Dose linearity of clonidine after transdermal application.

A prerequisite for optimal antihypertensive treatment is the possibility of individualized dosing. Therefore, three different dosages of the clonidine containing transdermal systems have been developed. The aim of this analysis was to clarify whether a linear enlargement of system size and consequently, a linear increase of the dose coming into contact with the skin will result in a linear increase of bioavailable drug.

Finger pulse plethysmographic effects of two oral sustained-release formulations of isosorbide dinitrate in normal man.

Two sustained release formulations of 40 mg isosorbide dinitrate, encapsulated pellets and a tablet, were compared double blind following oral administration of single doses in terms of response on finger pulse plethysmography in nine healthy male volunteers. Following both formulations there was a distinct effect on the depth of b-wave in the first derivative of the finger pulse up to 9 h after administration. This change of the parameter of nitrate action was significantly different from placebo for both formulations.

Plasma levels of isosorbide dinitrate and its main metabolites following oral administration of two sustained release formulations in normal man.

The plasma levels of isosorbide dinitrate (ISDN) and the two pharmacologically active metabolites were measured following administration of two oral sustained release formulations containing 40 mg ISDN in nine healthy male volunteers. The new galenic formulation (pellets in a hard gelatin capsule) resulted in generally higher plasma levels for all three assayed substances over the time period of 24 h. The pharmacokinetic interpretation of the plasma levels following administration of the sustained release capsule assuming a one-compartment body model with zero-order invasion and first-order elimination showed a constant liberation over approximately 5 h.

Relationship between the pharmacodynamics and pharmacokinetics of two oral sustained-release formulations of isosorbide dinitrate in normal man.

The relationship between the pharmacodynamics and pharmacokinetics of isosorbide dinitrate (ISDN) following oral administration of 40 mg of two different models. A model assuming an additive contribution of all active drug-related substances in plasma to pharmacological effect, i.e.