PMID- 29270003
OWN - NLM
STAT- MEDLINE
DCOM- 20180810
LR  - 20220318
IS  - 1177-8881 (Electronic)
IS  - 1177-8881 (Linking)
VI  - 11
DP  - 2017
TI  - Comparative pharmacokinetics of a fixed-dose combination vs concomitant 
      administration of telmisartan and S-amlodipine in healthy adult volunteers.
PG  - 3543-3550
LID - 10.2147/DDDT.S148534 [doi]
AB  - 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 (C(max)) and area under the curve from time zero to the last 
      sampling time (AUC(t)) 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 C(max) and AUC(t) 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.
FAU - Oh, Minkyung
AU  - Oh M
AD  - Department of Pharmacology.
AD  - PharmacoGenomics Research Center, Inje University College of Medicine, Busan.
FAU - Park, Sung-Eun
AU  - Park SE
AD  - Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, 
      Republic of Korea.
FAU - Ghim, Jong-Lyul
AU  - Ghim JL
AD  - Department of Pharmacology.
AD  - PharmacoGenomics Research Center, Inje University College of Medicine, Busan.
AD  - Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, 
      Republic of Korea.
FAU - Choi, Young-Kyung
AU  - Choi YK
AD  - Department of Pharmacology.
FAU - Shim, Eon-Jeong
AU  - Shim EJ
AD  - Department of Pharmacology.
AD  - PharmacoGenomics Research Center, Inje University College of Medicine, Busan.
AD  - Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, 
      Republic of Korea.
FAU - Shin, Jae-Gook
AU  - Shin JG
AD  - Department of Pharmacology.
AD  - PharmacoGenomics Research Center, Inje University College of Medicine, Busan.
AD  - Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, 
      Republic of Korea.
FAU - Kim, Eun-Young
AU  - Kim EY
AD  - Department of Pharmacology.
AD  - PharmacoGenomics Research Center, Inje University College of Medicine, Busan.
AD  - Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, 
      Republic of Korea.
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Randomized Controlled Trial
DEP - 20171211
PL  - New Zealand
TA  - Drug Des Devel Ther
JT  - Drug design, development and therapy
JID - 101475745
RN  - 0 (Benzimidazoles)
RN  - 0 (Benzoates)
RN  - 0 (Tablets)
RN  - 1J444QC288 (Amlodipine)
RN  - U5SYW473RQ (Telmisartan)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Amlodipine/administration & dosage/*pharmacokinetics
MH  - Benzimidazoles/administration & dosage/*pharmacokinetics
MH  - Benzoates/administration & dosage/*pharmacokinetics
MH  - Cross-Over Studies
MH  - Dose-Response Relationship, Drug
MH  - Healthy Volunteers
MH  - Humans
MH  - Male
MH  - Maximum Tolerated Dose
MH  - Middle Aged
MH  - Tablets/administration & dosage/pharmacokinetics
MH  - Telmisartan
MH  - Young Adult
PMC - PMC5729885
OTO - NOTNLM
OT  - S-amlodipine
OT  - bioequivalence
OT  - fixed-dose combination
OT  - pharmacokinetics
OT  - telmisartan
COIS- Disclosure The authors report no conflicts of interest in this work.
EDAT- 2017/12/23 06:00
MHDA- 2018/08/11 06:00
PMCR- 2017/12/11
CRDT- 2017/12/23 06:00
PHST- 2017/12/23 06:00 [entrez]
PHST- 2017/12/23 06:00 [pubmed]
PHST- 2018/08/11 06:00 [medline]
PHST- 2017/12/11 00:00 [pmc-release]
AID - dddt-11-3543 [pii]
AID - 10.2147/DDDT.S148534 [doi]
PST - epublish
SO  - Drug Des Devel Ther. 2017 Dec 11;11:3543-3550. doi: 10.2147/DDDT.S148534. 
      eCollection 2017.