Arzneimittelforschung 2008; 58(7): 363-366
DOI: 10.1055/s-0031-1296521
Antibiotics · Antimycotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Pharmacokinetics and Comparative Bioavailability of Two Terbinafine Hydrochloride Formulations after Single-dose Administration in Chinese Healthy Subjects

Xin Jiang
1  Laboratory of Physical and Chemical Analysis, JiangSu Centers for Diseases Prevention and Control, Nanjing, P. R. China
,
Na Wang
2  Key Laboratory of Drug Quality Control and Pharmacovigilance (China Pharmaceutical University), Ministry of Education, Nanjing, P. R. China
3  Center for Instrumental Analysis, China Pharmaceutical University, Nanjing, P. R. China
,
Zun-Jian Zhang
2  Key Laboratory of Drug Quality Control and Pharmacovigilance (China Pharmaceutical University), Ministry of Education, Nanjing, P. R. China
3  Center for Instrumental Analysis, China Pharmaceutical University, Nanjing, P. R. China
,
Yuan Tian
2  Key Laboratory of Drug Quality Control and Pharmacovigilance (China Pharmaceutical University), Ministry of Education, Nanjing, P. R. China
3  Center for Instrumental Analysis, China Pharmaceutical University, Nanjing, P. R. China
,
Yun Chen
4  Institute of Dermatology, Chinese Academy of Medical Sciences & Peking Union Medical College, Nanjing, P. R. China
› Author Affiliations
Further Information

Publication History

Publication Date:
15 December 2011 (online)

Abstract

The bioavailability of a new terbinafine (CAS 91161-71-6) preparation was compared with a commercially available original preparation (reference) of the drug in 19 Chinese healthy male volunteers. The study was performed in an open, randomized, single blind two-sequence, two-period crossover design. Under fasting conditions, each subject received a single oral dose of 250 mg terbinafine as a test or reference formulation with a 7-day washout period between the two preparations. The plasma concentrations of terbinafine were analyzed by a sensitive liquid chromatography-ultraviolet spectrometry method. The pharmacokinetic parameters included AUC0-τ, AUC0-∞, Cmax, t1/2, and Tmax. The values of AUC0–t demonstrated nearly identical bioavailability of terbinafine from the examined formulations. The AUC0–48 of terbinafine was 5982.85 ± 2449.17 and 6761.63 ± 3140.33 ng · h/ml for the test and reference formulation, respectively. The maximum plasma concentration (Cmax) of terbinafine was 1656.25 ± 623.18 ng/ml for the test and 1552.07 ± 660.35 ng/ml for the reference product, respectively. No statistical differences were observed for Cmax and the area under the plasma concentrationtime curve for terbinafine. The 90% confidence limits calculated for Cmax and AUC from zero to infinity (AUC0–∞) of terbinafine were within the bioequivalence range (80%– 125% for AUC). This study shows that the test formulation is bioequivalent to the reference formulation of terbinafine.