Study On Preparation Technology And Quality Standard Of Jianweixiaoshi Granules

Jianweixiaoshi granules are consists of heterophylla,dried tangerine peel,yam,fried malt,hawthorn,and they can promote gastrointestinal smooth muscle progression and gastric secretion,as well as enhance pepsin activity and so on,and Jianweixiaoshi granules can make spleen and stomach healthy,and benefit vital energy,which can promote digestion to eliminate stagnation.This thesis is a research on a modified formulation of an existing variety from Kehui pharmaceutical factory in Guizhou province,and it will be modified formulation from Jianweixiaoshi tablets to Jianweixiaoshi granules.This thesis studied systematic pharmacy research and complete the preliminary research of pharmacodynamics of Jianweixiaoshi granules,which were according to 2015 edition of the People’s Republic of China Pharmacopoeia and related requirements.The main research contents are as follows:1.Testing bulk drugs: according to 2015 edition of the Pharmacopoeia first part,tested the five bulk drugs in prescription.The results showed that the five bulk drugs chromatography had the same color spots or fluorescent spots with control chromatography in corresponding position,so the results meet requirement;the content of hesperidin(C₂₈H₃₄O₁₅)in dried tangerine peel was 3.38 %（P <0.05）,and the content of citrate（C₆H₈O₇）in the hawthorn was 8.88%,which showed that determination values were higher than those of the Pharmacopoeia,Indicated the content of dried tangerine peel and hawthorn were qualified.Appearance character and inspection results of the five kinds of raw materials had meet the requirements,therefore,the raw materials used for preparing Jianweixiaoshi granules were qualified,which could be used for the preparation.2.Preparation process research: this process included extraction process research and grinding process research.Results showed that the best extraction process was 12 times of water addition and extracted 3 times for 2.5 h each time;the best crushing process was as follows: yam powder over 150 mesh sieve,and crushing time and temperature was set to 6 min and-6 ℃,when water content was less than 8.100 %,powder rate reached 91.85 %.3.Molding process research: according to preparation process of Jianweixiaoshi granules to extracte to determine the type and the amount of accessories,relative density of concentrated extract,the mixing time,the drying time and drying temperature.The molding process was investigated with indexes of grain yield,fluidity,hygroscopicity,moisture,content and so on.From experimental results,it was preferable that sucrose:lactose as 3:1,and added 1.0 % chocolate flavor as flavoring agent,it tasted good;when the relative density of extract was 1.20¹.24（80 ℃）,soft material wet granulation was moderate,had good effect;the time was determined of 15 min to make soft material;the drying temperature was 80 ℃,and drying time was 4 h;granulation and sizing respectively used 14 mesh and 12 mesh sieve;after verification,screened test conditions could be used for the preparation of Jianweixiaoshi granules with good stability.4.Quality standards study: to study thin layer identification of five herbs in sample,and developed layer identification methods of heterophylla and yam.It was used HPLC method to quantified the content of hesperidin in sample.The preparation method was as follows: taking appropriate amount sample to scrutiny,and accurately weighed 1.5 g in a conical flask,added 25 mL of 50 % ethanol,than weighed and ultrasound 60 min,let it cool,with 50 % ethanol to make up the weight loss,filtered,that was;the HPLC chromatographic conditions were as follows: used Eliot C18 column（250 mm × 4.6 mm,5 μm）,and the mobile phase consisted of acetonitrile-water-glacial acetic acid（20:80:2）,and the detection wavelength was 285 nm,and the flow rate was 1 mL/min,and the column temperature was 30 ℃,and the injection volume was 10 μL.The results of the method were shown that the linearity of hesperidin in the range of 5.058 μg/mL²5.292 μg/m L was good（r=0.9998）;relative standard deviation were less than 2.0 % of precision,intermediate precision,repeatability and stability,and recovery was 96.24 %（RSD = 0.95 %）.From above study we can see,qualitative and quantitative methods of this preparationare are simple,accurate and reliable,which can be used for the quality control of Jianweixiaoshi granules.5.Pilot test: according to the optimization of parameters and process,prepared of three batches of Jianweixiaoshi granules,and determined the appearance,melting,yield,moisture and so on.From experimental results,we can see that the three batches of granules were uniform,had consistent color,and solubility were in compliance,and yield had reached more than 90 %,and water content were less than 4.0 %,microbial limit qualified as well as,to proved that product process stability.6.Stability study: by long-term test and accelerated test to observe Jianweixiaoshi granules stability,results were compliance through determination of appearance traits,loading differences,moistures,solubility,microbial limits,identifications,content determination and so on of granules,indicating that granules were stable during long-term test and accelerated test.7.Pharmacodynamics test: which included small intestine exercise test,digestive enzyme test and weight gain,food intake,food utilization test of mouses.After 20 days of continuous gavage of different doses of drugs and distilled water,it showed that groups of different doses could improve the small intestine ink propulsion rate,middle dose group and high dose group were higher than the positive control group;comparing with the positive control group,pepsin activity increased in the low and middle dose groups;high dose group could improve the food utilization of mouses.It mean that Jianweixiaoshi granules had a certain effect to promote digestion.