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Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects

Authors Kang WY, Seong SJ, Ohk B, Gwon MR, Kim BK, Cho S, Shim WS, Lee KT, Kim EH, Yang DH, Lee HW, Yoon YR

Received 25 July 2018

Accepted for publication 2 October 2018

Published 26 October 2018 Volume 2018:12 Pages 3607—3615

DOI https://doi.org/10.2147/DDDT.S161917

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Qiongyu Guo


Woo Youl Kang,1,2,* Sook Jin Seong,1,2,* Boram Ohk,1,2 Mi-Ri Gwon,1,2 Bo Kyung Kim,1,2 Seungil Cho,1,2 Wang-Seob Shim,3 Kyung-Tae Lee,4 Eun Hee Kim,5 Dong Heon Yang,6 Hae Won Lee,1,2 Young-Ran Yoon1,2

1Department of Molecular Medicine, School of Medicine, Kyungpook National University, Daegu, Republic of Korea; 2Department of Clinical Pharmacology, Kyungpook National University Hospital, Daegu, Republic of Korea; 3Kyung Hee Drug Analysis Center, Kyung Hee University, Seoul, Republic of Korea; 4College of Pharmacy, Kyung Hee University, Seoul, Republic of Korea; 5College of Nursing, Catholic University of Daegu, Gyeongsan-si, Gyeongbuk, Republic of Korea; 6Division of Cardiology, Department of Internal Medicine, Kyungpook National University Hospital, Daegu, Republic of Korea

*These authors contributed equally to this work

Purpose: A new fixed-dose combination (FDC) formulation of 120 mg fimasartan and 20 mg rosuvastatin was developed to increase therapeutic convenience and improve treatment compliance.
Methods: A randomized, open-label, single-dose, two-treatment, two-way crossover study with a 7-day washout period was conducted to compare the pharmacokinetic (PK) characteristics and bioequivalence between an FDC of fimasartan/rosuvastatin and the separate co-administration of fimasartan and rosuvastatin in healthy Korean volunteers. The plasma concentrations of fimasartan and rosuvastatin were analyzed by a validated liquid chromatography-tandem mass spectrometry method, for which serial blood samples were collected for up to 48 hours post-administration of fimasartan and 72 hours post-administration of rosuvastatin, in each period. The PK parameters were calculated using a non-compartmental method.
Results: A total of 78 subjects completed the study. All the 90% CIs of the geometric mean ratios (GMRs) fell within the predetermined acceptance range. The GMR and 90% CI for the area under the plasma concentration-time curve from time 0 to the last measurement (AUC0–t) and the maximum plasma concentration (Cmax) for fimasartan were 0.9999 (0.9391–1.0646) and 1.0399 (0.8665–1.2479), respectively. The GMR and 90% CI for the AUC0–t and Cmax for rosuvastatin were 1.0075 (0.9468–1.0722) and 1.0856 (0.9944–1.1852), respectively. Treatment with fimasartan and rosuvastatin was generally well tolerated without serious adverse events.
Conclusion: The new FDC formulation of 120 mg fimasartan and 20 mg rosuvastatin can be substituted for the separate co-administration of fimasartan and rosuvastatin, for the advantage of better compliance with convenient therapeutic administration.

Keywords: fixed-dose combination, pharmacokinetics, bioequivalence, fimasartan, rosuvastatin

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