The bioavailability of sustained release nicotinic acid formulations.

Neuvonen, Pertti J.; Roivas, Leena; Laine, Kari; Sundholm, O.

doi:10.1111/j.1365-2125.1991.tb03933.x

Cited by 13 publications

(10 citation statements)

References 13 publications

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“…NA has a relative bioavailability of up to 25%, whereas 15-30% of the absorbed vitamin bounds to plasma proteins. NA has an extensive hepatic metabolism, which is also associated with the hepatic toxicity caused by higher doses of NA [45][46][47]. Buccal delivery of APIs has the main advantage of bypassing the first pass effect, including the avoidance of presystemic elimination within the GI tract.…”

Section: Discussionmentioning

confidence: 99%

Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins

et al. 2020

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Buccal films containing two vitamins, i.e., thiamine hydrochloride (THCl) and nicotinic acid (NA), were fabricated via two-dimensional (2D) inkjet printing. For the preparation of buccal films, solubility studies and rheological evaluations were conducted in distilled water and propylene-glycol (PG) as main solvent and viscosity/surface tension modifier, respectively. The increased solubility in the solvents’ mixture indicated that manufacturing of several doses of the THCl and NA is achievable. Various doses were deposited onto sugar-sheet substrates, by increasing the number of printing passes. The physiochemical characterization (SEM, DSC, FTIR) revealed that inkjet printing does not affect the solid state of the matrix. Water uptake studies were conducted, to compare the different vitamin-loaded formulations. The in vitro release studies indicated the burst release of both vitamins within 10 min, a preferable feature for buccal administration. The in vitro permeation studies indicated that higher concentrations of the vitamins onto the sugar sheet improved the in vitro permeation performance of printed formulations.

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Section: Discussionmentioning

confidence: 99%

Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins

et al. 2020

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“…[6][7][8] The rate and extent of the metabolite formation via the glycine conjugation pathway (pathway 1, NUA) following niacin administration have been shown to depend on the rate of niacin release from the niacin formulations following single-dose administrations of 500 mg niacin. 18,19 However, the effect of rate on the NAM metabolic pathway (pathway 2) or at therapeutic doses of 2000 mg has not been characterized. The objective of this study was to characterize the single-dose pharmacokinetics of 2000 mg niacin in solution delivered orally at different input rates.…”

Section: Discussionmentioning

confidence: 99%

“…Immediate‐release niacin is associated with cutaneous flushing, whereas sustained‐release formulations have been associated with hepatotoxicity 6 – 8 . The rate and extent of the metabolite formation via the glycine conjugation pathway (pathway 1, NUA) following niacin administration have been shown to depend on the rate of niacin release from the niacin formulations following single‐dose administrations of 500 mg niacin 18 , 19 . However, the effect of rate on the NAM metabolic pathway (pathway 2) or at therapeutic doses of 2000 mg has not been characterized.…”

Section: Discussionmentioning

confidence: 99%

Effect of the Rate of Niacin Administration on the Plasma and Urine Pharmacokinetics of Niacin and Its Metabolites

Menon

González²,

Adams³

et al. 2007

The Journal of Clinical Pharma

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The metabolic profile of niacin is influenced by the rate of niacin administration. This study characterizes the effect of administration rate on the pharmacokinetics of niacin and its metabolites. Twelve healthy males were enrolled in an open-label, dose-rate escalation study and received 2000 mg niacin at 3 different dosing rates. Plasma was analyzed for niacin, nicotinuric acid, nicotinamide, and nicotinamide-N-oxide. Urine was analyzed for niacin and the metabolites nicotinuric acid, nicotinamide, nicotinamide-N-oxide, N-methylnicotinamide, and N-methyl-2-pyridone-5-carboxamide. C(max) and AUC(0-t) for niacin and nicotinuric acid increased with an increase in dosing rate. The changes observed in plasma nicotinamide and nicotinamide-N-oxide parameters, however, did not correlate to dosing rate. The total amount of niacin and metabolites excreted in urine was comparable for all 3 treatments. However, with the increase in dosing rate, urine recovery of niacin and nicotinuric acid showed a significant increase, whereas N-methyl-2-pyridone-5-carboxamide and N-methylnicotinamide showed a significant decrease.

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“…There is evidence that the flushing symptoms occur while the concentration of nicotinic acid and nicotinuric acid in plasma is increasing, independently of the absolute concentration (Cayen 1985;Neuvonen et al 1991).…”

Section: Discussionmentioning

confidence: 97%

Investigation of niacin on parameters of metabolism in a physiologic dose: randomized, double-blind clinical trial with three different dosages

Schweikart¹,

Reimann²,

Schön³

2009

International Journal of Food Sciences and Nutrition

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The aim of this double-blind, placebo-controlled cross-over design trial was to assess the safety of a multi-vitamin preparation containing nicotinic acid in a physiological dose. Seventy-two healthy volunteers took part in this trial. At six consecutive time-points, we systematically documented blood pressure, pulse, skin temperature and flushing symptoms after an oral dose of up to 50.1 mg nicotinic acid. The results suggest that nicotinic acid in a dosage of 16.7 mg does not cause flushing symptoms. In higher doses up to 50.1 mg, flushing symptoms are sporadically possible. There was no physiologically relevant change regarding the central metabolic parameters blood pressure, pulse and skin temperature.

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The bioavailability of sustained release nicotinic acid formulations.

Cited by 13 publications

References 13 publications

Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins

Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins

Effect of the Rate of Niacin Administration on the Plasma and Urine Pharmacokinetics of Niacin and Its Metabolites

Investigation of niacin on parameters of metabolism in a physiologic dose: randomized, double-blind clinical trial with three different dosages

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