Bioequivalence of Traline Tablet to Zoloft®Tablet (Sertraline HCI 50 mg)

Abstract

Sertraline HCl, (1S-cis)-4-(3, 4-dichloro-phenyl)-1, 2, 3, 4-tetrahydro-N-methyl-l-naphthalenamine hydro- chloride, is a potent and selective serotonin reuptake inhibitor which is used in the treatment of depression and obsessive- compulsive disorders. The purpose of the present study was to evaluate the bioequivalence of two sertraline HCl tablets, Traline tablet (Myungin Pharm. Co. Ltd.) and Zoloft ® tablet (Pfizer Inc.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The in vitro release of sertraline from the two sertraline HCl formulations was tested using KP VIII Apparatus II method with various dissolution media. Twenty four healthy Korean male volunteers, 23.50± 1.74 years in age and 64.09±7.10 kg in body weight, were divided into two groups and a randomized 2 × 2 crossover study was employed. After a single tablet containing 50 mg as sertraline HCl was orally administered, blood samples were taken at predetermined time intervals and the concentrations of sertraline in serum were determined using an online column- switching HPLC method with UV/Vis detection. The dissolution profiles of two formulations were similar in all tested dis- solution media. The pharmacokinetic parameters such as AUCt, Cmax and Tmax were calculated, and computer programs (Equiv Test and K-BE Test) were utilized for the statistical analysis of the parameters using logarithmically transformed AUCt, Cmax and un-transformed Tmax. The results showed that the differences between two formulations based on the ref- erence drug, Zoloft ® tablet, were 0.04, 3.26 and -1.29% for AUCt, Cmax, and Tmax, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log0.8 to log1.25. Thus, the criteria of the KFDA bioequivalence guideline were sat- isfied, indicating Traline tablet was bioequivalent to Zoloft ® tablet.