Preparation Of Compound Jianshen Granules And Its Preliminary Pharmacodynamics Study

Objective:The total saponins and total polysaccharides of Compound Jianshen were extracted and prepared granules with the effect of decreasing blood sugar,protecting the kidney.preformulation study,extraction process,preparation technology,quality evaluation and pharmacodynamics study were accomplished.Methods:Methodology establishment:The total saponins methodology was established with the indicator of astragaloside in alcohol extraction process;the total polysaccharides methodology was established with the indicator of glucose in water extraction process.Extraction technology:The optimal alcohol extraction process and water extraction process were confirmed by single factor study and orthogonal test.Preparation technology:The optimal preparation technology was ensured with the indicator of soft material condition,difficult and easy level of granulating,granules condition,ratio of briquetting,dissolubility etc by investigating excipients species,excipients dosage,wetting agent concentration and wetting agent dosage.Quality evaluation:Compound Jianshen Granules were evaluated by characters,thin layer chromatography,examination and content determination.Preliminary pharmacodynamics study:Type 2 diabetic nephropathy animal model was molded by feeding with high fat and sugar uniting low dose of STZ.24h food,water,urine volume,UPro content,FBS,Scr,BUN,GHb,TC,TG,SOD,MDA etc were measured to study its level of reducing blood glucose and protecting kidney.its pharmacodynamics effects were expounded by kidney and pancreas pathological section.MCP-1、ICAM-1、IL-6 were tested by ELISA to probe into its mechanism tentatively.Results:The total saponins and total polysaccharides methodology was established,the total saponins was with the indicator of astragaloside,standard curve equation was:Y=0.0184X-0.0659,r=0.9983,it had good linear relationship within the scope of 13.175～39.525μg/mL.The total polysaccharides was with the indicator of glucose,standard curve equation was:Y=0.0564X-0.0034,r=0.9993,it had good linear relationship within the scope of 2.600～15.600μg/mL.These two ways had good precision,repeatability,stability,standard recovery met the demand,methods were feasible.Extraction technology:The optimal alcohol extraction process of the total saponins was 85%alcohol,10-fold,extracted 3 times,2 h every time;The optimal water extraction process of the total polysaccharides was 14-fold,boiled 3 times,0.5 h every time.Three groups of validation test indicated that technological conditions were stable,reasonable and feasible.Preparation technology:extract powder:excipients=1:1,dextrin:lactose=4:1,wetting agent was 85%ethyl alcohol,wetting agent dosage was 15%.Quality evaluation:external properties fitted the demand,Thin layer chromatography of four kinds of crude drugs had vigoroso specificity,the total of granules and powder that couldn’t pass first sieve and could pass five sieve were less than 15%,moisture was less than 6%,content uniformity was less than±5%,which fitted pharmacopoeia rules.Dissolubility fitted the demand.The content determination of astragaloside was no less than 0.0356%,transport rate was 81.23%.Adenosine was no less than 0.005%,transport rate was 60.05%.Preliminary pharmacodynamics study:Compared with the model group,the weight of each drug administration group of Compound Jianshen Granules entirely rised,the difference had statistical significance(P<0.01);the food,water,urine volume,urine protein content of each drug administration group of Compound Jianshen Granules decreased,the difference had statistical significance(P<0.01 or P<0.05);the blood glucose level of each drug administration group of Compound Jianshen Granules decreased,the difference had statistical significance(P<0.01 or P<0.05);the SCr of each drug administration group of Compound Jianshen Granules decreased,the difference had statistical significance(P<0.01);the BUN of each drug administration group of Compound Jianshen Granules decreased,the difference had statistical significance(P<0.01 or P<0.05);the GHb of each drug administration group of Compound Jianshen Granules decreased significantly(P<0.01 or P<0.05);TC、TG、SOD of each drug administration group of Compound Jianshen Granules decreased significantly(P<0.01);SOD of each drug administration group of Compound Jianshen Granules increased significantly(P<0.01);IL-6、MCP-1、ICAM-lof each drug administration group of Compound Jianshen Granules decreased significantly(P<0.01).FBG and each biochemical criterion,pathological section results demonstrated that Compound Jianshen Granules had the certain effects of decreasing blood sugar and lipid,protecting kidney,antioxidation and anti-inflammation.Conclusions:The total saponins and total polysaccharides methodology were established,The optimal process of alcohol extraction and water extraction in extraction technology study,The optimal preparation technology of Compound Jianshen granules was confirmed in preparation technology study,The evaluation indicators of Compound Jianshen Granules were confirmed in quality evaluation,its effects on diabetic nephropathy were verified in preliminary pharmacodynamics study.The paper aim to develop Compound Jianshen Granules that were stable and reliable in quality,took conveniently,tasted good and had perfect effect in this paper,which laid a solid theoretical foundation for further research on drug action mechanism in future.