Itraconazole IV nanosuspension enhances efficacy through altered pharmacokinetics in the rat.

The goal of this research was to evaluate an intravenous itraconazole nanosuspension dosage form, relative to a solution formulation, in the rat. Itraconazole was formulated as a nanosuspension by a tandem process of microcrystallization followed by homogenization. Acute toxicity, pharmacokinetics, and distribution were studied in the rat, and compared with a solution formulation of itraconazole.

Histologic lesions associated with intravenous infusions of large volumes of isotonic saline solution in rats for 30 days.

The objective of this study was to characterize the changes associated with intravenous infusions of large volumes of isotonic saline solution in rats so that effects of the infusion process could be more easily distinguished from effects of test articles. Male Sprague-Dawley rats weighing approximately 225-275 g at the beginning of the study were given intravenous infusions of isotonic saline solution once daily for 30 consecutive days at dosages of 40 or 80 ml/kg body weight. Saline solution was administered through catheters placed in the caudal veins of the tail according to one of the following regimens: 80 ml/kg at 0.

Toxicity evaluations of L-cysteine and Procysteine, a cysteine prodrug, given once intravenously to neonatal rats.

Decreased enzymatic production of cysteine in premature and newborn infants may limit the synthesis of glutathione. Unfortunately, cysteine supplementation is limited by associated toxicity and product instability. Procysteine (L-2-oxothiazolidine-4-carboxylate) is a prodrug of cysteine that is inert until metabolized to cysteine intracellularly, thus stimulating glutathione synthesis.