Investigation of the sustained-release mechanism of hydroxypropyl methyl cellulose skeleton type Acipimox tablets

Abstract

In this study, we investigate the production of hypolipidemic agents in the form of Acipimox sustained-release tablets, using a wet pelleting process. The purpose of this research is to reduce the total intake time for patients and to lower the initial dose in such that the adverse reactions could be reduced. This study adopts the single-factor method and orthogonal experiments by using hydroxypropyl methyl cellulose (HPMC K15M) as the main sustained-release prescription composition. The final prescription is Acipimox 20%, HPMC K15M 26.67%, sodium carboxymethyl cellulose 30%, polyethylene glycol (PEG 6000) 1%, ethyl cellulose 16.6%, lactose 4.67% and magnesium stearate 1%. The dissolution of tablets reached 85.88% in 8 h. The difference in the weight, hardness and friability of the tables met the requirements in the Chinese Pharmacopoeia; to test the stability, a temperature and illumination accelerated test method was used, the results indicate that the Acipimox sustained-release tablets should be sealed and stored in a dark, cool area. A preliminary study on the tablets’ releasing mechanism showed that their release curve fitted the Higuchi model (the formula is Mt/M∞ = 31.137 t1/2–3.605 (R2 = 0.9903)). The Acipimox tablets’ release principle is dominated by the diffusion mechanism.

Keywords

• acipimox
• sustained-release tablet
• sodium carboxymethylcellulose
• hydroxypropyl methyl cellulose