Effect of food on the pharmacokinetics of the active metabolite of the prodrug repirinast.

The effect of food on the pharmacokinetics of the active metabolite of the new antiasthmatic drug repirinast was investigated in two different studies after oral administration of 300 mg of repirinast. In each study, 12 healthy volunteers received the repirinast dose under fasting or fed conditions in a crossover manner. In one study, a high-fat meal (American breakfast) was used and in another study, a low-fat, high-carbohydrate meal (continental breakfast) was used.

Pharmacokinetics of the active metabolite of the prodrug repirinast in healthy Caucasian volunteers after a single oral dose.

The pharmacokinetics of BAY w 8199, the active metabolite of the prodrug repirinast (BAY u 2372), has been investigated after oral administration of 150, 300 and 450 mg repirinast to twelve healthy male Caucasians. Plasma BAY w 8199 concentrations were very variable between subjects. The mean peak level (geom.

Bioequivalence of two atenolol formulations in healthy volunteers. Evaluation and prediction of effect kinetics at beta-adrenoceptors in vivo by means of a radioreceptor assay.

Pharmacokinetic and pharmacodynamic effects of single oral doses of 200 mg of two atenolol formulations (Tenormin, atenolol (T) and Duraatenolol, atenolol (D)) were assessed in eight male healthy volunteers for 48 h (double-blind crossover design). Both formulations were bioequivalent in terms of pharmacokinetic parameters (AUC, tmax, Cmax, t1/2) as detected by gas liquid chromatography. By means of a radioreceptor assay (RRA) any significant contribution of beta 2-adrenoceptors and active metabolites to effects observed in vivo was ruled out.

Clinical pharmacology of the hypocholesterolemic agent K 12.148 (lifibrol) in healthy volunteers.

K 12.148 (INN:lifibrol), a new cholesterol synthesis inhibitor, was studied in healthy volunteers to evaluate tolerance/safety, the effects on lipids, and pharmacokinetics. In a sequential block design the doses of 150, 300, 600, or 900 mg, given once daily in the morning for 14 consecutive days, were examined in 40 healthy young males (8 active drug and 2 placebo per group, randomized) under well-controlled conditions.

Subjective symptoms and pharmacokinetics/dynamics of metoprolol CR in elderly subjects--a comparison with atenolol.

In a double-blind, randomised, cross-over study, the pharmacokinetic/dynamic effects and subjective symptoms of a new controlled-release (CR) formulation of metoprolol (50 and 100 mg) have been compared with atenolol (50 mg) and placebo in 20 elderly healthy subjects. The metoprolol CR formulation displayed an even plasma concentration-time profile over the dosage interval while atenolol produced a peak at 2-4 h. All three active treatments produced significant beta 1-blockade at 24 h compared to placebo.