葡萄内酯分散片的处方筛选及其溶出度测定

Formulation Screening and Solubility Determination of Auraptene Dispersible Tablets

摘要:

目的: 优化葡萄内酯分散片的制备工艺及考察其体外溶出度. 方法: 以休止角、硬度、崩解时限为指标,考察交联聚乙烯吡咯烷酮(PVPP),微晶纤维素(MCC)、预胶化淀粉(PRS)、低取代羟丙基纤维素(L-HPC)、羧甲基淀粉钠(CMS-Na)等辅料对葡萄内酯分散片处方工艺的影响.采用HPLC测定分散片的体外溶出度,流动相甲醇-水(95:5),检测波长325 nm. 结果: 最佳处方为葡萄内酯10 g,MCC 40 g,L-HPC 20 g,PVPP 10 g,CSM-Na 20 g,PRS 30 g,淀粉20 g;崩解时间1 min,分散均匀性好,药物30 min内累积溶出率>85%. 结论: 制备的葡萄内酯分散片具有溶散快、分散均匀、溶出速率快的特性,适用于临床应用需要.

Abstract:

Objective: To optimize formulation process of auraptene dispersible tablets and evaluate its in vitro dissolution. Method: With angle of repose,hardness and disintegration time as indexes,effects of cross-linking polyvinyl pyrrolidone(PVPP),microcrystalline cellulose(MCC),pregelatinized starch(PRS),low substituted hydroxypropyl cellulose(L-HPC),sodium carboxymethyl starch(CMS-Na) and other excipients on formulation process were investigated.In vitro dissolution of dispersible tablets was determined by HPLC,mobile phase of methanol-water(95: 5),detection wavelength was set at 325 nm. Result: Optimal formula was as follows:auraptene 10 g,MCC 40 g,L-HPC 20 g,PVPP 10 g,CSM-Na 20 g,PRS 30 g,amylum 20 g;dispersible tablets disintegrated uniformly in 1 min,cumulative dissolution of this drug was more than 85% within 30 min. Conclusion: These prepared auraptene dispersible tablets have a fast,homogeneously dispersing profile and good releasing characteristics,which is suitable for clinical application.