Bioequivalence model for evaluation of Losartan in human plasma with special reference to drug–metabolite ratio

Abstract

Losartan and in-vivo active metabolite losartan carboxylic acid (LCA) formation into systemic circulation have been poorly characterized in different races. A bioequivalence study was therefore conducted on healthy male Indian volunteers with 50 mg losartan formulation and unique comparative analysis with other population is presented. Non-compartmental pharmacokinetic analysis elucidated metabolite formation ratio (MR) for losartan: LCA [C_max = 1.30 and AUC = 0.32] of 50 mg losartan was more varying compared to innovator [C_max = 0.82 and AUC = 0.22] though bioequivalence requirements were met successfully. This variation was less for losartan 100 mg losartan- hydrochlorothiazide formulation in our previous published bioequivalence study.

Keywords::

• Drug metabolism
• pharmacokinetics (DMPK)
• losartan:losartan carboxylic acid–metabolic ratio (MR) comparative analysis
• losartan bioequivalence

Acknowledgement

The authors would like to thank Ranbaxy Laboratories Ltd. India, for giving permission to write this paper and to use in-house data. A special thanks to our in-house formulation department for providing the formulation and Clinical Pharmacology Unit, Ranbaxy Research Laboratories, Majeedia Hospital, Delhi, India for conducting the clinic.

Declaration of interest: The authors report no conflicts of interest.