Pharmacokinetics of Lopinavir in HIV Type-1-Infected Children Taking the New Tablet Formulation Once Daily

Autor: David M. Burger, Linda C. van der Knaap, Manon J. van der Lee, Gertjan J. Driessen, Gwenda Verweel, Nico G. Hartwig, Petronette van Jaarsveld, Michiel van der Flier
Rok vydání: 2008
Předmět:
Zdroj: Antiviral Therapy. 13:1087-1090
ISSN: 2040-2058
1359-6535
Popis: BackgroundRecently, a new tablet formulation of the widely used HIV protease inhibitor lopinavir/ritonavir was licensed. Here, we present a pilot study of the pharmaco-kinetics of the new adult tablet formulation taken once daily in children.MethodsLopinavir pharmacokinetics of the new adult tablet formulation were evaluated in 15 HIV type-1-infected children between 4 and 15 years of age. A target dose of 460/115 mg/m2was administered once daily. Plasma concentrations of lopinavir over the course of 24 h were determined with a validated HPLC method.ResultsThe median lopinavir dose was 498 mg/m2(range 424–548). The mean ±sd for lopinavir area under the 24 h curve was 217.9 ±44.9 mg/l•h, the maximum concentration was 14.8 ±2.4 mg/l and the concentration 24 h after intake was 3.1 ±2.6 mg/l. The half-life of lopinavir was 5.8 ±4.5 h and the median time to maximum concentration was 5.8 h (range 1.8-12.2). Overall, the tablet formulation resulted in greater exposure to lopinavir with less variability compared with the soft-gel capsule formulation. All children treated with the new adult tablet formulation had undetectable viral loads (ConclusionsThe tablet formulation could probably result in improved lopinavir dosing and increases the feasibility of once-daily lopinavir/ritonavir-based regimens in children.
Databáze: OpenAIRE