Study On The Preparations Of Single-layer Of Puerarin Osmotic Pump Tablets And Its Pharmacokinetic In Domestic Dogs

This project is the active drug puerarin to effervescent substance?two parts consisting of an acid source and an alkali source?as an osmotic accelerator,after entering the water through a semipermeable membrane coated tablet cores,effervescent substan ce produced water a large amount of C02 gas generated by the pressure of the gas,increasing the pressure on the membrane,and thus sustained,constant puerarin suspension hole in the film is released from the coating.The expansion of the liquid suspension method and the die to form the core technology compared to low viscosity,releasing more thoroughly.Through the optimization of screening reasonable prescription prescription and coating liquid coating technology,combined with in vivo evaluation,optimization of preparation.Compared with the use of the drug itself,plus the acidic effervescent technology alkaline substance release more durable,can theoretically achieve zero order release 12-24 hours model.Objective:To prepare effervescent powered monolayer osmotic pump tablets of puerarin.Methods:To establish HPLC analysis method of puerarin in vitro pump tablets.Using single factor test to identify influence of mono layer osmotic pump tablets release behavior;in the study of coating factors,the dosage on the coating weight,plasticizers and pore forming agents and other excipients were investigated.Determine the best coating prescription.High performance liquid chromatography of Puerarin monolayer effervescent osmotic pump tablet in dogs were performed on the pharmacokinetics of the preliminary study.Results:Puerarin from effervescent to boost the release behavior of puerarin single release osmotic pump tablets with zero-order release model release dissolution experiments accumulated within 12h average of 88%;in vivo in puerarin osmotic pump tablets and effervescent tablets AUC was?3496.26 ± 151.3?and?1144.73 ± 18.8?ng·ml^-1·h,respectively,Tmax was 3h and?2.83±0.3?h,Cmax,respectively?77.59 ± 2.4?and?122.689± 3.0?ng/ml.The relative bioavailability of a single-layer osmotic pump tablets puerarin puerarin ordinary piece of 132.7%.Statistical calculations on the in vivo relevance,puerarin single osmotic pump tablets vivo absorption has a good correlation,r value of 0.9984 for the boost puerarin single osmotic pump tablets with zero-order rate of release of the drug based on effervescent?r>0.99?.Conclusion:The in vivo relevanc e of good experimental design in line with expectations.According to pharmacokinetic studies in dogs oral osmotic pump puerarin results show that,compared with the ordina ry puerarin tablets,osmotic pump tablets prepared to extend the half-life of the experi ment,lower peak concentration,a good correlation between in vivo.Completing this task,can greatly simplify the process of oral controlled-release formulations of drugs with poor solubility,reduce costs and increase patient compliance.Can be developed with independent intellectual property rights,release more stable structure is simpler and more suitable for the industrial production of osmotic pump preparations.