Research On The Preparation Of Laipin And Its Derivatives

With the deepening of the research on sulforaphene,sulforaphene has been proved to be an effective plant-derived anticancer drug,and it has an effect on cancer cell lines.In recent years,studies have reported that the use of a combination of sulforaphene and glutathione,maintains its anticancer activity and reduces the toxicity.The combination of sulforaphene and glutathione has a variety anticancer effect on different cancer cell lines.However,the vast majority of researches on sulforaphene and its derivatives are aimed at aspects such as separation and purification and efficacy mechanism.There are not many studies on the preparation of sulforaphene and derivatives dosage forms.In terms of drug formulations,the soft capsule itself has a good water absorption and water barrier effect,which can reduce the contact of the drug with moisture and reduce the degradation of the drug.Liposomes,as drug carriers,can have targeted targeting of encapsulated drugs.This project focuses on new preparations of sulforaphene and its derivatives,and changes the drug dosage form to improve drug stability and targeting.1.In the study of the preparation process of sulforaphene soft capsules,a formulation with a ratio of gelatin:water:glycerol=1:1:0.3(mass ratio).The best filling matrix was selected for sulforaphene soft capsules,and the content of sulforaphene in the soft capsule filling was 1%.In the experiment of dehydration of trace amounts of water,the methods of heat dehydration,3 A molecular sieve dehydration,freeze-dry dehydration,No.6 gasoline extraction dehydration and anhydrous sodium sulfate dehydration were compared to select the best method for soybean oil.By the dehydrated sodium sulfate method,the water content can be reduced to 230.11 ± 7.29 ppm.Established the production process of sulforaphene soft capsules.In the long-term stability study,six months after placing in a vial containing soda lime,the vials of soft capsules with a thickness of 8 mm were sealed and stored at-20 ?.The content of the SFE is 94.73±1.07%.At 4 0C condition,the residual content of SFE is 93.21±0.35%.At RT condition,the residual content of SFE is 88.18±1.52%.The residual content of SFE at 25 ? and 1%RH is 86.85±1.49%.In the soft capsule release experiment,a total of 98.91±1.29%was released in 150 min at 37 ? in a 0.1 M HCl environment.37 ?,0.5%SLS environment,150 min released 85.48 ± 1.51%,1.0%SLS 150 min released 60.13 ±1.12%.2.In the study on the preparation method of liposome formulation of sulforaphene-glutathione,a new SFE-GSH liposome preparation process was developed.By controlling the size of the glass spheres and the bead milling time,the size of the liposomes can be controlled.Particles size from 80 to 800 nm.SFE-GSH liposomes with a particle size of 73.60±19.57 nm,PDI=0.288 and ?=-39.3±0.0 mV were obtained by grinding with a 2 mm glass bead for 24 h,and the EE was above 91.03±1.51%.When the egg yolk lecithin:cholesterol:SFE-GSH = 75:25:10(mass ratio),the Tm is 36.85 ?,37 ? 0.01 M PBS solution,24 h cumulative release can be 41.30 ±2.47%.