Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Pharmacokinetics of a telmisartan, amlodipine and hydrochlorothiazide fixed-dose combination: A replicate crossover study in healthy Korean male subjects

Sang Young Lee^1,2, Kkot Nim Kang², Jae Hoon Kang², Kyu Ho Jeong² , Sang Won Lee¹, Hye Kyung Park¹, Eui-Kyung Lee¹

¹School of Pharmacy, Sungkyunkwan University; ²Research Laboratories, Ildong Pharmaceutical Co, Ltd, Gyeonggi-do, Republic of Korea.

For correspondence:- Kyu Jeong Email: whoai@ildong.com Tel:+82313712842

Accepted: 20 August 2017 Published: 30 September 2017

Citation: Lee SY, Kang KN, Kang JH, Jeong KH, Lee SW, Park HK, et al. Pharmacokinetics of a telmisartan, amlodipine and hydrochlorothiazide fixed-dose combination: A replicate crossover study in healthy Korean male subjects. Trop J Pharm Res 2017; 16(9):2245-2253 doi: 10.4314/tjpr.v16i9.28

© 2017 The authors.
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Abstract

Purpose: To compare the tolerability and pharmacokinetic profiles of telmisartan, amlodipine, and hydrochlorothiazide (HCTZ) in a fixed-dose combination (FDC, test product) with a co-administered telmisartan/amlodipine FDC and HCTZ in a single-entity tablet (reference product)

Methods: This was a single-dose, randomized, open-label, replicate crossover study conducted in healthy male Korean volunteers aged 19 – 50 years. Fasting randomized subjects received a newly developed test product (telmisartan/amlodipine/HCTZ, 80/10/25 mg) or two tablets of Twynsta® (40/5 mg) and one tablet of HCTZ (25 mg) as reference products. After a washout period, each group replicated the exposure of the other group.

Results: The AUC_last (h•ng/mL) geometric mean was 3,194.87 and 3,273.77 for the telmisartan test and reference products, respectively; 329.92 and 315.13 for the amlodipine test and reference products; 1,203.98 and 1,150.86 for the HCTZ test and reference products, respectively. The geometric mean of C_max (ng/mL) was 543.04 and 497.81 for the telmisartan test and reference products, respectively; 7.74 and 7.34 for the amlodipine test and reference products; 218.71 and 184.39 for the HCTZ test and reference products, respectively. For telmisartan, the 90 % CI of GMRs of AUC_last (h•ng/mL) and C_max (ng/mL) were 0.9414 – 1.0496 and 1.0246 – 1.2792, respectively; the coefficient of variation (CV) of telmisartan C_max was 41.96 %.

Conclusion: A formulated FDC tablet containing a telmisartan/amlodipine/HCTZ combination (80/10/25 mg) was bioequivalent to a co-administrated commercially available telmisartan/amlodipine combination and HCTZ tablets at equivalent concentrations.

Keywords: Fixed-dose combination, Hypertension, Telmisartan, Amlodipine besylate, Hydrochlorothiazide, Pharmacokinetics