COMBINATIONS OF HMG-COA INHIBITORS AND NICOTINIC ACID COMPOUNDS AND METHODS FOR TREATING HYPERLIPIDEMIA ONCE A DAY AT NIGHT
    15.
    发明公开
    COMBINATIONS OF HMG-COA INHIBITORS AND NICOTINIC ACID COMPOUNDS AND METHODS FOR TREATING HYPERLIPIDEMIA ONCE A DAY AT NIGHT 失效
    COAT片含烟酸的或者要烟酸代谢,延误UNLOCKED形式的物质,以及HMG-CoA还原酶COAT即时发布

    公开(公告)号:EP1017390A2

    公开(公告)日:2000-07-12

    申请号:EP98938228.8

    申请日:1998-07-31

    摘要: The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis. The present invention also relates to methods of altering serum lipids in subjects to treat, for example, hyperlipidemia in hyperlipidemics, lipidemia in normolipidemics diagnosed with or predisposed to cardiovascular disease, and atherosclerosis, by administering such oral solid pharmaceutical combinations once per day as a single dose during the evening hours, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis, or without causing in at least an appreciable number of individuals drug-induced hepatotoxicity, myopathy or rhabdomyolysis to such a level that discontinuation of such therapy would be required. More particularly, the present invention concerns oral solid pharmaceutical combinations comprised of, for example, (1) an HMG-CoA reductase inhibitor for immediate or extended release, (2) nicotinic acid, a nicotinic acid compound or mixtures thereof, and (3) a swelling agent to form a sustained release composition for extended release of the nicotinic acid or nicotinic acid compound or mixtures thereof for nocturnal or evening dosing for reducing serum lipids and increasing HDL-cholesterol. In accordance with the present invention, and by way of example, a composition for oral administration during the evening hours to alter serum lipids comprised of nicotinic acid and hydroxypropyl methylcellulose in the form of an extended or sustained release tablet or caplet coated with a coating comprising an HMG-CoA reductase inhibitor in immediate release form is disclosed. Also in accordance with the present invention, the pharmaceutical combinations may include a nonsteroidal anti-inflammatory agent for reducing the capacity of nicotinic acid or nicotinic acid compounds to provoke flushing reactions in individuals.

    COMBINATIONS OF HMG-COA REDUCTASE INHIBITORS AND NICOTINIC ACID AND METHODS FOR TREATING HYPERLIPIDEMIA
    16.
    发明公开
    COMBINATIONS OF HMG-COA REDUCTASE INHIBITORS AND NICOTINIC ACID AND METHODS FOR TREATING HYPERLIPIDEMIA 失效
    作者HMG-CoA还原酶抑制剂和烟酸和方法,用于治疗高脂血症的组合

    公开(公告)号:EP1003515A1

    公开(公告)日:2000-05-31

    申请号:EP98938227.0

    申请日:1998-07-31

    摘要: The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis. The present invention also relates to methods of altering serum lipids in subjects to treat, for example, hyperlipidemia in hyperlipidemics, lipidemia in normolipidemics diagnosed with or predisposed to cardiovascular disease, and atherosclerosis, by administering such oral solid pharmaceutical combinations once per day as a single dose during the evening hours, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis, or without causing in at least an appreciable number of individuals drug-induced hepatotoxicity, myopathy or rhabdomyolysis to such a level that discontinuation of such therapy would be required. More particularly, the present invention concerns oral solid pharmaceutical combinations comprised of, for example, (1) an HMG-CoA reductase inhibitor for immediate or extended release, (2) nicotinic acid, a nicotinic acid compound or mixtures thereof, and (3) a swelling agent to form a sustained release composition for extended release of the nicotinic acid or nicotinic acid compound or mixtures thereof for nocturnal or evening dosing for reducing serum lipids and increasing HDL-cholesterol. In accordance with the present invention, and by way of example, a composition for oral administration during the evening hours to alter serum lipids comprised of nicotinic acid and hydroxypropyl methylcellulose in the form of an extended or sustained release tablet or caplet coated with a coating comprising an HMG-CoA reductase inhibitor in immediate release form is disclosed. Also in accordance with the present invention, the pharmaceutical combinations may include a nonsteroidal anti-inflammatory agent for reducing the capacity of nicotinic acid or nicotinic acid compounds to provoke flushing reactions in individuals.

    PRETREATING HYPERLIPIDEMIC INDIVIDUALS WITH A FLUSH INHIBITING AGENT PRIOR TO NICOTINIC ACID THERAPY
    17.
    发明公开
    PRETREATING HYPERLIPIDEMIC INDIVIDUALS WITH A FLUSH INHIBITING AGENT PRIOR TO NICOTINIC ACID THERAPY 失效
    患者提供了高脂血症抑制剂皮肤发红烟碱治疗前治疗

    公开(公告)号:EP0999844A1

    公开(公告)日:2000-05-17

    申请号:EP98937313.9

    申请日:1998-07-31

    摘要: The present invention relates to pretreating individuals with an effective amount of a flush inhibiting agent for a sufficient period of time prior to the start of single daily dose nicotinic acid therapy to reduce the capacity of nicotinic acid to induce flushing reactions in such individuals during nicotinic acid therapy. In accordance with the present invention, the flush inhibiting agents are administered orally one to four times a day, and preferably one to two times per day, for between about 7 to about 14 days prior to the start of the nicotinic acid therapy. Examples of flush inhibiting agents include nonsteroidal anti-inflammatory agents. Aspirin is a prefered flush inhibiting agent and may be orally administered in daily doses of between about 80 mg to about 1000 mg, and preferably between about 80 mg and about 650 mg, and more preferably between about 80 mg and about 325 mg, during the pretreatment period. Also consistent with the present invention, the pretreatment therapy may be continued during and administered concurrently with the nicotinic acid therapy, in which the nicotinic acid is preferably administered once per day as a single dose during the evening hours or before or at bedtime. The nicotinic acid may be administered alone or in combination with HMG-CoA reductase inhibitors as well as other lipid-altering agents, like cholestyramine and colestipol.