Physiological research / Academia Scientiarum Bohemoslovaca 2015-01-01

The use of a hydrogel matrix for controlled delivery of niacin to the gastrointestinal tract for treatment of hyperlipidemia.

J Sirc, J Hrib, M Vetrik, R Hobzova, A Zak, B Stankova, O Slanar, R Hromadka, V Sandrikova, J Michalek

Index: Physiol. Res. 64 Suppl 1 , S51-60, (2015)

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Abstract

Hyperlipidemia treatment based on niacin requires gastrointestinal administration of relatively high doses. The recommended dietary allowance of niacin as vitamin B3 is 14 to 16 mg daily in adults, while the doses of niacin used in the treatment of hyperlipidemia are generally in the range of 1 to 3 g. Administration of such large doses requires a high concentration of the active compound in the tablet and proper control of the drug release. In this study, a hydrogel matrix based on poly(2-hydroxyethyl methacrylate) and polyvinylpyrrolidone was investigated as delivery vehicle for controlled NA release into the gastrointestinal environment. The prepared hydrogel matrices varied in used monomer and crosslinker types and concentrations. The content of NA in tablets was between 65-80 %. The release profiles of NA from tablets were examined under three different pH values (1, 4.5 and 6.8) over the time period of 30 h. The effects of the monomer ratio, the crosslinking of the polymer network, and the solubility of niacin during drug release under various pH are discussed. The results showed that the release time period can be achieved in a relatively wide range of time and can be adjusted according to the medical requirements.