The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry (LC-MS) method. The pharmacokinetic software Data Analysis System (Version 3.0) was ...

The large surface area and the short diffusion distance from capillaries of the blood brain barrier (BBB) to the neurons facilitate the drugs and nutrients access to the brain. Penetration of chemicals to the BBB occurs using a combination of intra and intercellular passages. Tight junctions regulate the intracellular passage of molecules according to their physicochemical properties (e.g. lipo...

Pharmacokinetic properties of dihydroartemisinin (DHA) were determined in mice given 100 mg/kg intraperitoneal DHA. Half-life, CL/F, and V/F were 25 min, 61.3 L/hr/kg, and 36.3 L/kg in malaria-infected mice and 19 min, 50.9 L/hr/kg, and 23.0 L/kg in controls. These data are valuable for pharmacokinetic-pharmacodynamic evaluations of DHA in murine models.

Attachment of poly(ethylene glycol) (PEG) to proteins, peptides, liposomes, drugs, and nanoparticles can improve pharmaceutical pharmacokinetic properties and enhance in vivo biological efficacy. Since the first PEGylated product was approved by the Food and Drug Administration in 1990, increasing numbers of PEGylated compounds have entered clinical use. Successful clinical development of PEGyl...

Mathematical models are routinely used in clinical pharmacology to study the pharmacokinetic and pharmacodynamic properties of a drug in the body. Identifiability of these models is an important requirement for the success of these clinical studies. Identifiability is classified into two types, structural identifiability related to the structure of the mathematical model and deterministic ident...

A new xanthine derivative bronchodilator, 1-methyl-3-propylxanthine (MPX), and 1-methyl-3-butylxanthine (MBX) were synthesized. We evaluated their relaxant effects on tracheal smooth muscle isolated from guinea pigs and pharmacokinetic characteristics in rats using 1,3-dimethylxanthine (theophylline, TPH) as the reference drug. Dose-dependent relaxant effects were observed in the concentration ...

Cephalosporins are of key clinical importance for treatment of bacterial infections. In the past decade, many cephalosporins have been synthesized and evaluated for antibacterial activity. These cephalosporins, with broad spectra of activity and high stability against various β-lactamases such as cefixime, cefteram pivoxil, and cefpodoxime proxetil, have been developed and introduced in clinica...

      The pharmacokinetic properties of amoxicillin and clavulanic acid when used alone or in combination may be different and show interaction between these two agents that might decrease the absolute bioavailability of clavulanic acid. In an open, randomized, replicated Latin square under fasting condition, pharmacokinetics of new formulations of amoxicillin/clavulanic acid were compared with...