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Pharmacokinetics and bioequivalence of a rosuvastatin/ezetimibe fixed-dose combination tablet versus single agents in healthy male subjects .
Int J Clin Pharmacol Ther. 2018 Jan; 56(1):43-52.IJ

Abstract

OBJECTIVE

The pharmacokinetic profiles and bioequivalence of a new rosuvastatin/ezetimibe fixed-dose combination (FDC; NVP-1205) vs. rosuvastatin and ezetimibe concomitantly administered as single agents were evaluated.

MATERIALS AND METHODS

In this open-label, single-dose, crossover study (NCT02029625), eligible subjects were randomly assigned in a 1 : 1 ratio to receive a single dose of rosuvastatin (10 mg) with ezetimibe (10 mg) as either a FDC or as single agents concomitantly administered under fasted conditions, followed by a 2-week washout period and administration of the alternate formulation. Serial blood samples were collected predose and up to 96 hours postdose in each period for determination of plasma rosuvastatin and ezetimibe concentrations by liquid-chromatography tandem mass spectroscopy and calculation of pharmacokinetic parameters.

RESULTS

The mean Cmax and AUC0-t values of rosuvastatin were 12.5 ng/mL and 115.6 ng×h/mL for the FDC, and 12.2 ng/mL and 115.1 ng×h/mL for the single agents concomitantly administered, respectively. The mean Cmax and AUC0-t values of ezetimibe were 4.7 ng/mL and 67.3 ng×h/mL for the FDC, and 4.5 ng/mL and 68.2 ng×h/mL for the single agents concomitantly administered, respectively. The geometric mean ratio (GMR) and 90% confidence interval (CI) for the rosuvastatin Cmax and AUC0-t were 106.20 (96.62 - 116.74) and 102.88 (96.32 - 109.90), respectively. The GMR and 90% CI for the ezetimibe Cmax and AUC0-t were 108.96 (98.56 - 120.51) and 98.13 (92.01 - 104.66), respectively. All treatments were well tolerated during this study, with no serious adverse events reported.

CONCLUSION

The rosuvastatin/ezetimibe (10/10 mg) FDC was bioequivalent to single agents concomitantly administered. A single dose of rosuvastatin/ezetimibe as the FDC or as single agents was well tolerated. .

Authors

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Pub Type(s)

Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

29162214

Citation

Kang, Woo Youl, et al. "Pharmacokinetics and Bioequivalence of a Rosuvastatin/ezetimibe Fixed-dose Combination Tablet Versus Single Agents in Healthy Male Subjects ." International Journal of Clinical Pharmacology and Therapeutics, vol. 56, no. 1, 2018, pp. 43-52.
Kang WY, Seong SJ, Ohk B, et al. Pharmacokinetics and bioequivalence of a rosuvastatin/ezetimibe fixed-dose combination tablet versus single agents in healthy male subjects . Int J Clin Pharmacol Ther. 2018;56(1):43-52.
Kang, W. Y., Seong, S. J., Ohk, B., Gwon, M. R., Kim, B. K., Na, S., Kim, H. J., Yoon, Y. R., & Lee, H. W. (2018). Pharmacokinetics and bioequivalence of a rosuvastatin/ezetimibe fixed-dose combination tablet versus single agents in healthy male subjects . International Journal of Clinical Pharmacology and Therapeutics, 56(1), 43-52. https://doi.org/10.5414/CP203026
Kang WY, et al. Pharmacokinetics and Bioequivalence of a Rosuvastatin/ezetimibe Fixed-dose Combination Tablet Versus Single Agents in Healthy Male Subjects. Int J Clin Pharmacol Ther. 2018;56(1):43-52. PubMed PMID: 29162214.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetics and bioequivalence of a rosuvastatin/ezetimibe fixed-dose combination tablet versus single agents in healthy male subjects . AU - Kang,Woo Youl, AU - Seong,Sook Jin, AU - Ohk,Boram, AU - Gwon,Mi-Ri, AU - Kim,Bo Kyung, AU - Na,Sookie, AU - Kim,Hyun-Ju, AU - Yoon,Young-Ran, AU - Lee,Hae Won, PY - 2017/12/20/accepted PY - 2017/11/23/pubmed PY - 2018/3/2/medline PY - 2017/11/23/entrez SP - 43 EP - 52 JF - International journal of clinical pharmacology and therapeutics JO - Int J Clin Pharmacol Ther VL - 56 IS - 1 N2 - OBJECTIVE: The pharmacokinetic profiles and bioequivalence of a new rosuvastatin/ezetimibe fixed-dose combination (FDC; NVP-1205) vs. rosuvastatin and ezetimibe concomitantly administered as single agents were evaluated. MATERIALS AND METHODS: In this open-label, single-dose, crossover study (NCT02029625), eligible subjects were randomly assigned in a 1 : 1 ratio to receive a single dose of rosuvastatin (10 mg) with ezetimibe (10 mg) as either a FDC or as single agents concomitantly administered under fasted conditions, followed by a 2-week washout period and administration of the alternate formulation. Serial blood samples were collected predose and up to 96 hours postdose in each period for determination of plasma rosuvastatin and ezetimibe concentrations by liquid-chromatography tandem mass spectroscopy and calculation of pharmacokinetic parameters. RESULTS: The mean Cmax and AUC0-t values of rosuvastatin were 12.5 ng/mL and 115.6 ng×h/mL for the FDC, and 12.2 ng/mL and 115.1 ng×h/mL for the single agents concomitantly administered, respectively. The mean Cmax and AUC0-t values of ezetimibe were 4.7 ng/mL and 67.3 ng×h/mL for the FDC, and 4.5 ng/mL and 68.2 ng×h/mL for the single agents concomitantly administered, respectively. The geometric mean ratio (GMR) and 90% confidence interval (CI) for the rosuvastatin Cmax and AUC0-t were 106.20 (96.62 - 116.74) and 102.88 (96.32 - 109.90), respectively. The GMR and 90% CI for the ezetimibe Cmax and AUC0-t were 108.96 (98.56 - 120.51) and 98.13 (92.01 - 104.66), respectively. All treatments were well tolerated during this study, with no serious adverse events reported. CONCLUSION: The rosuvastatin/ezetimibe (10/10 mg) FDC was bioequivalent to single agents concomitantly administered. A single dose of rosuvastatin/ezetimibe as the FDC or as single agents was well tolerated. . SN - 0946-1965 UR - https://www.unboundmedicine.com/medline/citation/29162214/Pharmacokinetics_and_bioequivalence_of_a_rosuvastatin/ezetimibe_fixed_dose_combination_tablet_versus_single_agents_in_healthy_male_subjects__ L2 - https://www.dustri.com/nc/journals-in-english?artId=16403 DB - PRIME DP - Unbound Medicine ER -