioanalytical limitations it was previously not possible to evaluate the pharmacokinetics of dabigatran etexilate. We have developed validated methods to assay dabigatran etexilate, unconjugated dabigatran, and total dabigatran that will allow for a complete investigation into the pharmacokinetics of dabigatran etexilate mesylate. This study was designed to evaluate the pharmacokinetics of these analytes in healthy subjects. METHODS: This was an open-label, single-dose, one-period, one-treatment study. A single oral dose of dabigatran etexilate mesylate capsule containing the equivalent of 150 mg dabigatran etexilate was administered to each subject. A total of 23 blood samples for pharmacokinetic analysis were collected and analyzed from each subject. Safety and tolerability were monitored throughout the study. RESULTS: was 0.54±0.26 h. Only one subject experienced an adverse event. CONCLUSION: Using validated bioanalytical methods, a complete characterization of dabigatran etexilate, total dabigatran, and unconjugated dabigatran pharmacokinetics was achieved. Advancements in the development of new more accurate, specific, and sensitive validated bioanalytical methods such as these enable for a complete understanding of the drug's pharmacokinetics and this, in turn, can have an impact on both the drug development and the evaluation of generic formulations.
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Bouhajib et al. (2019) studied Healthy subjects. Dabigatran etexilate mesylate was evaluated on Pharmacokinetics of dabigatran etexilate, total dabigatran, and unconjugated dabigatran. Administration of a single 150 mg dose of dabigatran etexilate mesylate in healthy subjects allowed for complete pharmacokinetic characterization using newly validated bioanalytical methods.
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