Study On Preparation Technology Of The Shunwei Jiangni Granules

Objective:To prepare Shunwei Jiangni Granule,a new Chinese medicine for reflux esophagitis,the preparation technology of Shunwei Jiangni Granule was studied in this study.The extraction technology route,optimum extraction conditions,concentration and drying parameters were selected to determine a scientific and feasible preparation process,which laid a foundation for the research and development of Shunwei Jiangni Granule and the marketing of new drugs.Method:1.Selection of extraction process route:Based on the literature,the chemical constituents,modern pharmacological studies and physical and chemical properties of each medicinal flavor in the prescription were analyzed.Combining with the clinical application and main characteristics of function,three extraction process routes were drawn up:process route 1:whole-prescription plus water decoction?abbreviated as whole-water extraction?,process route 2:whole-prescription plus water decoction,and volatile oil?abbreviated as total-water extraction plus oil-exertion?,process route 3:dried ginger,patchouli,Magnolia officinalis,capsicum,90%ethanol heated reflux extraction,Pinellia ternata,Coptis chinensis,Scutellaria baicalensis,ginseng,liquorice,five flavors with water decoction?abbreviated as partial alcohol-water extraction?.By using high performance liquid chromatography?HPLC?,the fingerprints of three processes were established.The retention time and area of common peaks were analyzed and compared.The contents of baicalin and berberine hydrochloride were determined.The total alkaloids content and the extract rate were compared.The gastrointestinal peristalsis function of mice was compared by gastric emptying test and small intestinal propulsion test.Combining with the clinical and production practice,the gastrointestinal peristalsis function of mice was compared.The extraction process was determined by comprehensive consideration.2.Optimum extraction conditions:According to the selected extraction process route,the factors affecting extraction such as soaking time,water addition and extraction time were investigated by single factor test.According to the results of single factor investigation,three levels of water addition,extraction time and extraction times were selected,and three factors and three levels of orthogonal test were used to investigate baicalin content and berberine hydrochloride content.Indicators,using the method of total evaluation"normalized value",calculate"normalized value",carry out comprehensive evaluation,and optimize the best extraction conditions.3.Concentration parameters:With the content of astragaloside and berberine hydrochloride as the index,the extract was prepared according to the validation process,and the concentrating effect of vacuum and atmospheric concentrating methods was compared.Result:1.The determination of extraction process route:?1?comparison of extraction rate:the extraction rate of process 1,2 and 3 was 18.6%,18.9%and 15.0%respectively;?2?comparison of the content of effective components:there were some differences,in which the total alkaloid content was 159 mg,153 mg and 169 mg,baicalin content was 763 mg,654 mg and 723 mg,berine hydrochloride content was 68mg,72mg and 87mg respectively;?3?characteristic fingerprint.Comparisons of atlas:There was no significant difference in relative retention time of known common peaks among the three processes,and the peak area corresponding to each g of crude drug was synthesized by common peaks folding.The peak area of magnolol and honokiol was the highest,while the other peak areas had no significant difference;?4?Comparison of pharmacodynamic effects of gastric emptying and small intestinal propulsion in mice:All three processes had the trend of promoting gastrointestinal motility,of which the first and third groups had the trend of promoting gastrointestinal motility compared with the blank control group,the gastric emptying rate and small intestine propulsion rate were significantly higher than those of the blank control group?p<0.05?.There was no significant difference in the gastric emptying rate and small intestine propulsion rate between the 1 and 3 groups?p>0.05?.Pharmacodynamic effects of process 1 and 3 had the function of promoting gastrointestinal motility,and the contents of alkaloids,baicalin and berine hydrochloride had no significant difference.Considering the actual industrial cost,and alcohol extraction process included risk,combined with clinical practice,the traditional water decoction has been used for many years,and the effect is remarkable.Considering comprehensively,process 1,i.e.water extraction of the whole prescription,is chosen as the extraction process route of the preparation.2.The optimum extraction conditions were as follows:?1?the water absorption rate of the prescription medicines was 117%after 8 hours of immersion,the water absorption was no longer increased,and the water absorption curve tended to be flat,indicating that the water absorption of the medicines reached saturation after 8 hours of immersion;?2?the immersion time:the content of baicalin and berine hydrochloride changed at different time:0.5 h,1.5 h,2.5 h,3 h,4 h,5 h,6 h,8 h and 16 h.The content of 5 h was the highest,and the time of immersion was 5 h;the extraction times and extraction time were unchanged,and the amount of water added was 6-10 times to optimize further;the amount of water added and extraction times were unchanged,and the extraction time was 1 h,1.5 h and 2 h to optimize further;orthogonal test analysis:A?water added?,B?extraction time?,C?extraction time?as three factors.The OD mean of the three factors was k3,which was the highest.Comprehensive evaluation showed that the optimum extraction conditions were A₃B₃C₃,i.e.10 times,3 times and 2 hours each time.3.Concentration process investigation:Comparing the two concentrating methods,the results show that,compared with atmospheric pressure concentrating,vacuum concentrating has a higher content of effective ingredients,which proves that the concentrating efficiency is high,and vacuum concentrating is selected.The decompression conditions are 80 C,-0.08MPa⁰.005 MPa.Conclusion:In this study,Shunwei Jiangni Granules was determined to be a complete water extraction process.The soaking time was 5 hours.The optimum extraction conditions of water extraction process parameters including water addition,extraction time and extraction times were 10 times of water,1.5 hours and 3 times.The concentration mode was selected as decompression concentration,and the temperature was controlled at 80?.The process validation showed that the optimized extraction process parameters were reasonable,stable and controllable.