琥珀酸去甲文拉法辛缓释片的制备及体外释药特性研究

Preparation of Desvenlafaxine Succinate Sustained-release Tablets and Study of Release Behavior in Vitro

目的制备琥珀酸去甲文拉法辛(desvenlafaxine succinate,DVS)缓释片,确定最佳处方及制备工艺,并进行体外释放特性研究。方法建立紫外分光光度法测定DVS缓释片的体外释放度,以体外释放度为评价指标,通过单因素考察,确定DVS缓释片的最佳处方及制备工艺。结果最佳处方及工艺:以HPMC K15M为骨架材料,用量50%;MCC为填充剂;硬脂酸镁为润滑剂,用量8%;湿法制粒后,以70 k N的压力压片。制备的DVS缓释片体外释放行为良好,可持续释药24 h,符合试验要求。结论 DVS缓释片的制备工艺稳定可靠,体外释放度测定方法简便易行。

OBJECTIVE To prepare desvenlafaxine succinate sustained-release tablets, determine the best prescription and preparation method, and study its in vitro release property. METHODS Establishing UV spectrophotometry method determine the in vitro release degree of desvenlafaxine succinate sustained-release tablets. With vitro release as index, we determine the best prescription and preparation process through single factor investigation. RESULTS The best prescription and preparation process were as follows： HPMC K15 M was matrix materials, amount of 50%; MCC was filler; magnesium stearate was a lubricant, amount of 8%; preparing wet granules; compressing tablets with pressure of 70 k N. The desvenlafaxine succinate sustained-release tablets had good release property in vitro, and could release drug for 24 h, which met the testing requirements. CONCLUSION The preparation progress of desvenlafaxine succinate sustained-release tablets is stable and reliable, and the in vitro release determination method is simple.