Research On The Preparation Technology And Quality Standards And Pharmacodynamics Of Baichanting Tablet

Objective:Determine the preparation technology of BCT tablet;establish quality standards;investigate the stability of the tablets;and through animal model to investigate its effectiveness.Methods:1.Through the single factor variable experiment to screen prescription,including tabletting method,filler,adhesive,disintegrating agent,adhesive alcohol concentration and joining way of disintegrating agent.2.Central composite design-response surface methodology is adopted to optimize the amount of materials in the tablet prescription,design with disintegration time limit and the moisture absorption rate as response parameters(Y),the dosage of microcrystalline cellulose(MCC),cross-linked carboxymethyl cellulose sodium(cCMC-Na),silica and magnesium stearate as independent factors(X),set to work with tests of four factors-five levels,a total of 30 prescriptions.3.According to the requirements in 2010 edition of China pharmacopoeia,tablet weight variation,hardness,disintegration time limited,friability,dissolu-tion rate are inspected.3.BCT tablets were identified with thin layer chromatography(TLC);Using of high performance liquid chromatography(HPLC)to content determination.The objects needing to determine are Eleutheroside B,Eleutheroside E,paeoniflorin,chlorogenic acid.4.Exploration influencing factor test,including high temperature,high humidity,strong illumination.And within the prescribed time,investigating disintegration time limit,characteristics and content change,to evaluate the results of accelerated testing.5.Experimental animals C57BL/6 mice were divided into blank group,model group,BCT high,medium and low dosage group,rhynchophylline group,isorhynchophylline group,and induced by intraperitoneal injection 1-methy 1-4-phenyl-1,2,3,6-tetrahydropyridine(MPTP)for five days,then intragastric administration.We carried out the behavior tests on the day 10,day 15,and day 20.Determine content of dopamine(DA)and homovanillic acid(HVA)in striatal on the day 21.Results:1.According to the single factor investigations,BCT tablet will choose MCC as filling agent,cCMC-Na as disintegrating agent,70%alcohol as adhesive,silica as the glidant,and magnesium stearate as lubricant.2.Central composite design-response surface methodology got the best prescription:drug 59%,MCC 30.60%,cCMC-Na 10%,silica 0.3%,magnesium stearate 0.1%.3.Tablet weight variation,hardness,disintegration time limited,friability,dissolution rate are conform to the stipulations of the Chinese pharmacopoeia 2010 version.In the identification test,isofraxidin,paeoniflorin and rhynchophylline in tablets appeared corresponding spot or fluorescence.With C18 chromatographic column,methanol-0.1%phosphoric acid water in gradient elution,and 230 nm for detection wavelength,the flow rate of 1 ml/min,column temperature 30 C,detect the tablet in HPLC.Results show that the tablets of Eleutheroside B,Eleutheroside E,paeoniflorin,chlorogenic acid content is 0.20%,0.57%,0.20%and 0.57%respectively.4.The test of influencing factors indicated that the temperature and light conditions had no affect on the stability of BCT tablet,but humidity has a very bad influence on BCT tablet.90%humidity makes tablet weight increased by more than 5%,70%humidity will induce tablets content decreased or mildew.Studies on accelerated test,in the environment of the 40?,relative humidity 75%,tablets in white plastic bottles quality is stable for six months.5.Animal experimental results show that the climbing pole time,model group takes one more second than the blank group,and having significant meaning(P<0.05),the number of independent activity model group compared with blank group have much more about 20 times/15 min,and also having significant meaning(P<0.05).Each dose group makes the climbing pole time shorter,more autonomous activity,compared with the model group.Content of DA and HVA in corpus striatum,content of model group decrease by 48%(P<0.01)and 20%(P<0.05)compared with the blank control group.Successive medication for 20 days,within each group mice all showed a trend of increase in the content of DA and HVA,BCT medium dosage group and isorhynchophylline group increasing degree is larger.Conclusions:1.Combining with the single factor investigation and central composite design-response surface methodology to screen BCT tablet prescription,scientific and reliable.2.Using isofraxidin,paeoniflorin and rhynchophylline as the reference substance to identification tablets,the method is feasible;using the content of Eleutheroside B,Eleutheroside E,paeoniflorin,chlorogenic acid to evaluation of tablets,the method is easy and accurate.3.The quality of BCT tablets is stable.4.Pharmacodynamics experiment results showed that the BCT medium dosage group and isorhynchophylline group treat PD with better results.