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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

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 w...

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Autores principales: Kang, Woo Youl, Seong, Sook Jin, Ohk, Boram, Gwon, Mi-Ri, Kim, Bo Kyung, Cho, Seungil, Shim, Wang-Seob, Lee, Kyung-Tae, Kim, Eun Hee, Yang, Dong Heon, Lee, Hae Won, Yoon, Young-Ran
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6208487/
https://www.ncbi.nlm.nih.gov/pubmed/30464392
http://dx.doi.org/10.2147/DDDT.S161917
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author Kang, Woo Youl
Seong, Sook Jin
Ohk, Boram
Gwon, Mi-Ri
Kim, Bo Kyung
Cho, Seungil
Shim, Wang-Seob
Lee, Kyung-Tae
Kim, Eun Hee
Yang, Dong Heon
Lee, Hae Won
Yoon, Young-Ran
author_facet Kang, Woo Youl
Seong, Sook Jin
Ohk, Boram
Gwon, Mi-Ri
Kim, Bo Kyung
Cho, Seungil
Shim, Wang-Seob
Lee, Kyung-Tae
Kim, Eun Hee
Yang, Dong Heon
Lee, Hae Won
Yoon, Young-Ran
author_sort Kang, Woo Youl
collection PubMed
description 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 (AUC(0–t)) and the maximum plasma concentration (C(max)) for fimasartan were 0.9999 (0.9391–1.0646) and 1.0399 (0.8665–1.2479), respectively. The GMR and 90% CI for the AUC(0–t) and C(max) 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.
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spelling pubmed-62084872018-11-21 Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects Kang, Woo Youl Seong, Sook Jin Ohk, Boram Gwon, Mi-Ri Kim, Bo Kyung Cho, Seungil Shim, Wang-Seob Lee, Kyung-Tae Kim, Eun Hee Yang, Dong Heon Lee, Hae Won Yoon, Young-Ran Drug Des Devel Ther Original Research 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 (AUC(0–t)) and the maximum plasma concentration (C(max)) for fimasartan were 0.9999 (0.9391–1.0646) and 1.0399 (0.8665–1.2479), respectively. The GMR and 90% CI for the AUC(0–t) and C(max) 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. Dove Medical Press 2018-10-26 /pmc/articles/PMC6208487/ /pubmed/30464392 http://dx.doi.org/10.2147/DDDT.S161917 Text en © 2018 Kang et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Kang, Woo Youl
Seong, Sook Jin
Ohk, Boram
Gwon, Mi-Ri
Kim, Bo Kyung
Cho, Seungil
Shim, Wang-Seob
Lee, Kyung-Tae
Kim, Eun Hee
Yang, Dong Heon
Lee, Hae Won
Yoon, Young-Ran
Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
title Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
title_full Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
title_fullStr Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
title_full_unstemmed Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
title_short Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
title_sort pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6208487/
https://www.ncbi.nlm.nih.gov/pubmed/30464392
http://dx.doi.org/10.2147/DDDT.S161917
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