Comparison between the Absorption of Nicotinic Acid and Pentaerythritol Tetranicotinate (Perycit®) from Ordinary and Enterocoated Tablets

Abstract

Nicotinic acid was shown to be rapidly absorbed from the gastrointestinal tract but also rapidly eliminated from the blood stream. Administration of nicotinic acid was therefore associated with large fluctuations of nicotinic acid concentration in the plasma. Two alternative ways of maintaining a moderate but more constant increase of the nicotinic acid concentration in the blood were studied. One way was to give nicotinic acid as a "sustained release" preparation. Nicotinic acid in enterocoated tablets with dissolution times of 2 hrs (in simulated intestinal juice), induced only an irregular and transitory increase of the plasma nicotinic acid concentration after 5 hrs and in some subjects only a reduction in plasma FFA. Enterocoated tablets with a dissolution time of 4 hrs were ineffective. Nicotinic acid is a weak acid and as such is poorly absorbed from the more distal parts of the digestive tract. Therefore the biological prerequisites for this alternative method were not so good. The second alternative method studied was to give a nicotinic acid ester which would continuously release nicotinic acid in the body. The nicotinic acid ester used (pentaerythritol tetranicotinate, perycita, Bofors) given in an oral dose of 1 g, was found to give a moderate but consistent and prolonged increase in the free nicotinic acid concentration and a consistent decrease in the FFA-level of plasma with a moderate flush. Nicotinic acid in ordinary tablets and in an equivalent dose induced a considerably more pronounced flush and a somewhat larger reduction in plasma FFA which however was of shorter duration. The decrease was accompanied by a secondary and prolonged elevation of the plasma FFA concentration. This secondary increase was not observed in the experiments with pentaerythritol tetranicotinate. The possible importance of these differences from a pharmacotherapeutical point of view is discussed.

Nicotinic acid: an old drug with a promising future

“…After oral administration, nicotinic acid is absorbed rapidly and maximal plasma concentrations are reached after 30–60 min. The plasma half‐life after administration of 1 g nicotinic acid is around 1 h ( Carlson et al , 1968b ; Svedmyr and Harthon, 1970 ). Nicotinic acid is in part metabolized by the liver and in part excreted unchanged by the kidney.…”

Niacin Alternatives for Dyslipidemia: Fool’s Gold or Gold Mine? Part I: Alternative Niacin Regimens

“…Having used combination therapy, the SIHDS is corroboratory but less definitive than the CDP. Furthermore, having used a longer acting pro-drug [ 29 ], we think SIHDS supports the concept that dosing 1 g thrice daily is more important than the release rate of free nicotinic acid. Long-term follow-up of CDP revealed the niacin-treated group had lower all-cause mortality despite stopping niacin after 5 years [ 4 ].…”

pH-Responsive Inorganic/Organic Nanohybrids System for Controlled Nicotinic Acid Drug Release

“…Additionally, it was reported that oral administration of NA in human gut rapidly absorbed with fast blood clearance in 1.5–2 h. According to the experiment, 1 g of orally administered NA had an improved plasma level of free NA (26–28 µg/mL), which was rapidly cleared after 6 h. Moreover, the plasma level of NA showed no elevation, and the pharmacological effects and even the drug disappeared in less than an hour after infusion being inactivated [ 12 , 13 ]. Additionally, NA-IR required a multiple-dosage regimen to meet the required efficacy (typically two or three times a day) [ 14 , 15 , 16 ].…”