摘要
目的利用泡腾剂提供稳定持续的释药动力,制备葛根素(PU)泡腾性渗透泵控释片,并考察其体外释药机制。方法以碳酸氢钠和柠檬酸为泡腾剂,聚氧乙烯N80为助悬剂制备片芯;以醋酸纤维素为包衣材料,邻苯二甲酸二乙酯为增塑剂,聚乙二醇-400为致孔剂制备PU单层渗透泵片;以体外释放度为评价指标,单因素考察确定最佳处方。结果泡腾剂种类和用量、助悬剂的种类和用量、促渗剂的种类及剂量、包衣增重对累积释放度均有显著影响,增塑剂、释放介质及转速对累积释放度无显著影响。考察工艺的重现性,并对其释药曲线进行模型拟合,结果表明工艺可重现。结论成功制备了PU泡腾性渗透泵控释片,其在12 h内呈现零级释放(r>0.999 0),药物释放比较完全(累积释放度>85%),工艺简单。
Objective To prepare pueratin （PU）-effervescent osmotic pump （controlled release） tablets （EOPT） based on the stable and sustained drug release dynamics of effervescent, and to study their in vitro release mechanism. Methods The EOPT cores were prepared using sodium hydrogen carbonate and citric acid as effervescent and polyethylene oxide N80 as suspending agent. The PU monolayer osmotic pump tablets were prepared using acetyl cellulose as coating, diethyl phthalate as plasticizer, and PEG 400 as porogen. The single-factor test was used to optimize the formulation depending on drug release. Results The types and amounts of effervescent agent, suspending agent, osmotic promoter, and the weight of coating substance showed the significant influence on the cumulative release rate, while the amount of plasticizer in the coating, the release media, and the rotation rate had no significant effects on the drug release. The drug release model was fitting and the results of in vitro release model simulation showed a good reproducibility. Conclusion A successful method for the preparation of PU-EOPT is developed. More than 85% of PU is released from PU-EOPT within 12 h in vitro （r 〉 0.999 0） following with zero-order release and the preparation process is simple.
出处
《中草药》
CAS
CSCD
北大核心
2013年第6期686-691,共6页
Chinese Traditional and Herbal Drugs
基金
黑龙江省博士后科研启动金(LBH-Q11077)
哈尔滨商业大学研究生创新科研资金(YJSCX2011-188HSD)
关键词
葛根素
泡腾
渗透泵
控释
体外释药
pueratin
effervescent
osmotic pump
controlled release
cumulative release rate
