Study On Preparation Technology,Quality Standard And Hypoglycemic Effect Of Compound Carambola Granules

Objective:To optimize the conditions of the extraction technique for compound carambola,and develop into compound carambola granules(FFYTG);To study the quality of FFYTG and establish the method for its quality control standard;To investigate on hypoglycemic effect of FFYTG on diabetic mice induced by streptozotocin(STZ),and to explore its possibly hypoglycemic mechanism.Methods:In this paper,the preparation technology and quality standard of FFYTG are studied systematically by using modern pharmaceutical technology.1.Research methods of preparation technologyExtraction precipitation process:The comprehensive score of content 2-dodecyl-6methoxy-2,5-diene(-1)(DMDD),puerarin and dried paste was taken as the evaluation index.using the L9(34)orthogonal experimental design to optimize the water extraction technology of compound carambola.Alcohol sinking process:The comprehensive score of miscellaneous,total polysaccharide was taken as the evaluation index,using the L9(34)orthogonal experimental design to optimize the alcohol sinking process of compound carambola.Preparation forming process:Based on the key quality control index of granular moisture absorption rate,molding rate and melt examination,choose the type of diluent,with the ratio of dry paste and wetting agent concentration,screening out the appropriate diluent,finally determine the optimum preparation formation process.2.Research method of quality standardthe article build the TLC identification method of Carambola root,the root of kudzu vine and Astragalus membranaceus.The DMDD and puerarin content is determined by HPLC method,using the HPLC-ELSD method to determine the content of astragaloside.The moisture,solubility and granularity in the preparation was examined.3.research methods of PharmacodynamicTo establish type 2 diabets mouse model by using STZ combined high fat and sugar diets,and then STZ was injected at dose of 100 mg·kg.After 72 h,the mice with FBG?11.1 mmol/L were identified as a diabetic mouse model.FFYTG was given by gavage for three weeks.Fasting blood glucose(FBG)and the change of body weight were determined every week.The levels of insulin(FINS),the contents of IL-6?IL-8?TNF-? in serum were measured by ELISA;The serum triglycerides(TG),total cholesterol(TC),creatinine(Cr)and urea nitrogen(BUN)of mice were determine.Renal Index and superoxide dismutase(SOD)activity,Malondialdehyde(MDA)and reactive oxygen species(ROS)in renal tissue were measured.histologically examined was used to observe pathological changes of kidneys and pancreas tissues.Determination of expression of NF-?B?TGF-?1 protein in kidney by immunohistochemical method.Results:1.Results of preparation process research:The optimal water extraction process is as follows:10 fold amount of water,2 times of decoction and 1.5h each time.The optimal alcohol precipitation process is as follows:Extracted liquid was vacuum concentrated to a relative density of 1.05,alcohol sinking concentration of 65%,standingl2h.The physic liquor was centrifugated and concentrated right amount,and use refrigeration vacuum dryer to dry.The suitable materials were added after the dry paste,The dried extracts:starch:dextrin=1:1:0.2 is the best.2.Results of quality standard researchIn the FFYTG,the roots of carambola,pueraria,and astragali in the selected TLC conditions show the same color spot on the sample and the standard sample in the corresponding position,and the negative control group does not show the spot in the corresponding position.The linear relationship of DMDD within the range of 0.82?8.2 ?g was ideal(R2=0.9990),The retrieve rate was 100.17%,RSD=1.27%.The linear relationship of puerarin within the range of 0.055?0.88?g was ideal(R2=0.9992),The retrieve rate was 100.37%,RSD=1.83%.The linear relationship of astragaloside within the range of 0.4?2.8 ?g was ideal(R2=0.9996),The retrieve rate was99.56%,RSD=0.76%.3.Results of hypoglycemic effect on diabetic miceCompared with the normal control group,the fasting blood glucose increased significantly in each time period of the model group.Compared with the model group,the contents of fasting blood glucose,blood lipids,serum Cr,BUN,IL-6,IL-8 and TNF-? in each drug group decreased,the level of FINS increased,the content of MDA and ROS decreased in renal homogenization,and the activity of SOD increased,Pathological results suggest that the morphology of pancreas and kidney tissue has improved.Immunohistochemical results suggested that the expression of NF-?B and TGF-?1 protein in each drug delivery group was lower than that of the model group.Conclusions:1.The experimental results show that the extraction,removal and forming process of the particulate agent are stable and feasible.2.TLC and content determination method of FFYTG active components were established,the quality standard is feasible and the preparation quality is controllable.3.FFYTG has certain hypoglycemic effect and has protective effect on the kidneys and pancreas.It may be related to the promotion of insulin secretion,the reduction of inflammatory factor content,the improvement of antioxidant capacity in mouse body and the reduction of NF-?B and TGF-?1 protein expression in renal tissue.