Pharmaceutical composition for single daily dose administration for lipid alteration in a subject without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis, coated tablet and method for administering said composition

摘要

"PHARMACEUTICAL COMPOSITION FOR DAILY SINGLE ADMINISTRATION FOR LIPID CHANGE IN AN INDIVIDUAL WITHOUT CAUSING DRUG-INDUCED HEPATOTOXICITY, TABLET AND ADDICTED DRUG-ADDED TABLET. The present invention relates to solid pharmaceutical composition for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures derived in a sustained release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in individuals suffering for example hyperlipidemia and arteriosclerosis without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis. The present invention is also related to a method for altering serum lipids of individuals for treating, for example, hyperlipidemia in hyperlipidemics, lipidemia in normolipidemics diagnosed or predisposed to cardiovascular disease, and atherosclerosis by administering said solid pharmaceutical composition orally. once a day as a single dose during the night, without causing drug-induced hepatotoxicity, myopathies or rhabdomyolysis, or without causing at least an appreciable number of patients drug-induced hepatotoxicity, myopathies or rhabdomyolysis to such an extent as to require discontinuation of the drug. said treatment. More particularly, the present invention relates to oral solid pharmaceutical composition comprising, for example, (1) an HMG-CoA reductase inhibitor for immediate or prolonged release, (2) nicotinic acid, a nicotinic acid compound or mixtures thereof, and (3) a potentiating agent to form a sustained release composition for the sustained release of nicotinic acid or nicotinic acid compound or mixtures for nocturnal or afternoon dosing to reduce serum lipid percentage and increase HDL cholesterol. In accordance with the present invention, and by way of example, there is provided a composition for oral administration at night time for altering serum lipids comprising nicotinic acid and hydroxypropyl methylcellulose in the form of a prolonged or sustained release tablet or tablet coated with a coating composed of an HMG-CoA reductase inhibitor in an immediate release form. Also in accordance with the present invention, the pharmaceutical composition may include a non-steroidal anti-inflammatory agent for reducing the ability of nicotinic acid or nicotinic acid compounds to cause flushing reactions in individuals.