The Preparation Research Of Solid SMEDDS For Oryzanol

Objects:To prepare S-SMEDDS of oryzanol which has less secondary action and higher biological availability. The preparation of oryzanol are upgraded.Some saponins with the similar pharmacologic action as oryzanol are chosen to be the emulsifying agent. The utilization dosage of synthesis SA are reduced,the venenosity are lowered and the synergism pharmacodynamic action are enhanced.Methods:Pre-formulation studies of oryzanol were carried out. UV method was built to measure the contents of oryzanol. The solubilities of oryzanol in different SA,Co-SA and oil were measured. Oil-Water coefficient of distribution of oryzanol were measured. The suitable SA,Co-SA and Oils were screening by drawing the psedu ternary diagram .The optimize preparations were selected on the basis of emulsifying velocity particle diameter .The fitable adsorbing materials were chosen to prepared the S-SMEDDS.The preliminary quality control was carried out. Vitro dissolutions in three mediators were determned.The oryzanol exists metabolic product sodium ferulate in blood.HPLC method was built to measure the content of sodium ferulate.By lavaging rats with the suspension of oryzanol tablets,the micelle solution of oryzanol and S-SMEDDS of oryzanol these AUC were measured.Results:The Oil-Water coefficient of distribution of oryzanol was 1.22±0.07.The recovery rate lines between 95%～107%.Experiments in vivo show that suspl of oryzanol tablet,emulsifier micelle solution of oryzanol and oryzanol SMEDDS solution has the Tmax Cmax,AUC of 2.49,2.51,2.32 hours,11.85, 6.98,7.01μg/ml, 55.0,20.3,25.3μg/ml*h.Conclusions:The results show that the dosage-carried of oryzanol S-SMEDDS is improved highly.The SMEDDS solution of oryzanol are less fluctuating in blood-drug concentration and the AUC is higher than the other two. The results demonstrate that the biological availability of solid oryzanol SMEDDS is improved obviously.