| Objective:Preparation of Longxue hydroxypropyl-β-cyclodextrin inclusion complex(HP-β-CD)thermosensitive gel,and in vitro evaluation of the establishment of quality standards,to investigate its experimental rat cervical columnar epithelial ectopic model influences.Methods:(1)The content of hemoglobin A and B in Longxue exhausted HP-β-CD and Longxue HP-β-CD thermosensitive gel was determined by HPLC.(2)The inclusion complex was prepared by aqueous solution agitation method.The inclusion ratio and the yield of inclusion compound were used as the evaluation indexes.Combined with the orthogonal test method,the inclusion time,inclusion temperature and mass ratio of host to guest were the influencing factors.The preparation process of HP-β-CD was identified and evaluated by ultraviolet scanning(UV),differential scanning calorimetry(DSC),thin layer chromatography(TLC),and water-soluble inclusion complex.(3)The HP-β-CD inclusion complex thermosensitive gel was prepared by cold-dissolving method.The gelation temperature and gelation time were determined by the tube inversion method.The gelation temperature and gelation time were used as evaluation indexes to screen the substrate type and dosage.The preparation process of Dragon Blood Exhaust HP-β-CD thermosensitive gel is optimized,and the small test process is verified.(4)The dragon blood in the HP-β-CD temperature-sensitive gel of Dragon’s blood was identified by TLC method.The amount of aureus A and B was determined by HPLC,and the gelation temperature,gelation time,viscosity and pH were determined.Value,density,and in vitro release were investigated.(5)Using Eckstein’s stimulating evaluation standard as an indicator,the vaginal irritancy of rats with HP-β-CD inclusion complex temperature-sensitive gel was studied;Investigating the residence time of HP-β-CD inclusion complex thermosensitive gel in rats by vaginal lavage;Investigating the establishment of animal models of cervical columnar epithelial ectopic rats;Investigating the establishment of animal models of cervical columnar epithelial ectopic rats;The effects of vaginal appearance,vaginal pathology,uterine tissue section and uterine anatomy were used to investigate the effects of HP-β-CD inclusion complex temperature-sensitive gel on cervical columnar epithelial ectopic rats.Results:(1)Loureirin A and B have maximum absorption at 275nm.In the linear relationship,the peak areas of Loureirin A and B have a good linear relationship with the injection volume,and the linear range is 16.5-198.0μg/ml,15.0~180.0μg/ml,the regressionequationisY_a=18.35x-13.171(r=0.99915),Y_b=15.662x-9.1581(r=0.99915),the recovery rate of three test products,hemoglobin A、B.All qualified(Dragon’s blood medicine is 99.2%、99.0%;Dragon’s blood HP-β-CD was 100.9%、100.2%;Dragon’s blood HP-β-CD temperature-sensitive gel was 100.7%、101.9%).(2)The optimal conditions for the preparation of HP-β-CD inclusion complex of Dragon’s blood:the inclusion time of 2h,the inclusion temperature of 40°C,the mass ratio of Dragon’s blood to HP-β-CD is 1:10,UV scanning,differential scanning The results of calorimetry showed that the Dragon Blood and HP-β-CD formed inclusion complex,and the water solubility was significantly higher than that of Longxue medicine.(3)The optimum conditions for the formation of HP-β-CD thermosensitive gel:32%P407,4%P188 and 0.2%HPMC plus appropriate amount of water,stir well,place at 40°C for 24h to swell,stir to dissolve,add 40%The inclusion compound was stirred evenly,and then 0.05%Niebuethyl ethyl ester,5%glycerin was added,and the mixture was homogenized and sterilized at 105°C for 30 minutes to obtain a small test process with good reproducibility.(4)The obtained thermosensitive gel liquid is uniform and fine,and is dark reddish brown;the average contents of dragon blood A and B are 0.241 mg/g and0.253 mg/g,respectively;the TLC method can identify the dragon blood;the gelation temperature is stable at 34±1.0°C.the gelation time is 93~111s;the viscosity after gelation is above 20000mPa;pH4.48~4.57;the density is 1.1195~1.1267mg/g;the release medium is water,and the release in vitro is 4h 81.4%to 89.8%.Conclusion:The results of stimulating evaluation of rat vaginal HP-β-CD thermosensitive gel were similar to those of normal saline;the retention time in the vagina of rats was greater than 4h;after 14 days,the middle dose group(0.2ml/day).The scores of the treatment results of the cervical columnar epithelial ectopic rat model(the lower the score,the better the curative effect)were much lower than the model group and the positive control group. |
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