【摘要】 目的通过处方优化制备液体基质的冬凌草总二萜硬胶囊剂,提高冬凌草总二萜的体外溶出度。方法通过不同溶剂中的溶解度实验及体外溶出度实验,筛选并优化处方。结果药物在聚乙二醇400(PEG400)中的溶解度最大,最优处方基质为PEG400,含丙二醇的质量分数为5%、Labra-sol为0.5%,冬凌草甲素在该基质里的表观溶解度达到25.8 g.L-1,最优处方中总二萜在溶出介质水、人工胃液和人工肠液中的45 min累积溶出量均达98%,而冬凌草总二萜粉末中其值仅为53%,且最优处方溶出度受pH的影响较小。结论液体基质的冬凌草总二萜硬胶囊剂能显著提高总二萜的体外溶出度。更多还原

【Abstract】 Objective To prepare hard capsules included rubescens total diterpenoids(RTD) solution and improve its dissolution rate in vitro.Methods The optimal formulation of liquid type carrier was screened through the measurement of apparent solubility in different solvents and dissolution test in vitro.Results RTD solubility in PEG400 was the best among the given solvents.PEG400 containing 5% propylene glycol and 0.5% Labrasol was selected as the optimal carrier for the RTD hard capsule.The apparent solubility of oridonin in RTD was significantly increased to 25.8 g·L-1 in the carrier.RTD dissolution percentage from the optimized formulation was about 98% in distilled water,hydrochloric acid of pH1.2 and phosphate buffer solution of pH6.8.The results were better than that of RTD powder which was only 53%.The RTD dissolution rate from the hard capsules was slightly influenced by pH.Conclusions The dissolution rate of RTD from the hard capsules is obviously enhanced.更多还原