卡托普利脉冲片的制备及处方优化

Preparation and prescription optimization of Captopril Pulse Tablets

目的以卡托普利为药物模型,用其制备蜡质脉冲片。方法采用湿法制粒制备速释片芯,再用熔融法制备蜡质包衣,采用干法包衣技术制备卡托普利脉冲片;以释药时滞为指标,采用星点设计进行实验,通过效应面法预测最佳处方,并对其进行验证。结果优化得到最优处方,交联聚乙烯吡咯烷酮为10%,聚乙二醇6000为34.32%,硬度为4,优化得到的处方时滞在250 min,并且脉冲片能够在25 min左右起漂,并能持续漂浮。结论采用星点设计-效应面法优化出来的处方结果较为良好,并且得到的脉冲片具有良好的控释能力。

Objective To prepare the pulsatile release tablets of Captopril. Methods The core of tablet was manufactured by wet-granulation squashing squashing mathod and useing melting method to prepare waxy coated.The evaluation parameter was lag time.Experiments were done on the central composite design.The possibly optimal formulation was predicted by response surface method.The lag time of the tablets prepared under the optimum condition was compared with the predicted. Results Optimized to the best prescription,PVPP was 10%,PEG6000 was 34.32%,hardness was 4.The lag time in vitro of the tablets prepared under the optimum conditions was about 250 minutes and the pulsatile release tablets was able to float in 30 min and keep floating. Conclusion Central composite design-response surface methodology was successful in optimizing the preparation of tablets with accurate prediction and to prepare the pulsatile release tablets have good control of release.