Evaluation Of Preparation Methods And Character For Solid Dispersion Based On Improving Dissolution Behavior Of Ibuprofen

Ibuprofen（IBU） solid dispersions（SD） were prepared using fusion method,supercritical fluid method and pulse combustion dryer method in order to improve the dissolution property of IBU.The physicochemical properties of SD were investigated and SD tablets were prepared.Studies were made about process in vivo of rat for solid dispersions.SDs of IBU were prepared with Kollidon system,Kollicoat IR,hydrophilic silica particles（Aerosil and Sylysia） as carriers using fusion method.Differential scanning calorimetry（DSC） and powder X-ray diffraction（PXRD） analysis showed that IBU in SDs had changed to an amorphous state.The dissolution rate of IBU from all SD systems prepared by fusion method increased markedly,corresponding to PMs and pure IBU.Type and property（particle size,specific surface,interval porosity et al.） of carriers had great effect on the dissolution of the drug.IBU solid dispersions were prepared using supercritical fluid method.Preparation condition for forming SD was investigated.DSC and PXRD analysis showed that IBU in SDs had changed to an amorphous state.IR analysis proved that a hydrogen bond was formed between IBU and carrier.Result of dissolution test indicated that dissolution rate of IBU in the SDs prepared by supercritical fluid method was markedly improved.IBU solid dispersions were prepared with Kollidon,Kollicoat IR,HPMC,PVA as carriers using a pulse combustion dryer system.DSC and PXRD analysis indicated that IBU in SDs with Kollidon and HPMC systems of 1:5 ratio as carriers had possibly changed to an amorphous state,also with Kollicoat IR of 1:10 ratio as carriers.IBU in SDs with PVA systems as carriers were crystal.IR analysis proved that interactions between the drug and Kollidon existed.The dissolution property of IBU in the SDs was markedly enhanced and the dissolution rate for IBU-Kollidon SDs prepared by pulse method was improved markedly than that prepared by the spray dryer.Comparing dissolution rate,cumulative dissolution, solubility and stability for three methods,systematic evaluations were carried out about three methods.IBU-Sylysia 350 SD tablets were prepared.Effect of various kinds of factors（type and amount of disintegrant and loading agent,pressure,surface area et al.） for dissolution was investigated.IBU-Kollidon CL SD disaggregation tablets were prepared.Disaggregation time in vitro and in oral cavity was determined.Optimization prescriptions of two types of tablet were determined.With physical mixture（PM） as the reference,studies were made about release behavior of rats in vivo by means of HPLC.The C_max of SD prepared by supercritical fluid method and pulse method are 19.29μg/ml and 16.99μg/ml,T_max is 33 min and 39min,however,C_max of PM is 6.87μg/ml,T_max is 48 min.