Abstract | OBJECTIVE: MATERIALS AND METHODS: This was an open-label, two-period (single-dose treatment followed by a multiple-dose (once-daily for 9 days), with a 7-day intertreatment washout period) study conducted in 18 subjects. Serial blood samples were collected at pre-defined time points, and the plasma concentrations of valsartan and amlodipine were measured using LC-MS/MS. Safety was evaluated after single- and multiple-dose drug administration. RESULTS: Following the single-dose oral administration of valsartan/ amlodipine 80/5 mg, valsartan and amlodipine plasma concentrations reached peak levels at median tmax of 3 and 6 h, respectively. These concentrations declined thereafter, with mean elimination half-lives of 7.7 h (single dose) and 8.6 h (multiple dose) for valsartan, and 47 h (single dose) and 45 h (multiple dose) for amlodipine. After a 9-day multiple-dose treatment (at steady state), accumulation of valsartan and amlodipine was consistent with their half-lives. The single- and multiple-dose administration of valsartan/ amlodipine 80/5 mg was associated with asymptomatic hypotension, consistent with the pharmacological activity of the combination of these two blood pressure-lowering drugs when co-administered in healthy subjects. CONCLUSION:
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Authors | Jingli Duan, Jin Chen, Qi Yin, Rajesh Karan, Karin Meiser, Harold Tom Smith, Gangadhar Sunkara |
Journal | International journal of clinical pharmacology and therapeutics
(Int J Clin Pharmacol Ther)
Vol. 50
Issue 1
Pg. 33-43
(Jan 2012)
ISSN: 0946-1965 [Print] Germany |
PMID | 22192643
(Publication Type: Controlled Clinical Trial, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Amlodipine, Valsartan Drug Combination
- Antihypertensive Agents
- Drug Combinations
- Tetrazoles
- Amlodipine
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Topics |
- Administration, Ophthalmic
- Administration, Oral
- Adolescent
- Adult
- Amlodipine
(administration & dosage, adverse effects, pharmacokinetics)
- Amlodipine, Valsartan Drug Combination
- Antihypertensive Agents
(administration & dosage, adverse effects, pharmacokinetics)
- China
- Chromatography, Liquid
- Drug Combinations
- Half-Life
- Humans
- Male
- Middle Aged
- Tandem Mass Spectrometry
- Tetrazoles
(administration & dosage, adverse effects, pharmacokinetics)
- Young Adult
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