The bioavailability of sustained release nicotinic acid formulations. 1991

P J Neuvonen, and L Roivas, and K Laine, and O Sundholm
Department of Pharmacology, University of Turku, Finland.

1. The bioavailability of three nicotinic acid formulations was investigated in a randomized cross-over study. 2. Single doses of nicotinic acid (500 mg) were given to seven healthy volunteers. The concentrations of nicotinic acid and its main metabolite nicotinuric acid were measured in serum up to 8 h and in urine up to 24 h. 3. The relative bioavailability of unchanged nicotinic acid from two slow release formulations compared with a rapid-release form was only 1% and 25%, respectively. Relative values of AUC (0.8 h) for nicotinuric acid were 15% and 58%, and relative urinary recoveries were 18% and 59%, respectively. Facial flushing was less when slow release formulations were used. 4. The bioavailability of unchanged nicotinic acid is low and the ratio of nicotinuric acid to nicotinic acid in serum and urine is high when slow release formulations are used.

UI MeSH Term Description Entries
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008297 Male Males
D009525 Niacin A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties. Nicotinic Acid,3-Pyridinecarboxylic Acid,Enduracin,Induracin,Lithium Nicotinate,Niacin Aluminum Salt,Niacin Ammonium Salt,Niacin Calcium Salt,Niacin Cobalt (2+) Salt,Niacin Copper (2+) Salt,Niacin Hydrochloride,Niacin Iron (2+) Salt,Niacin Lithium Salt,Niacin Lithium Salt, Hemihydrate,Niacin Magnesium Salt,Niacin Manganese (2+) Salt,Niacin Potassium Salt,Niacin Sodium Salt,Niacin Tartrate,Niacin Tosylate,Niacin Zinc Salt,Nicamin,Nico-400,Nicobid,Nicocap,Nicolar,Nicotinate,Wampocap,3 Pyridinecarboxylic Acid,Aluminum Salt, Niacin,Hydrochloride, Niacin,Nico 400,Nico400,Nicotinate, Lithium,Potassium Salt, Niacin,Sodium Salt, Niacin,Tartrate, Niacin,Tosylate, Niacin
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities

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