The technique of accelerator mass spectrometry (AMS) was validated successfully and used to study the pharmacokinetics and disposition in dogs of a preclinical drug candidate (7-deaza-2'-C-methyl-adenosine; Compound A), after oral and intravenous administration. The primary objective of this study was to examine whether Compound A displayed linear kinetics across subpharmacological (microdose) ...

Fifteen broiler chickens (COBB 400) of 42 days of age weighing 1.8 to 2.0 kg were equally divided into 3 groups, each consisting of 5 birds. Hepatopathy was induced by oral administration of paracetamol while nephropathy was induced by intravenous administration of uranyl nitrate. Kinetic study was investigated in healthy, hepatopathic and nephropathic birds following single oral administration...

All-trans retinoic acid (atRA) is a front-line treatment of acute promyelocytic leukemia (APL). Due to its activity in regulating the cell cycle, it has also been evaluated for the treatment of other cancers. However, the efficacy of atRA has been limited by atRA inducing its own metabolism during therapy, resulting in a decrease of atRA exposure during continuous dosing. Frequent relapse occur...

In recent years a considerable amount of data have been produced on the activity of the microsomal drug metabolizing Systems in the human fetus [10, 16, 17,18, 19, 21, 26, 29, 32]. They all indicate that the various metabolic Systems responsible for drug degradation are already present in the intrauterine life, though their specific activity is in most cases considerably lower than that of adul...

Diclofenac sodium and diclofenac potassium in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of 18 rabbits in normal and Escherichia coli induced febrile condition with a washout period of 7 days. Biochemical and physiological parameters were measured in both normal and febrile state. Diclofenac levels in plasma were determined using a reversed-phas...

Intravitreally administered lampalizumab is an investigational complement inhibitor directed against complement factor D (CFD) for the treatment of geographic atrophy (GA) secondary to age-related macular degeneration. We sought to develop an integrated ocular and systemic pharmacokinetic/pharmacodynamic model for lampalizumab in patients with GA using the data from the clinical phase I and II ...

AIMS To investigate the kinetics of the (+)RS- and (-)SR-enantiomers and the carboxylic acid metabolite (MMQ) of the antimalarial drug mefloquine (MQ) in healthy volunteers. METHODS Ten subjects of which three were poor metabolizers of debrisoquine received racemic MQ 250 mg once weekly for 16 weeks. The kinetics were followed in plasma and urine and evaluated by individual kinetic modelling ...