OBJECTIVE: To prepare Desvenlafaxine succinate (DVS) sustained-release pellets capsules, and to investigate the release property in vitro of pellets. METHODS: The pellets containing DVS were prepared by alcohol solution. The quality and micromeritics of DVS pellets were studied. Using ethylcellulose (EC) and hydroxypropyl methyl cellulose (HPMC) as coating materials, DVS sustained-release pellets were prepared by fluid-bed, and then put into enteric hollow capsule. The release property in vitro of DVS sustained-release pellets, and the effects of different drying time (1-24 h) and artificial gastric juice on drug release were investigated. RESULTS: DVS pellets and DVS sustained-release pellets were smooth and had scattered ostiole in surface. The content of DVS in DVS pellets was 19.56% (RSD=0.53%, n=10), and drug-loading rate was 94%; bulk density was 0.792 1 g/ml; roundness degree was 7.84 °; angle of repose was 21.3 °. There was no statistical significance in the difference of drug release for DVS sustained-release pellets after dried for different time (P>0.05), and accumulative release rate decreased 3 h after treated with artificial gastric juice; the release regularity of DVS sustained-release pellets fitted to first-order kinetic equation. CONCLUSIONS: DVS sustained-release capsules are prepared successfully by this method, and can be not dried during preparation.
关键词
琥珀酸去甲文拉法辛缓释微丸流化床包衣体外释药制备
Keywords
Desvenlafaxine succinateSustained-release pelletFluid-bed coatingDrug release in vitroPreparation