Clinical pharmacology of nisoldipine coat core

Nisoldipine is a second-generation dihydropyridine calcium antagonist structurally related to nifedipine and used in the treatment of stable angina and arterial hypertension. It is also under investigation for the treatment of left ventricular dysfunction. It was first developed as an immediate release tablet, but this formulation was not considered optimal for once-daily administration because of the variable results obtained at peak and trough in clinical studies. Consequently, nisoldipine coat core (CC) was developed with the aim of optimizing the drug's time--effect profile over the 24-hour dosing interval. The in vitro release pattern classifies this tablet as an "extended release" formulation according to European Community guidelines. The present article outlines the pharmacokinetic and pharmacodynamic profiles of nisoldipine CC, as obtained from recent clinical studies.