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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...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Dove Medical Press
2018
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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. |
format | Online Article Text |
id | pubmed-6208487 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
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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