| Objective: To study the optimal preparation technology of Gallstone VI Granules,tablish quality standards,evaluation the preliminary pharmacodynamics and provide the experimental basis for the development of the new drug.Methods: 1.Extraction and purification study:With the total score of total flavonoids,geniposide and medicinal powder as the index,through the single factor test and orthogonal design to explore extraction time,solvent dosage and extraction times on the extraction efficiency were investigated,Preferable the best water extraction process for the Gallstone VI Granules.With the total score of transfer rate as total flavonoids,geniposide and dry cream rate as the index,we used orthogonal design method to investigate the relative density,ethanol volume fraction and standing time of alcohol precipitation,choose a better purification process condition.2.Forming process research:With the moisture absorption rate,forming rate,angle of repose as the investigate index,and the appropriate ratio of excipients and dosage was screened.With soft material and granulation difficult situation,select the appropriate wetting agent.Finally,the corresponding process parameters are determined by orthogonal design method,the study optimizes the best molding process.3.Quality control standards:According to the 2015 version of "Chinese Pharmacopoeia" four general rules 0104 particles required,the traits,grain size,moisture,solubility check.The qualitative identifications of fructus aurantil,lysimachin chirstinae hance,radix aucklandiae,fructus gardeniae,rhizoma corydalis,Polygonum cuspidatum,heum affcinale baille were carried out by TLC,and the content of geniposide was determined by HPLC,the content of total flavonoids was determined by UV method,established the quality standard initially.The initial stability of the Gallstone VI Granules was studied by accelerated test and long-term experiment.4.Preliminary Pharmacodynamics Study: The model of cholesterol gallstone was established on C57BL / 6 mice by using stone feed.The stone composition of gallstones was determined by infrared spectrophotometer.The blood samples were determined by blood lipid index,liver and gallbladder pathological sections.The role of the initial pharmacodynamic study.Results: 1.Gallstone VI Granules particles of the best water extraction process:adding water equivalent to 12 times of volume of material medication,extraction for 3times and extracting for 1 hours each time.The optimum purification process was as follows: the solution was concentrated under reduced pressure to a relative density of1.11 to 1.15,and 95% ethanol was added to the alcohol concentration of 50% for 18 h.2.Molding process: dextrin and mannitol as an excipient(dextrin: mannitol = 1: 2),with 80% ethanol as a wetting agent,soft material,wet granulation,drying,whole grains,that is.3.Quality control standards:Gallstone VI Granules appearance traits,particle size,moisture and so on are in line with regulations.In TLC chromatograms,the features spot was obvious without interference of negative control.Determination of geniposide content by HPLC,UV determination of total flavonoids content,the establishment of the content determination method is simple,easy.In the preliminary stability study,the samples were in compliance with the regulations during the inspection period.4.Preliminary pharmacodynamics study:Gallstone VI Granules cholesterol gallstone model particles can reduce the rate of stone formation,effectively reduce in serum C57BL/6 triglyceride(TG),the content of low density lipoprotein cholesterol(LDL-C).Conclusion: The quality control method is accurate and feasible,the specificity is strong and the preparation is stable,and it has certain therapeutic effect on cholesterol gallstone in C57 BL / 6 mice. |
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