Studies on Preparation of Puerarin Phytosomes and Their Solid Dispersions

Abstract

OBJECTIVE To optimize preparation techniques for puerarin phytosomes and explore their solid dispersions to increase the dissolution of puerarin in vitro.METHODS The preparation conditions for puerarin phytosomes were optimized by means of orthogonal design,and the puerarin-phytosome-PVP coprecipitates were prepared by means of solvent evaporation.The accumulative dissolution rate of puerarin in coprecipitates with different ratios of puerarin-phytosomes to PVP was investigated according to dissolution release in vitro.RESULTS The optimized preparation conditions for puerarin phytosomes were obtained as follows.Solvent was ethanol.The ratio of puerarin to phospholipid was 1 to 1.2.Temperature was 30 ℃.Reaction time was 0.5 h.The solubility of puerarin was enhanced by 2.08,1.42 and 1.82 times in three media with different pH and its oil/water apparent partition coefficient was also enhanced by 1.11,1.25 and 1.30 times respectively by phospholipid.The accumulative dissolution rate of puerarin-phytosome-PVP coprecipitate(ratio of mass was 1 to 3) was significantly higher than that of its physical mixture and puerarin phytosome.CONCLUSION Phospholipid can effectively enhance the solubility and oil/water apparent partition coefficient of puerarin,and the coprecipitate of puerarin-phytosome and PVP can improve its dissolution in vitro,but the pharmacokinetics needs further study.