Nicotinic acid compositions for treating hyperlipidemia and...

A - Human Necessities – 61 – K

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A61K 31/455 (2006.01) A61K 9/22 (2006.01) A61P 3/06 (2006.01)

Patent

CA 2574987

An oral dosage sustained release pharmaceutical formulation for use once per day during the evening or at night, or before bedtime, as a single dose, has use in daily treatment of hyperlipidemia in a patient without inducing treatment-limiting liver damage, the formulation comprises a compressed blend of nicotinic acid in a hydrophilic matrix which controls delivery of the nicotinic acid; the compressed blend comprises agglomerates and contains an effective antihyperlipidemic amount of nicotinic acid, a swelling agent, a granulation binder, and a lubricant; the swelling agent is a hydrophilic polymer which on initial wetting starts to partially hydrate forming a gel layer, such that as water permeates into the formulation the thickness of the gel layer increases and the nicotinic acid diffuses out of the gel layer and an outer layer of the formulation erodes with increasing hydration, whereby the swelling agent of the hydophilic matrix provides controlled sustained release of the nicotinic acid from the hydophilic matrix, whereby the blend forms an oral sustained release solid dosage form in which the sustained release is without inducing treatment- limiting liver damage to the liver of the patient.

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