更昔洛韦口腔崩解片的处方优化及质量评价

Formula Optimization and Quality Evaluation of Ganciclovir Oral Disintegrating Tablets

目的:优化更昔洛韦口腔崩解片的处方,并评价其质量。方法:以崩解时限为评价指标,通过单因素试验筛选崩解剂、稀释剂和润滑剂的种类,并通过正交试验对崩解剂、稀释剂、润滑剂和矫味剂用量进行优化。对优选处方制得的口腔崩解片进行质量检查,包括崩解时限、含量测定、体外溶出度和加速试验。结果:最佳处方为:10%交联聚维酮、30%微晶纤维素、3%微粉硅胶和2%阿斯巴甜。三批样品的崩解时限分别为47.4,48.6,47.8 s;含量分别为100.2%,99.7%,99.8%;2 min时累积溶出度达到80%以上;加速试验3个月的样品检测指标与0天相比无明显变化。结论:更昔洛韦口腔崩解片的处方及工艺稳定可行,重复性好,制得的样品质量均符合要求。

Objective： To optimize the formula of ganciclovir oral disintegrating tablets, and evaluate the quality. Methods： The disintegration time was used as the evaluation index, the disintegration agent, diluent and lubricant were screened by single factor experiments, and the amounts of disintegration agent, diluent, lubricant and flavoring agent were optimized by orthogonal tests. The quality of ganciclovir oral disintegrating tablets was determined including the disintegration time, contenl determination, dissolution in vitro and accelerated stability test. Results： The best formula was as follows： 10% PVPP, 30% MCC, 3% silica gel and 2% aspartame. The disintegration time of three batches of samples was 47.4, 48.6 and 47.8 s, and the content was 100.2%, 99.7% and 99.8%, respectively. The cumulative dissolution in 2 rain reached more than 80%. Compared with those on 0 day, the indicators of samples after 3-month accelerated test had no significant changes. Conclusion： The formula and preparation process of ganciclovir oral disintegrating tablet are stable, feasible and reproducible, and the quality of samples meets the related requirements.