Simple, Rapid and Validated LC Determination of Lopinavir in Rat Plasma and its Application in Pharmacokinetic Studies

Sci Pharm. 2011 Oct-Dec;79(4):849-63. doi: 10.3797/scipharm.1107-24. Epub 2011 Sep 17.

Abstract

Lopinavir is a new specific and potent HIV-1 protease inhibitor. A simple and rapid Reverse Phase High-Performance Liquid Chromatographic method using UV detection was developed and validated for the analysis of lopinavir in rat plasma under isocratic conditions. The method involves a single step protein precipitation technique. The detector response was linear over the concentration range of 250 to 4000 ng mL (-1). High recovery ranging from 97.5 to 101.2 percent was obtained which precludes the use of internal standard. The developed method was validated as per standard guidelines. Validation of the developed method demonstrated accuracy, precision and selectivity of the proposed method. The drug was found to be stable under various processing and storage conditions. This rapid and cost-effective method was successfully applied in the estimation of lopinavir and determination of various pharmacokinetic parameters during post intravenous bolus administration of the drug in rats. The developed method can be suitably employed in preclinical pharmacokinetic evaluation of new formulations designed to improve the bioavailability of lopinavir.

Keywords: HIV-1 protease inhibitor; HPLC; Liquid chromatography; Lopinavir; Pharmacokinetic studies; Rat plasma.