Pluronic F127胶束的载药、固化及其片剂的溶出度

Drug loading and solidification of Pluronic F127 micellar solution and dissolution of its tablets

考察Pluronic F127(F127)增溶难溶性药物及载药胶束溶液固化的方法,制备载药胶束的固体制剂,提高口服药物的溶出度。本研究以辛伐他汀(simvastatin,SIM)为模型药物,采用薄膜分散-水化法制备F127-SIM胶束溶液。以载药率为指标,通过正交试验优化载药胶束处方工艺;用喷雾干燥法对胶束进行固化,并对粉末进行物理性质表征;进行复溶实验,考察温度和稀释对载药胶束固体粉末复溶的影响;最后制备成片剂,考察片剂的体外溶出性能。最终得到的胶束载药量为13%,提高了F127对SIM的载药能力,同时SIM在水中的溶解度提高了近950倍。喷雾干燥后,载药胶束粉末为多孔状的无定形固体分散体。复溶后,对温度和稀释的稳定性显著提高。SIM载药胶束片的溶出度显著高于市售片的溶出度。

The purposes of this study were to prepare simvastatin（SIM）-loading Pluronic F127（F127） micellar solution and to study the solidification of the solution as an oral dosage form.Film-hydration method was used to prepared simvastatin（SIM）-loading F127 micellar solution,whose processing parameters were optimized using orthogonal design and drug loading efficiency.Then the drug-loaded micelle solution was solidificated with spray-drying,and the resultant powders were characterized by scanning electron microscopy（SEM）,differential scanning calorimetry（DSC）,powder X-ray diffraction（PXRD）.Aqueous reconstitution of the solidified micellar powders was performed,and the dissolution of tablet containing SIM-F127 micelles was carried out in comparison to commercially available tablets.It was indicated that the solubility of SIM in the micellar solution increased 950 times and that the loading efficiency reached 13%.The amorphous characteristics and good flow property were evident using the spray drying powders.Once upon contact with water,SIM micellar solution was spontaneously reconstituted and more stable against the temperature and dilution.In vitro dissolution test showed that SIM dissolution from the solidification micelles tablet was increased significantly if compared to that of the market tablets.