琥珀酸索利那新口腔崩解片的制备及质量研究

Preparation and Quality of Analysis Solifenacin Succinate Orally Disintegrating Tablets

目的采用干法制粒制备琥珀酸索利那新口腔崩解片,并对其进行质量评价。方法以崩解时间为考察指标,采用正交试验设计对处方进行优化,以处方中微晶纤维素用量、甘露醇的用量及交联羧甲基纤维素钠的用量为因素进行处方的优化。对优化后处方所制片剂进行崩解时间、体外溶出度验证试验、含量测定及影响因素(高温、强光、高湿)考察。结果最佳处方为微晶纤维素的用量50mg/片、甘露醇的用量30mg/片、交联羧甲基纤维素钠的用量5mg/片,所制片剂崩解时间约为15s,5min时溶出度可达95%。影响因素试验中制剂的稳定性均较好。结论成功制备了索利那新口腔崩解片,各指标符合规定,该处方工艺可靠。

Objective Solifenacin succinate orally disintegrating tablets were prepared by granulation method, and the quality was controlled effectively. Methods The formulation of orally disintegrating tablets were optimized by orthogonal design using disintegration time as the main evaluation parameter. The amount of microcrystalline cellulose （MCC）, mannitol, croscarmellose sodium （CCMC-Na） was used as factors. Then verification test on the in vitro drug dissolution characteristics, content and influencing factors （high temperature, high light, and high moisture） of the optimized tablets were investigated as well. Results The optimized formulation of solifenacin succinate orally disintegrating tablets was as follows： 50 mg MCC, 30 mg Mannitol and 5 mg CCMC-Na. The disintegration time of the tablets was about 15 s and the accumulative dissolution rate in 5 min was up to 95%. In the influencing factor test, the tablets were stable. Conclusions Solifenacin Succinate orally disintegrating tablets are prepared successfully and controllable in quality. The technology is stable and reliable.