黄芩素包合物单层渗透泵片制备工艺研究

目的 采用包合技术提高黄芩素的溶解度及溶出速率,进而考察渗透泵片片芯及包衣处方对黄芩素包合物单层渗透泵片体外释药行为的影响,并优化最佳处方.方法 利用包合技术制备黄芩素包合物,并测定其溶解度及溶出速率.以累积释放度为评价指标,通过单因素考察NaCl用量、聚氧乙烯(PEO)用量、包衣增重及增塑剂用量对释药行为的影响,并采用正交试验得到黄芩素包合物单层渗透泵片最佳处方.结果 将黄芩素制备成包合物后,溶解度及溶出速率得到显著提高.正交试验结果显示,渗透泵片片芯处方中PEO用量和包衣膜处方中增塑剂聚乙二醇(PEG)400用量对释药行为有较大影响,得到的最佳处方为:黄芩素包合物180 mg,NaCl用量100mg,PEO用量80 mg,包衣增重4％,增塑剂用量为9％.优化后的黄芩素包合物渗透泵片在12 h内呈现良好的零级释放(r=0.997 8),药物释放比较完全(＞88％).结论 以环糊精包合物为中间体成功制备了黄芩素单层渗透泵片,其释药行为符合零级动力学方程.

Preparation technique of monolithic osmotic pump tablet containing inclusion complex of baicalein

Objective Inclusion technology was used to improve the solubility and dissolution rate of baicalein. Then investigated the effects of the formulation of core tablet and coating on drug release from monolithic osmotic tablet and optimize the formulation. Methods Baicalein-inclusion complex was prepared, and the solubility and dissolution rate were also determined. The percent of cumulative release was used as the evaluation standard for the drug release profile in vitro. The effects of amounts of NaCl and PEO, coating weight and plasticizer were investigated through single-factor method. And then the optimal formulation of monolithic osmotic pump tablet containing baicalein-inclusion complex was selected via the orthogonal design. Results After baicalein was prepared into inclusion complex, its solubility and dissolution rate were enhanced greatly. The results of orthogonal design indicated that amount of PEO in core tablet and PEG 400 in coating has significant effects on the drug release. The optimum formulation was: baicalein-inclusion complex 180 mg, NaCl 100 mg, PEO 80 mg, coating weigh 4% and plasticizer 9%. The tablets with optimized formulation could achieve the desired zero-order release profile (r=0.997 8) within 12 hours and the cumulative release was more than 88%. Conclusion Monolithic osmotic pump tablet of baicalein was successfully prepared based on the intermediate of inclusion complex, and the release behavior followed zero-order kinetics equation (Y=7.573 7t+0.692 7).