[Pharmacokinetics and -dynamics of retard formation of isradipine. Summary of studies]

Abstract

The newly developed sustained-release form of isradipine (Vascal uno/Lomir SRO) releases the active substance continuously from a gel matrix over a period of 24 hours. In comparison with the standard formulation, the absolute bioavailability of the sustained-release preparation is somewhat increased at about 22.5%. Maximum plasma levels are reached five to seven hours after oral administration of a capsule, and then level off. Both maximum plasma levels and bioavailability increase linearly with dose. At therapeutic dosage isradipine does not accumulate. Twenty-four hours after ingestion of the capsule, plasma levels are still half the maximum. As a result of slow absorption and minimal fluctuations in the concentration of the active agent, side effects of the sustained-release version of isradipine are even rarer than with the standard preparation.