头孢氨苄胃漂浮缓释片的制备与质量评价

Preparation and quality evaluation of Cephalexin Gastric Floating Sustained-Release Tablets

目的制备头孢氨苄胃漂浮缓释片,并考察其漂浮延迟时间及体外药物释放度。方法采用粉末直接压片工艺制备头孢氨苄胃漂浮缓释片,采用单因素实验方法筛选得到影响头孢氨苄胃漂浮缓释片体外漂浮延迟时间、漂浮时间和释放度的关键性辅料用量范围,最终以羟丙甲纤维素(HPMC K15M)用量、碳酸氢钠用量以及压片主压力作为考察因素,以头孢氨苄胃漂浮缓释片的漂浮延迟时间和1,4和8 h时间点的药物释放度作为评价指标,通过Box-Behnken实验设计优化得到头孢氨苄胃漂浮缓释片处方设计空间,并在设计空间任取一点连续制备3批头孢氨苄胃漂浮缓释片,评价其漂浮延迟时间及体外释放度。结果优化得到头孢氨苄胃漂浮缓释片的处方设计空间,每片HPMC K15M用量为260 mg,碳酸氢钠用量为60 mg,压片主压力为8 kN,制备的头孢氨苄胃漂浮缓释片漂浮延迟时间仅为12.1±0.5 min,在12 h内药物释放平缓,无药物突释。结论通过Box-Behnken实验设计优化得到的头孢氨苄胃漂浮缓释片处方,漂浮延迟时间较短,12 h维持漂浮状态,药物释放平稳。

Objective To prepare Cephalexin Gastric Floating Sustained-Release Tablets and investigate their floating delay time and drug release in vitro.Methods Cephalexin Gastric Floating Sustained-Release Tablets were prepared by direct compression method.The single-factor experiment method was used to screen the key adjuvant dosage range affecting the floating delay time,floating time and drug release of Cephalexin Gastric Floating Sustained-Release Tablets.Finally,the amount of HPMC K15M,the amount of sodium bicarbonate and the main pressure were taken as the investigation factors,and the floating delay time and at the time points drug dissolution of 1,4 and 8 h were used as the evaluation index.The formulation design space of Cephalexin Gastric Floating Sustained-Release Tablets was optimized by Box-Behnken experiment design,and 3 consecutive batches of Cephalexin Gastric Floating Sustained-Release Tablets were taken in the design space to evaluate the floating delay time and drug release in vitro.Results The formulation design space of Cephalexin Gastric Floating Sustained-Release Tablets was optimized by experiment design.The amount of HPMC K15M was 260 mg per tablet,the amount of sodium bicarbonate was 60 mg per tablet,and the main pressure was 8 kN.The prepared Cephalexin Gastric Floating Sustained-Release Tablets had a floating delay time of only 12.1±0.5 min,and the drug was gently released within 12 h.Conclusion In this study,the preparation of Cephalexin Gastric Floating Sustained-Release Tablets was optimized by Box-Behnken experiment design.The floating delay time was short,the floating state was maintained for 12 h,and the drug release was stable.It is expected to further carry out in vivo pharmacokinetic studies.