Construction Of Fasudil Hydrochloride Liposome Tablets And Application Study On Release Performance

Objective:The model drug was Fasudil hydrochloride(FH).Using niosome technology,the commercially available injection dosage form was changed to oral tablets.To establish in vitro analysis methods,To optimize the Fasudil hydrochloride liposome and its tablet prescription,preparation technology.The liposome powder of fasudil hydrochloride was evaluated.The mechanism of drug release in vitro was investigated by mathematical model fitting.It provides more basis for the new technology research of fasudil hydrochloride.Method:To establish a HPLC method for the analysis of fasudil hydrochloride and the determination of its release in vitro.In order to optimize the preparation process of fasudil hydrochloride niosome,the entrapment rate was taken as the index,and the single factor method and response surface test were used to optimize the niosome.The niosome of fasudil hydrochloride were characterized by differential thermal scanning(DSC),infrared scanning and particle size.The formation of niosomes was verified by verification test.The preparation technology of niosome tablets was optimized by single factor test,and the quality of fasudil hydrochloride niosome tablets was evaluated with the characteristics,hardness and reactant Angle of tablets as the indexes.The release mechanism of fasudil hydrochloride niosome tablets was fitted by mathematical model.Results:The method of HPLC analysis and in vitro release degree of fasudil hydrochloride are stable and feasible.The optimal preparation process of fasudil hydrochloride niosomes was determined by single factor investigation and response surface test.The final prescription preparation process for FH-NIO is follows: the ratio of organic phase to water phase is(3:1),The organic phase is diethyl ether,.its dosage is 21 ml,PBS is the water phase,dosage is 7ml,surface-to-bile ratio is(11:1),drug-to-bile ratio is 0.6:1,HLB value of emulsifier is 6.25,dosage of emulsifier is1.35 g,ultrasonic emulsification time is 6min,hydration temperature is 55?,The pH value of hydration medium PBS is 7.0,the dosage of hydration PBS(pH7.0)is 20 ml,and the hydration time is 20 min.process was as follows: mannitol was used as protective agent,and the amount of protective agent was 5% of freeze dried powder.The freeze-drying time is 48 h.,pH value of hydration medium PBS is 6.8,dosage of hydration PBS is 40 ml,hydration time is 20 min.Using 6% mannitol as the protective agent is the best technology to obtain the liposome drying powder of facudil hydrochloride by freeze-drying.The freeze-drying time was 48 h.The formation of fasudil niosomes was determined by the comprehensive analysis of DSC scan and irspectra.eventually the formation of fasudil hydrochloride niosomes was determined.The optimal preparation process of fasudil hydrochloride niosome tablets is as follows:Using microcrystalline cellulose as filler,the dosage is 18%,and the dosage of flow aid is 0.2%.The test results show that the process is stable and feasible.The results of in vitro release test showed that fasudil hydrochloride niosome had a sustained release effect,and the model was proved to be One order equation.Conclusion: The preparation of fasudil Niosomes with hydrochloric acid solves the defects of the commercially available dosage form with high cost and poor compliance of patients,and meets the requirements.