酮洛芬肠溶口腔崩解片的处方优化

Formulation of ketoprofen enteric and rapidly disintegrating tablets

目的优化酮洛芬肠溶口腔崩解片的处方,考察不同压片力和不同微晶纤维素与甘露醇比例对空白崩解片孔隙率、抗张强度和崩解时限的影响。方法采用乳化溶剂扩散法制备酮洛芬肠溶微球;以微球为原料,采用粉末直接压片法制备口腔崩解片。用Statistica统计软件对处方组成进行优化,确定微晶纤维素与甘露醇的比例。结果微晶纤维素用量一定时,随压片力的增大,空白崩解片的孔隙率减小,抗张强度增大,崩解时限延长;压片力一定时,随微晶纤维素用量的增加,空白崩解片的孔隙率和抗张强度增大,崩解时限延长;根据处方优化的结果,选择微晶纤维素与甘露醇质量比为3∶1。当片剂中加入质量分数为8%的PVPP作为崩解剂时,空白崩解片的抗张强度略微增加,崩解时限显著缩短。结论根据优化后的处方,采用粉末直接压片法制备的酮洛芬肠溶口腔崩解片符合设计要求。

Objective To optimize the preparation of ketoprofen enteric and rapidly disintegrating tablets. Methods The effects of different pressures and MCC to mannitol ratios on the porosity, tensile strength （ St） and disintegration time （/d） of blank tablets were investigated. The optimal formulation was picked out by the analysis of Statistica software. The effect of different kinds of disintegrants and their amounts on St and td of blank tablets were also tested. Then, ketoprofen enteric and rapidly disintegrating tablets were prepared by direct compression method. Results The porosity of blank tablets was decreased gradually and St and td were increased significantly with the increase of the pressure. The porosity and St of blank tablets were increased, while td was decreased under the same compression when the ratios of MCC to mannitol was increased. When MCC-mannitol ratio was three and the amount of PVPP was 8 %, the blank tablets were fine at St and td. Conclusions Ketoprofen enteric and rapidly disintegrating tablets meet the requirements of the standard.