A Former The Mok Secretary Sustained Release Tablets And Its Pharmacokinetic Study

Acipimox is a novel lipid-lowering agent currently used for the treatment of hyperlipoproteinemia. It can effectively lower the risk of coronary heart disease(CHD). To improve the patient compliance and maintain relatively constant plasma concentration, a sustained -release tablet (SRT) administrated once daily was designed and prepared by using hydroxypropylmethylcellulose (HPMC) as basic matrix material.According to the literature, UV spectrophotomatry was developed for in vitro assay of physicochemical properties, content and drug release. High-performance liquid chromatography (HPLC) was applied in the determination of plasma concentration in dogs. The method was quick and accurate which could meet the requirement of the analysis.In the preformulation studies, the drug solubility in various mediums was determined. The influences of formulation, manufacture and release condition on the drug release were investigated with the accumulative drug release over 12 h as standard. Basing on the results of single-factor tests, orthogonal design test was carried out to optimize the formulation and the optimal tablet administrated once a day was screened. Stability studies of acipimox-SRT showed that light, temperature, moisture and air had little effect on the content and release behavior of drug.To study the mechanism of drug release, some factors which greatly influence the drug release were investigated. Finally drug release mechanism was confirmed as non-Fickian diffusion, which was the combination result of diffusion and erosion and mainly by diffusion.The pharmacokinetics of Acipimox SRT and capsule in dogs were studied.