Results The blood plasma Cot curve of A771726 conformed to one compartment model of the first order absorption. The main pharmacokinetic parameters of A771726(3, 6, 12 mg/kg) were T1/2ka(h): 3.91±3.43, 5.63±2.07, 6.73±1.67;
PRE-CLINICAL AND CLINICAL PHARMACOKINETICS OF THE DIASTEREOMERS OF ARTEETHER, A POTENT ANTIMALARIAL
The pharmacokinetics of α- and β-diastereomers of Arteether, a well-known antimalarial drug and its active metabolite dihydroartemisinin (DHA) were studied in Sprague-Dawley rats, Rhesus monkeys and human volunteers.
Studies in rats revealed dose dependency/ non-linearity in arteether pharmacokinetics with in the dose levels used.
The biological activity on cancer cells and the pharmacokinetics have also been evaluated, showing a very high liver-to-skin ratio and short retention time in tissues.
The pharmacokinetics of Selank, an anxiolytic peptide, was also studied in brain tissues using the intranasal in vivo administration of this peptide.
Overall the pharmacokinetic properties of both isomers were similar in rats, monkeys and humans, with β-isomer exhibiting longer elimination half-life, MRT, volume of distribution and clearance, irrespective of the route of administration.
Because of their complimentary pharmacokinetic characteristics, the isomeric mixture of arteether can be therapeutically more beneficial than β- isomer used alone.
At present, however, side effects and/or insufficient pharmacokinetic profiles have made most of the drug candidates undesirable.
The genetic factors involved in Parkinson's and Alzheimer's diseases are conventionally divided into pharmacodynamic and pharmacokinetic.
The pharmacokinetic factors play a role in Parkinson's disease (PD) at the level of metabolism of DA, dioxyphenylalanine, and tyrosine and include polymorphisms of enzymes and proteins involved in the relevant metabolic reactions.
The different doses had no significant effect on the main pharmacokinetic data and the kinetics seemed to be linear in dosage range 2.5-15?mg?kg-1.
No statistically significant differences between the main pharmacokinetic parameters of NETO and NET as well as NETO-AC and NET-AC were found.
Estimations of the main pharmacokinetic parameters (elimination half life: 230±102 min, total body clearance: 520±283 ml·min-1, total volume of distribution: 2.23±1.15 l·kg-1) showed no marked differences with normal patients.
In the group of patients with severe renal dysfunction, the main pharmacokinetic finding was a longer half-life after multiple dosing.
The main pharmacokinetic parameters (half-lives, total volume of distribution, total plasma clearance) were estimated in the test group by maximum-likelihood estimation using all samples and by Bayesian estimation using three samples.