Absolute bioavailability and bioequivalence of glibenclamide (Semi-Euglucon N).

The absolute bioavailability of HB 420 (a new pharmaceutical form of glibenclamide) was investigated in comparison with an i.v. infusion of glibenclamide and also in comparison with HB 419 (Semi-Euglucon) on a group of 10 healthy volunteers with the aid of a highly specific bioanalytical detection method.

Evaluation of bioavailability by different methods.

Demonstration of bioavailability (or bioequivalence) is a condition for marketing of a drug product, unless a waiver is granted. Biovailability is usually based on some statistical evaluation of three parameters, the area under the concentration-time curve, AUC, the peak concentration, Cmax, and the peak time, tmax, obtained for both the test drug product and the standard, using a crossover design with 12 to 24 subjects. The three biovailability parameters can be obtained by various mathematical procedures, and may vary according to the procedure selected and the operator's decision.

Pharmacokinetics and metabolism of isosorbide-dinitrate after intravenous and oral administration.

The bioavailabilities of a conventional and two slow release 20 mg isosorbide dinitrate (ISDN) formulations were compared after oral administration in a three way cross-over study in 8 male volunteers. In a further group of 6 male volunteers the pharmacokinetics and metabolism of ISDN were investigated after intravenous infusion of a median dose of 14.1 mg for 2.

Simulation studies of errors of parameter estimates in pharmacokinetics.

Pharmacokinetic parameters are indispensable for the development and evaluation of drugs. Therefore, they are required by international drug agencies and may influence relevant decisions. Their determination from experimental results is only possible with statistical errors.

KINPAK--a new program package for standardized evaluation of kinetic parameters.

Concept and basic routines of a new program package (KINPAK) for standardized evaluation of kinetic parameters are described. This new program is not based on compartmental analysis. Instead the experimental data sequence is fitted by flexible regression functions adequate for concentration-time curves.