| Scutellaria(Scutellaria baicalensis Georgi)was born in the BC more than 100 years of "Shennong Bencao Jing",is Perennial herbaceous plants,alias mountain tea root and Soil gold tea,with its dry root into medicine,is widely used in clinical medicine,one of the large number of herbs.Scutellaria is mainly produced in Hebei,Heilongjiang,Liaoning and Inner Mongolia and other places,Hebei Chengde in the history of the land for the Scutellaria real estateone,known as the name of “hot river Scutellaria”.This product is bitter,cold,go to the lungs,gallbladder,spleen,stomach,large intestine,small intestine,with heat dampness,xiehuo detoxification,cooling blood to stop bleeding,the effect of tocolysis.The main ingredient of Scutellaria is Baicalin,Baicalein,wogonoside and Wogonin flavonoids,which the highest content of Baicalin,the formula is C21H18O11,with anti-virus,anti-inflammatory,anti-tumor,and immune regulation and other effects,Clinical application is very extensive."Chinese Pharmacopoeia" 2015 regulations record Scutellaria,ontains baicalin content should not be less than 8%,Scutellaria baicalensis extract contains no less than the content of baicalin 85%.So now,more than baicalin as the main active ingredient medicine."Chinese Pharmacopoeia" record Baicalin is obtained by the method of purification of Scutellaria baicalensis,currently on the market to sell Baicalin,are extracted through this method to get.But this method extracts the Baicalin integral insoluble in water,low oral bioavailability,greatly limiting the clinical application.To address the problem above,the research group after a lot of preliminary research,found that Baicalin in the original form of Scutellaria is magnesium salt form,this form of water is very good,can be directly extracted by water-soluble method.Research validation found that Pharmacopoeia method after adding acid destroyed the original form of Baicalin,so that thewater solubility of Baicalin worse,absorption rate is reduced.The research group after the preliminary study,without changing the original form of baicalin in scutellaria to us no acid extraction and purification methods,extraction of Baicalin-Mg from Scutellaria Baicalensis;Moreover,the method of synthesizing Baicalin as raw material and synthesizing Baicalin magnesium salt,the original form of baicalin in Scutellaria baicalensis was restored.Also,Baicalin-Mg can also play a synergistic pharmacological effect of Baicalin and magnesium ion,increase the efficacy.After four spectral tests to verify,It can be determined that the Baicalin-Mg obtained by the addition of acid refining and the glyphosate magnesium salt obtained by the synthetic method have the same structure,and has applied for National invention patents.In this study,the main method of preparation of Baicalin-Mg as the target drug,to study the effects of different drying methods,process stability and environmental stability at different temperatures and at different p H conditions,in vitro inhibition of bacterial action and in your intestinal absorption kinetics,to lay the foundation for the further study of Baicalin-Mg preparation.Objective:Screening the best drying method of Baicalin-Mg and optimizing the preparation process of Baicalin-Mg in order to ensure the stability of preparation process.The stability of Baicalin-Mg at different temperatures and ph conditions was investigated by the experiment,The storage and quality of Baicalin-Mg were controlled.Inhibitory effect of Baicalin-Mg on three drug-resistant bacteria in vitro and to determine whether Baicalin-Mg has better inhibitory effect and effect than Baicalin.The study of rat intestinal absorption kinetics was used to study the absorption characteristics of Baicalin-Mg in the intestinal tract,and to provide basis for the modern research and clinical application of Baicalin-Mg.Methods:(1)Three kinds of dry methods were used to dry the Baicalin-Mg and the contents of three kinds of dried baicalin were determined by HPLC.The bestdrying method of Baicalin-Mg was selected.(2)The stability of Baicalin-Mg at different temperatures and p H conditions was investigated by HPLC.(3)The inhibitory effect of Baicalin and Baicalin-Mg on the resistance of three drug-resistant bacteria was studied by in vitro antibacterial test.(4)The absorption characteristics of Baicalin-Mg in the intestine were determined by rat experiment.Results:(1)Compared with the three drying methods,the content of the drug was determined by HPLC,and the content of freeze-dried Baicalin-Mg was the highest,which was the best drying process,and the preparation process was stable.(2)The stability of Baicalin-Mg was not good at different temperatures and p H.(3)In vitro antibacterial test,compared with Baicalin and Baicalin-Mg inhibition zone diameter,proved that Baicalin-Mg on the inhibition of three kinds of bacteria than Baicalin good,and the strongest inhibition of Staphylococcus aureus.(4)In the study of intestinal absorption kinetics,it was proved that the absorption rate of Baicalin-Mg in the intestine was faster than that of Baicalin,and the intestinal absorption kinetics of Baicalin-Mg was clarified.Conclusions:In this study,three kinds of drying methods were used to dry the Baicalin-Mg and the drug content was determined by HPLC.It was proved that the best drying method of Baicalin-Mg was freeze-drying method,which provided the technical basis for the preparation of Baicalin-Mg.Preparation of Baicalin-Mg process in the process of stability.The stability of Baicalin-Mg was better than that of Baicalin-Mg at different temperatures and different p H conditions.The results showed that the stability of Baicalin-Mg in water was better than that in phosphate solution Sex.In vitro antibacterial experiments showed that Baicalin-Mg on the three kinds of drug-resistant bacteria havedifferent inhibitory effect,and antibacterial effect is more significant than Baicalin.In the study of intestinal absorption kinetics,Baicalin-Mg in the intestinal absorption than Baicalin good.In summary,the clinical application of Baicalin-Mg provides a theoretical basis. |
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