| Purpose:The preparation technology,quality standard and pharmacodynamics of Bi shu ning thermosensitive gel were studied in order to provide basis for the clinical application as well as industrial manufacture.Method: 1.Study on Preparation Process of Bi shu ning thermosensitive gel.The extraction amount of pseudoephedrine hydrochloride and ephedrine hydrochloride in ephedra,were applied as the inspection index,L9(34)orthogonal examination was used to optimize the extraction process of Bi shu ning thermosensitive gel.Optimize it to get the optimized extraction project.Using poloxamer 407(P407)and poloxamer 188(P188)as gel matrix,the gel was prepared by cold-dissolving method.The binomial model of P407 and P188 concentrations were fitted by central composite design-response surface methodology using gel temperature(T)and gel time(t)as index.The contents of P407?P188 were determined by central composite design.In vitro drug release was determined mainly by membranefree dissolution and dialysis bag means.2.The study based on the quality standard of Bi shu ning thermosensitive gelIdentification of Ephedra and Angelica by TLC;TLC was used for identification studies;HPLC was used for content determination studies;and a draft standard for Bi shu ning in situ thermosensitive was established.3.The main pharmacodynamics study of Bi shu ning thermosensitive gelInvestigate the anti-inflammatory effect on rats.The AR rat model was established and the therapeutic effect was determined by the score of symptom.Results:1.The optimal extraction technology of Bi shu ning in situ thermosensitive obtained through the experiment is: using water as the solvent for extraction and extracting twice.The first time,add eight times the amount of water,soak for two hours,reflux for one hour;add six times as much water for a second time,reflux for one hour.The filtrate concentrate is obtained the amount of ethanol and letting stand overnight.2.The results of content determination showed that Ephedrine hydrochloride injection volume has good linearity in the range of 0.116 to 1.450 ?g,r=0.99997.The precision,repeatability and stability of the content determination method were all good.The recovery rate was 100.81%,RSD=0.610%;Pseudoephedrine hydrochloride injection volume has good linearity in the range of 0.106?1.325 ?g,r=0.99998.The precision,repeatability and stability of the method were all good,the recovery was 103.32%,RSD=2.627%.Oxypeucedanin hydrate injection volume had a good linearity in the range of 0.0680?1.3600 ?g,r=0.99998.The precision,repeatability and stability of the content determination method were all good.The recovery rate was 101.27% and the RSD=1.08%.Chlorhexidine acetate injection vo lume had a good linearity in the range of 0.4002?4.0020 ?g,r=0.99990.The precision,repeatability and stability of the content determination method were all good.The recovery rate was 103.28% and the RSD=1.757%.3.The optimal formulation was as P407 for 20.88%,P188 for 5.03% and predicted value were all lower than 5%;Bi shu ning in situ thermosensitive is mainly released by diffusion rather than dissolution,and the release curve conforms to the first-order release equation.4.Among the low,medium and high dose group,Bi shu ning temperature sensitive gel had therapeutic effect on ear swelling caused by foot swelling,granuloma as well as xylene in rats.The effect of treatment in the model group after 6 hours of administration was lower than that of the high-dose group on foot swelling.It can reduce the sneezing and the nasal scratching effectively in AR rats.Bi shu ning temperature sensitive gel high dose group is more effective than the positive drug group.Conclusion: 1.The preferred prosess of Bi shu ning thermosensitive gel is stable and reliable,which is released mainly by diffusion and has the effect of slow release.2.Established the TLC identification and content determination method of Bi shu ning thermosensitive gel,formulated the quality standard of Bi shu ning in situ thermosensitive.3.Bi shu ning thermosensitive gel can relieve the allergic rhinitis and has anti-infammatory effect. |
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