Development Of Gynura Procumbens Compound Tablets For Prevention Of Hyperuricemia

Gynura Procumbens compound tablets are composed of Gynura Procumbens,Puerariae Lobatae Radix,Stigma Maydis,and Lophatheri Herba.After being extracted and Spray drying process by scientific technology,it is prepared by adding suitable excipients.Among them,Gynura Procumbens acts as a monarch drug,which can not only reduce the blood uric acid value of mice with hyperuricemia,but also have anti-inflammatory and analgesic effects,thereby providing an anti-gout pharmacological effects.When it is combined with Pueraria lobata,corn silk and light bamboo leaves,the obtained compound can achieve the synergistic effect to prevent hyperuricemia.In this experiment,the extraction solvent was determined by the transfer rate of total flavonoids,which was a functional index component,and the prescription was screened through pharmacological experiments.The extraction process was optimized by single factor combined with BBD.The spray drying process was optimized by Plackeet-Burmann design and Central-Composite design.Then,the forming process was determined.The quality standard of Gynura Procumbens compound tablets was studied and the quality standard of Gynura Procumbens compound tablets was established.The pharmacodynamic validation of Compound Tablets was carried out to provide technical guidance for the development and industrialization of Gynura Compound Tablets.1.Study on Prescription Screening and Extraction TechnologyThe prescription was screened through pharmacological experiments.With the transfer rate of total flavonoids as the index,the extraction solvent was determined.In order to optimize the extraction process,BBD was used to optimize the extraction process.The transfer rate of total flavonoids and the extract powder was taken as evaluation indexes and the concentration of ethanol,extraction time,extraction multiple and extraction times was taken as factors.Finally,the optimum extraction process parameters were obtained.2.Study on spray drying processThe effects of inlet temperature,feed rate,atomization pressure,relative density of liquid and liquid temperature on spray drying were investigated by Plackeet-Burmann design and Central-Composite design.With the help of minitab17.0 software’s response optimizer,the experimental results were optimized,and the best technological parameters of spray drying were obtained.3.Study on Preparation Technology（1）Selection of granulation methods.In the pre-prescription study,the hygroscopicity and repose angle of the extract powder were investigated.It was found that the extract powder had strong hygroscopicity and poor fluidity.The direct pressing method was easy to fragment,so the granulation and pressing method was selected.This experiment by comparing the dry granulation method with the wet granulation methoh was also performed.The results showed that the dry granulation was prone to stick wheel phenomenon and the yield of granules was low,while the wet granulation was easier and the yield of granules was higher,so the wet granulation was chosen in final.（2）Selection of filler.By mixing the extract powder with starch,microcrystalline cellulose（MCC）,lactose,dextrin and maltodextrin,respectively,the granule yield and moisture resistance as measurement index were determined.The results showed that when microcrystalline cellulose（MCC）:lactose reached 1:2,the anti-hygroscopicity effect was the best and the yield of granules was the highest.（3）Selection of wetting agent.In this experiment,the yield of granules and the appearance of granules were taken as indexes to investigate the different wetting agents（water,60%ethanol,70%ethanol,80%ethanol,90%ethanol）.The results showed that 80%ethanol was the best wetting agent.（4）Selection of lubricants.In this experiment,common lubricants of talc powder,SiO₂ and magnesium stearate were selected as objects of study,and the angle of repose of particles,the time limit of disintegration of tablets and the condition of pressing tablets were taken as indexes to screen the kinds and dosage of lubricants.The results showed that 0.5%magnesium stearate had the best effect.4.Study on Quality Standards and Pharmacodynamic Validation of ProductsThis experiment studied the sensory of Gynura Procumbens Compound Tablets,the determination of total flavonoids in Compound Tablets by ultraviolet-visible spectrophotometry,the identification of Gynura Procumbens and Pueraria lobata by TLC.The properties of water,ash,disintegration time limit,heavy metals in Compound Tablets were also examined.Based on the above experimental data,the draft quality standard of Gynura Procumbens Compound Tablets was formulated.And Accelerated and long-term stability tests showed that the quality of the tablet was stable and controllable.Finally,the pharmacodynamic validation of Gynura Procumbens Compound Tablets showed that the medium dose and high doses（1.0g/kg.bw,1.5g/kg.bw）of the tested tablets could significantly reduce serum uric acid in rats with renal dysexcretion hyperuricemia,and the high doses（1.5g/kg.bw）might have some protective effects on renal injury caused by adenine and ethambutol.