Study On Oral Tablets Of Insoluble Drugs Based On Electrospinning Technology

With the continuous development of high-throughput screening technology,more and more valuable drugs are discovered by scientists.However,due to the poor solubility of many of these drugs,the clinical effect cannot be achieved.It is of great significance to solve the problem of solubility of insoluble drugs in the field of pharmaceutical preparations.Insoluble drugs can be loaded into nanofibers,which have the advantages of large specific surface area,small diameter and high porosity,to greatly improve the water solubility by electrospinning technology.In this study,itraconazole was selected as the model drug,polyvinylpyrrolidone(PVP)as the base material,hydroxypropylmethyl cellulose(HPMC)as the stabilizer,and xylitol as solubilizing small molecules.The drug-loaded nanofibers were then made into solid oral tablets through the tableting process.the morphology of electrospun fibers were observed by environmental electron scanning electron microscope(FSEM)and the diameter distribution was analyzed,the existence of drugs in nanofibers was characterized by XRD,and the dissolution rate of drugs in the gastrointestinal tract was simulated by in vitro dissolution experiments.,It was proved that the drugs could be transformed from crystalline state to amorphous state by electrospinning technology,and existed uniformly and stably in nanofibers,which greatly improved the dissolution of insoluble drugs.Thereby,the rate of drug delivery increased the bioavailability of the drug.The research results are as follows:(1)The establishment of PVP electrospinning process.PVP was used as the base material.The influence of polymer solution concentration,voltage,flow rate and drug loading amount on the morphology of fibers was investigated.The results showed that when the concentration of electrospinning solution was 10wt%,the electrospinning voltage was 13 k V,the flow rate was 0.6 m L/h,and the theoretical drug loading amount was 15%,the drug loaded PVP nanofibers were smooth,uniform in diameter and good in morphology.(2)Preparation and characterization of PVP/HPMC drug-loaded nano-systems.HPMC doped PVP nanofibers were prepared by electrospinning under the optimalspinning conditions of the PVP system.The effects of different HPMC contents on fiber morphology and drug crystallization inhibition were investigated.The results show that when the ratio of HPMC to PVP is 2: 8,the morphology of the fibers and the inhibition of drug crystallization were the best.(3)Determination of HPMC/PVP/xylitol composite drug-loaded nano-system and preparation of oral tablets.The HPMC/PVP/xylitol composite drug-loaded nano-system was prepared,and the drug-loaded nanofibers were made into oral solid tablets by the tableting process.The experiment showed that when the concentration of xylitol was 0.5wt%,HPMC was 2 wt%,PVP was 8wt%,the obtained drug-loaded nanofibrous tablets could not only greatly improve the dissolution rate of the drug,but also inhibit the recrystallization.