Kos Pharmaceuticals, Incorporated

Pharmena S.a.

Eugenio A Cefali

Jerzy Gebicki

David J Bova

Intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, such as Cmax, Tmax and AUC, which are suitable for oral administration once per day 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 intermediate nicotinic acid formulations can be administered as tablets in dosage strengths of, for example, 375 mg, 500 mg, 750 mg and 1000 mg.

Intermediate release nicotinic acid compositions for treating hyperlipidemia

Intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, which are suitable for oral administration once per day as a single dose preferably administered 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 intermediate nicotinic acid formulations can be administered as tablets in dosage strengths of, for example, 375 mg, 500 mg, 750 mg and 1000 mg. The 375 mg, 500 mg and 750 mg nicotinic acid tablets of the present invention have a dissolution curve similarity fit factor F of at least about 79, and the 1000 mg nicotinic acid tablets of the present invention have a dissolution curve similarity fit factor F of at least 44.

Intermediate release nicotinic acid compositions for treating hyperlipidemia having unique biopharmaceutical characteristics

Methods for reducing flushing in individuals being treated for hyperlipidemia with nicotinic acid are disclosed. According to the methods of the present invention, flushing can be reduced in individuals under going nicotinic acid therapy without causing drug-induced hepatotoxicity to a level that would require the nicotinic acid therapy to be discontinued by orally administering to the individuals intermediate nicotinic acid formualtions having unique biopharmaceutical characteristics as a single dose once per day. While the methods of the present invention contemplate administering the intermediate release nicotinic acid formulations at any time during a 24 hour period, it is preferable to administer them once-a-day as a single dose during the evening or at night between about 6:00 pm. and 12:00 a.m., preferably between about 8:00 p.m. and 12:00 a.m., and most preferably between about 8:00 p.m. and 10:00 p.m.

Methods for reducing flushing in individuals being treated with nicotinic acid for hyperlipidemia

Intermediate release nicotinic acid formulations having unique urinary metabolite profiles, which are suitable for oral administration once-a-day as a single dose during a 24 hour period for treating hyperlipidemia without causing drug-induced hepatotoxicity or drug-induced elevations in uric acid or glucose or both to levels that require the therapy to be discontinued, are disclosed.

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Fort Lauderdale, FL, United States of America

Eugenio A Cefali