Study On The Applicable Development Of Natural Drug Of Sophora Alopecuroides L. Total Alkaloids

Objective Adopting natural drug of Sophora alopecuroides L. total alkaloids （SATA） as main drugs and chitosan, sodium alginate, Fe3O4nanoparticle, lactose and microcrystalline cellulose as main accessories. Studying and exploring three new pharmaceutical preparations:SATA sustained-release magnetic beads, SATA pH/magnetic double sensitive beads and SATA capsules. Providing new SATA dosage forms for clinical treatment of digestive tract tumor.Methods Firstly, taking chitosan, sodium alginate, Fe3O4nanoparticle, microcrystalline cellulose and lactose as accessories, via optimizing the preparation technology of the SATA sustained-release magnetic beads using orthogonal test, studying its magnetic properties and in vitro release behavior. Elucidating its release mechanism. Secondly, taking chitosan and sodium alginate as pH sensitive carriers, and Fe₃O₄nanoparticle as magnet sensitive material. Preparing SATA pH/magnetic double sensitive beads using ion gelatinization. Optimizing its preparation technology according to the method of single factor experiment and characterizing its related physical and chemical properties. Meanwhile, studying its swelling capacity and release characteristics in different pH medium. Finally, investigating the effects of different accessories on the hydroscopicity of SATA and the dosage of the glidant based on hydroscopicity and flowing properties. Sieving via pressing pellet fabrication and adding glidant, then putting up in medicinal empty capsules Ⅰ, then obtaining SATA capsules. Constructing the Quality specification and its draft explanation. Studying its quality specification and inspecting its initial stability.Results Firstly, in the orthogonal test of SATA sustained-release magnetic beads in vitro pH6.8phosphoric acid buffer solution medium,0.5h totally releases29.90%, while12h may release up to97.32%, refecting some certain sustained-release effect. Secondly, SATA pH/magnetic double sensitive beads is brown before drying. Its appearance is rounding and regular. Its saturation magnetization is5.02emu/g. manifesting typical superparamagnetism. Its swelling capacity and release behavior show that it is pH sensitive. In the pH1.5hydrochloric acid solution, it scarcely releases, while it does so in pH6.8phosphate buffer solution. In a similar manner.2h drug release of particles in pH1.5sour environment is49.17%, while it is87.43%for pH6.8alkaline environment. Thirdly, the ratio of SATA, lactose and microcrystalline cellulose dosage is3:1:2, passing through60mesh fineness after being homogenized. Adding5%magnesium stearate after drying at50℃and passing through80mesh fineness, we put it up in medicinal empty capsules I. The critical relative humidity is67.6%. All of the inspection of relevant indicators, such as moisture content, disintegration time limited, content uniformity and so on, meet Pharmacopoeia requirements. Stability tests show that high temperature and high humidity surroundings affects the capsule a lot, thus it should be stored in the shade and in the dry place.Conclusion SATA sustained-release magnetic beads has the properties of magnetism and slow release and can be used to realize magnetic targeting on the area of digestive tumor. After oral dosing, it could rapidly reach the therapy consistency. Drug slow release property can be used to sustain therapy consistency and reduce adverse reactions to drug. SATA pH/magnetic double sensitive beads can be utilized to explore intestinal tract drug delivery system. After oral dosing, drug could be released rightly on the area of tumors of intestine with the double location of intestinal tract pH value as well as magnet field, realizing, in the treatment of digestive tumor, the aim of intelligentization on dosing and releasing drug on demand. The preparation technology of SATA capsule is simple, the method is feasible, the property is stable and it can enveil the bitterness of SATA, facilitating dosing. The development of these new three pharmaceutical preparations would enrich SATA and make them possess a variety of research potential and application prospect on curing digestive tumor.