INTERMEDIATE RELEASE NICOTINIC ACID COMPOSITIONS FOR TREATING HYPERLIPIDEMIA WHICH EXHIBIT AN IN VIVO STAIR-STEPPED ABSORPTION CURVE

摘要

Intermediate release nicotinic acid formulations exhibiting an in vivo stair-stepped or sigmoidally-shaped absorption curves when the plasma nicotinic acid or nicotinuric acid curves are deconvoluted using the Wagner-Nelson method, which are suitable for oral administration once-a-day preferably during the evening or at night for treating hyperlipidemia without causing drug-induced hepatotoxicity to such a level that requires the therapy to be discontinued, are disclosed. The stair-stepped or sigmoidal-shaped absorption profiles for nicotinic acid or nicotinuric acid absorbed from the nicotinic acid formulations of the instant invention are characterized by three phases and by the fact that significant quantities of nicotinic acid are absorbed during the first two phases. The first phase generally ends at about 2.3 hours following ingestion and the second phase generally ends at about 7.3 hours after consumption. Approximately 6% of the nicotinic acid dose is generally absorbed by the end of the first phase and approximately 91% of the nicotinic acid dose is absorbed by the end of the second phase.