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Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers.
Drug Des Devel Ther. 2017; 11:3543-3550.DD

Abstract

Objective

This study compared the pharmacokinetic (PK) and safety profiles of a fixed-dose combination (FDC) formulation of telmisartan and S-amlodipine with those of concomitant administration of the two drugs.

Materials and methods

This was an open-label, randomized, crossover study in healthy male Koreans. All subjects were administered an FDC tablet containing 40 mg telmisartan and 5 mg S-amlodipine and were also coadministered the same dose of both drugs given separately. The crossover study design included a 14-day washout period between the two treatments. Blood samples were collected up to 168 h following drug administration. The plasma concentrations of telmisartan and S-amlodipine were determined by liquid chromatography tandem mass spectrometry. PK parameters and plasma concentration-time curves were compared. Safety was assessed by measuring vital signs, clinical laboratory tests, physical examinations, and patient interviews.

Results

The geometric mean ratios and 90% CIs for the maximum plasma concentration (Cmax) and area under the curve from time zero to the last sampling time (AUCt) were 0.8782 (0.8167-0.9444) and 0.9662 (0.9210-1.0136) for telmisartan and 1.0069 (0.9723-1.0427) and 1.0324 (0.9969-1.0690) for S-amlodipine, respectively. A total of 36 adverse events (AEs) were reported by 23 subjects, but no statistical differences were observed between the two treatments. The most frequently reported AE was a mild-to-moderate headache that was generally self-limiting.

Conclusion

For both telmisartan and S-amlodipine, the Cmax and AUCt 90% CIs were between ln (0.8) and ln (1.25). These results suggest that the FDC formulation is pharmacokinetically bioequivalent and has a similar safety profile to the coadministration of these drugs.

Authors+Show Affiliations

Department of Pharmacology. PharmacoGenomics Research Center, Inje University College of Medicine, Busan.Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, Republic of Korea.Department of Pharmacology. PharmacoGenomics Research Center, Inje University College of Medicine, Busan. Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, Republic of Korea.Department of Pharmacology.Department of Pharmacology. PharmacoGenomics Research Center, Inje University College of Medicine, Busan. Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, Republic of Korea.Department of Pharmacology. PharmacoGenomics Research Center, Inje University College of Medicine, Busan. Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, Republic of Korea.Department of Pharmacology. PharmacoGenomics Research Center, Inje University College of Medicine, Busan. Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, Republic of Korea.

Pub Type(s)

Comparative Study
Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

29270003

Citation

Oh, Minkyung, et al. "Comparative Pharmacokinetics of a Fixed-dose Combination Vs Concomitant Administration of Telmisartan and S-amlodipine in Healthy Adult Volunteers." Drug Design, Development and Therapy, vol. 11, 2017, pp. 3543-3550.
Oh M, Park SE, Ghim JL, et al. Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers. Drug Des Devel Ther. 2017;11:3543-3550.
Oh, M., Park, S. E., Ghim, J. L., Choi, Y. K., Shim, E. J., Shin, J. G., & Kim, E. Y. (2017). Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers. Drug Design, Development and Therapy, 11, 3543-3550. https://doi.org/10.2147/DDDT.S148534
Oh M, et al. Comparative Pharmacokinetics of a Fixed-dose Combination Vs Concomitant Administration of Telmisartan and S-amlodipine in Healthy Adult Volunteers. Drug Des Devel Ther. 2017;11:3543-3550. PubMed PMID: 29270003.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers. AU - Oh,Minkyung, AU - Park,Sung-Eun, AU - Ghim,Jong-Lyul, AU - Choi,Young-Kyung, AU - Shim,Eon-Jeong, AU - Shin,Jae-Gook, AU - Kim,Eun-Young, Y1 - 2017/12/11/ PY - 2017/12/23/entrez PY - 2017/12/23/pubmed PY - 2018/8/11/medline KW - S-amlodipine KW - bioequivalence KW - fixed-dose combination KW - pharmacokinetics KW - telmisartan SP - 3543 EP - 3550 JF - Drug design, development and therapy JO - Drug Des Devel Ther VL - 11 N2 - Objective: This study compared the pharmacokinetic (PK) and safety profiles of a fixed-dose combination (FDC) formulation of telmisartan and S-amlodipine with those of concomitant administration of the two drugs. Materials and methods: This was an open-label, randomized, crossover study in healthy male Koreans. All subjects were administered an FDC tablet containing 40 mg telmisartan and 5 mg S-amlodipine and were also coadministered the same dose of both drugs given separately. The crossover study design included a 14-day washout period between the two treatments. Blood samples were collected up to 168 h following drug administration. The plasma concentrations of telmisartan and S-amlodipine were determined by liquid chromatography tandem mass spectrometry. PK parameters and plasma concentration-time curves were compared. Safety was assessed by measuring vital signs, clinical laboratory tests, physical examinations, and patient interviews. Results: The geometric mean ratios and 90% CIs for the maximum plasma concentration (Cmax) and area under the curve from time zero to the last sampling time (AUCt) were 0.8782 (0.8167-0.9444) and 0.9662 (0.9210-1.0136) for telmisartan and 1.0069 (0.9723-1.0427) and 1.0324 (0.9969-1.0690) for S-amlodipine, respectively. A total of 36 adverse events (AEs) were reported by 23 subjects, but no statistical differences were observed between the two treatments. The most frequently reported AE was a mild-to-moderate headache that was generally self-limiting. Conclusion: For both telmisartan and S-amlodipine, the Cmax and AUCt 90% CIs were between ln (0.8) and ln (1.25). These results suggest that the FDC formulation is pharmacokinetically bioequivalent and has a similar safety profile to the coadministration of these drugs. SN - 1177-8881 UR - https://www.unboundmedicine.com/medline/citation/29270003/Comparative_pharmacokinetics_of_a_fixed_dose_combination_vs_concomitant_administration_of_telmisartan_and_S_amlodipine_in_healthy_adult_volunteers_ L2 - https://dx.doi.org/10.2147/DDDT.S148534 DB - PRIME DP - Unbound Medicine ER -