盐酸阿夫唑嗪胃漂浮片的设计、制备与评价

Design,preparation and evaluation of Alfuzosin hydrochloride gastric floating tablets

目的制备盐酸阿夫唑嗪胃漂浮片,并评价其质量。方法使用粉末直接压片工艺制备盐酸阿夫唑嗪胃漂浮片,通过单因素实验确定了盐酸阿夫唑嗪胃漂浮片中辅料的种类和用量。并以HPMC K100M、硬脂醇及NaHCO3的用量为考察因素,以盐酸阿夫唑嗪胃漂浮片的漂浮延迟时间和1、12、20 h时间点的释放度为评价指标,采用Box-Behnken实验设计对盐酸阿夫唑嗪胃漂浮片的处方进行优化,并评价其漂浮延迟时间、漂浮时间以及释放度。结果优化得到每片盐酸阿夫唑嗪胃漂浮片的最优处方组成为:HPMC K100M、硬脂醇、NaHCO3的用量分别为60、14、10 mg,盐酸阿夫唑嗪胃漂浮片漂浮延迟时间为81±2 s,漂浮时间大于24 h,在释药周期内药物释放平稳。结论文中制备盐酸阿夫唑嗪胃漂浮片的工艺具有处方设计合理,制备工艺简单,漂浮延迟时间较短、漂浮时间较长,药物释放平稳等特点,有望进一步开发研究。

OBJECTIVE To prepare Alfuzosin hydrochloride gastric floating tablets(AGFTs)and evaluate its quality.METHODS The AGFTs were prepared by direct compression.The single-factor experiment was used to determine the excipient types and amount in the formulation of AGFTs.Amounts of HPMC K100 M,stearyl alcohol and NaHCO3 were taken as the investigation factors,the floating delay time and dissolution at 1 h,12 h and 20 h were used as the evaluation index,and the formulation of AGFTs was optimized by Box-Behnken experiment design.The floating delay time,floating time and dissolution of AGFTs were evaluated.RESULTS The optimal formulation of AGFTs as followed:the amount of HPMC K100 M was 60 mg,the amount of stearyl alcohol was 14 mg and the amount of NaHCO3 was 10 mg.The floating delay time of AGFTs was 81±2 s,and the floating time was more than 24 h.The dissolution was relatively gentle,and no sudden release occurs.CONCLUSION In this study the prepared AGFTs have reasonable formulation design,simple preparation process,short floating delay time,long floating time and stable drug dissolution.It is expected to be further developed.