The Development Of Dispersible Tablet Of Berberine And Paeonol And The Pharmacokinetics Study In Rabbits

Dispersible tablets is a notale new preparation which developed in recent years,It is easy to prepare and easy for the patients to take,and it can decrease the side effects and increase the bioavailability of the drugs. With the help of paenol,berberine hydrochloride can be used to kill helicobacter pylori(HP) and has the effect of anti-inflammatory and analgesia. However, both of the two drugs are poor dissolutable and show slow dissolubility rate and low bioavailability.We developed the dispersible tablets of berberine hydrochloride and paenol in order that it can be absorbed quickly, so the bioavailability of the two drugs will be increased.The basic prescription and preparation technology was initially defined by the study about formulation screening and technology optimizing , based on the pharmacy rule as indicator. Orthogonal project was employed to screen the prescriptions which based on the study of mono-factor experiment.Verification experiments about the dissolution rate of optimized prescription were done and the results showed that the dissolution rate of Berberine hydrochloride was over 90% after 15 minutes,and the dissolution rate of paeonol was over 70% at the same time. The in vitro dissolubility of the dispersible tablet was better than that of common tablets.The quality study of the dispersible tablet of berberine hydrochloride and paenol was done.The main componets included that the identification methods were set up,the HPLC method was established for the content determination of both of the two components.Further more,the dispersible tablet of berberine hydrochloride and paenol examing method of the correlated material was founded.The initial stability study showed that light,high temperature and humidity all had some effects on the dispersible tablet.The results suggest the the dispersible tablet of berberine hydrochloride and paenol shoule be packed in moistureproof material and preserved under cold,diy enviroment.The pharmacokinetics and bioavailability study of the dispersible tablet of berberine hydrochloride and paenol in rabbits was made.The HPLC method which determinates the berberine hydrochloride concentration in the rabbit plasma was established.The method was tested and proved to be suited for studying pharmacokinetics in rabbits.The berberine hydrochloride ordinary tablet was used as the reference preparation,the pharmacokinetics study of the dispersible tablet of berberine hydrochloride and paenol in the rabbit and the bioequivalence evaluation were made by two preparations two cycles crossing trial desigh.The results of the pharmacokinetics trial in six rabbits indicates that the dispersible tablet in vivo single dosage tests fits the two-compartment.AUCo-t of berberine hydrochloride of the two preparations were 542.95 ng ? h/ml and 492.68ng ? h/ml.Cmax were 184.02 ng/ml and 118.03 ng/ml.Tmax were 0.444h and 0.556h.The bioavailability between the two preparations were 125.42%.The evaluation result of bioequivalence showed that AUCo-t and CmaX is bioequivalent but Tmax are beyond the confine. Tmax is brought forward.The results come to the purpose of the paper design.