Pharmaceutical composition for administration in a single daily dose to change lipids in an individual without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis, coated tablet for oral administration and method for administering said composition

摘要

B "PHARMACEUTICAL COMPOSITION FOR ADMINISTRATION IN A DAILY DOSE FOR ALTERATION OF LIPIDS IN AN INDIVIDUAL WITHOUT CAUSING DRUG-INDUCED HEPATOTOXICITY, MYOPATHY OR RABDOMYLYSIS, COMPRESSED COMPRESSION FOR ADMINISTRATION OF THIS ADMINISTRATION FOR THE ADMINISTRATION OF ADMINISTRATION FOR ADMINISTRATION with solid pharmaceutical combinations for oral administration oral administration comprising nicotinic acid or nicotinic acid compounds or mixtures thereof in a sustained release form and an HMG-CoA reductase inhibitor, which serve to alter the levels of lipids in suffering individuals from, for example, hyperlipidemia and arteriosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis. The present invention is also related to methods of altering serum lipids in individuals to treat, for example, hyperlipidemia in hyperlipidemics, lipidemia in normolipidemics diagnosed or predisposed to cardiovascular diseases, and aretereosclerosis, administering said solid pharmaceutical composition orally once per day as a single dose during the night hours, without causing drug-induced hepatotoxicity, myopathies or rhabdomyolysis, or without causing, at least in an appreciable number of patients, drug-induced hepatotoxicity, myopathies or rhabdomyolysis of such severity that imposes the suspension of the aforementioned treatment. More particularly, the present invention relates to the solid oral pharmaceutical composition composed of, for example, (1) an HMG-CoA reductase inhibitor for immediate or prolonged release, (2) nicotinic acid, a compound of nicotinic acid or mixtures thereof , and (3) an expanding agent to form a sustained release composition for prolonged release of nicotinic acid or nicotinic acid compound or mixtures thereof for night or evening dosing to reduce the percentage of serum lipids and increase HDL cholesterol. In accordance with the present invention, and as an example, there is a composition for oral administration during the night time to alter serum lipids comprising nicotinic acid and hydroxypropyl methylcellulose in the form of a tablet or pill of prolonged or continuous release coated with a coating composed of an HMG-CoA reductase inhibitor in an immediate release form. Also in accordance with the present invention, pharmaceutical compositions can include a non-steroidal anti-inflammatory agent for reducing the ability of nicotinic acid or nicotinic acid compounds to cause flushing reactions in individuals.