Studies And Assessment On Rutin Self-microemulsifying Drug Delivery System

PURPOSE:Rutin self-microemulsifying drug delivery system(PB-SMEDDS) would be prepared,to improve its oral bioavailability and meet the requirement for clinical use.METHOD:Pre-formulation studies of oryzanol were carried out. HPLC(High performance liquid chromatogram)methodwas built to measure the contents of Rutin. The solubilities of oryzanol in different SA,Co-SA and oil were measured. Oil-Water coefficient ofdistribution of Rutin were measured. Pseudo-ternary phase diagrams,oil(TAC)-mix emulsifier(Shot)-Water,were constructed by water-dropping method,to identify the efficient self-emulsification region, The prescription ofPB-SMEDDS was optimized by multi-target orthogonal experiment; Pharmaceutics assessment for the certain prescription of RUT-SMEDDS, Vitro dissolutions and stability experiments were determned; HPLC method was built to measure the content of Rutin in vivo, By lavaging rats with the suspension of Rutin tablets and RUT-SMEDDS these AUC were measured.RESULT:HPLC method of Rutin was developed for assay.The regression equation is Y=77529X+11844,which is linear over the range of 12.75-255ug/ml. The recovery rate lines between 99.32%-98.82%, Experiments in vivo show that suspl of Rutin tablet and RUT-SMEDDS solution has the Cmax,AUC of 6.98±1.13,11.85±1.79 ug/ml and 20.3±2.10,55.0±4.01 h*ug/ml. Conclusions:The results show that the dosage-carried of RUT-SMEDDS is improved highly.The SMEDDS solution of Rutin are less fluctuating in blood-drug concentration and the AUC is higher than the Rutin tablets.The results demonstrate that the biological availability of RUT-SMEDDS is improved obviously.