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

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。

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）, mierocrystalline 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 rain. Conclusion： These prepared auraptene dispersible tablets have a fast, homogeneously dispersing profile and good releasing characteristics, which is suitable for clinical application.