An improved method and composition for the treatment of hyperlipidemia,
hypercholesterolemia, and hypertriglyceridemia as well as other disease
states, particularly cardiovascular problems, uses a multiple release
system that provides an immediate release of nicotinic acid followed by a
subsequent release of nicotinic acid from the hydrolysis of a compound
that generates nicotinic acid. In general, a composition according to the
present invention comprises: (1) a quantity of nicotinic acid intended to
saturate liver enzymes during a period from about 0.5 hours to about 2.5
hours after administration of the pharmaceutical composition but
insufficient to trigger significant generation of nicotinuric acid; (2) a
quantity of a derivative or analogue of nicotinic acid that is subject to
hydrolysis after ingestion such that preferrably no more than about 10%
of the derivative or analogue is hydrolyzed by about 8 hours after
ingestion and such that substantially all of the derivative or analogue
is hydrolyzed by about 12 hours after ingestion; and (3) at least one
pharmaceutically acceptable carrier.