Puerarin Phospholipid Complex Sustained Release Tablets Of The Study

The purpose of the present study was designed to develop a kind of Puerariacontrolled release tables by using phospholipid and PVP as material which wouldenhance the absorption of Pueraria in gastrointestinal tract and improve itsbioavailability, and which would be more convenient for patients to use. Different kindsof scientific methods in vivo and in vitro were used to evaluate the self-made sustainedrelease tables.The present research focuses on the reaction mechanism of Pueraria-phospholipidsolid dispersion and its physicochemical and biological characteristics. Study theplasma concentration-time curve and pharmacokinetic parameters and then the relativebioavailability was compared with puerarin and solid dispersion. The results show theapparent partition coefficient of the solid dispersion with phospholipid and PVP(drug-phospholipid-PVP, 2:4:1) as carrier was satisfactory. The relative bioavailabilityof solid at dispersion is higher 2.53 times than puerarin.Pueraria solubility in different solvent and stability were determined. HPLCmethod was utilized to determine the Pueraria content in tablets, UV method forassaying release of Pueraria controlled release tablets. HPLC method was developed toanalyze the drug plasma concentration level of Pueraria in rats. The HPLC method wasestablished to determinate the drug plasma concentration level in vivo. Methods weredemonstrated convenient, rapid, and suitable to the study.The effect of different formula composition, preparation procedure and dissolutioncondition on the drug release from the formulation was studied. Based on single-factortests, the optimal formulation was obtained。With single dose crossover design, the pharmacokinetics of Pueraria self-madesustained release tablets in dogs was studied comparing with the commercial tablet. The results indicated that the concentration-time curves of Pueraria tablets fit intwo-compartment model. Compared with commercial tablets' peak time, T_max ofself-made capsules was extended to 3 h, the curve of plasma concentration versus timebecame more flat with a satisfactory controlled release result. Besides, the comparativebioavailability in controlled release tables reference commercial tablets was about 295.2%, with a good correlation coefficient between vivo and vitro experiments.