The Pharmaceutical Research Of Xiefei Lishui Granules

The prescription of Xiefei Lishui granules is a proved effective recipe and has sma 11 side effects.It has been used for many years in the treatment for MPE by the oncolo gy deparment of Integrative Medicine Hospital of Jiangsu Province.The prescription is m ade up of Semen Descurainiae,Perilla Frutescens seeds,Mori Cortex,Coptis chinensis,Rhiz oma Pinelliae Praeparata,Pericarpium Trichosanthis,Herba Lycopi,Herba Leonuri,Semen PI antaginis,Radix Glycyrrhizae etc. This compound used to be boiled in traditional ways,an d it is inconvenient to be stored and transported.We found that it is unscientific to mix ed decoction after determining the content of the acitve ingredients of the compound.Wi thout purification process,the dose is large. This research aims to optimize the preparation processes by literature and experimental researching. Three batches of pilot scale products prove the preparation process is stable and controllable.Formulate its quality standard an d make six months stablility test.It is proved stable when wrapped with PET/AL/PE in six months.The last chapter shows the pharmacokinetics of the granules.We detect three components in the blood and get their pharmacokinetics parameters.The specific research as follows.Preparation technology:Optimizing the exraction process according to the physical and chemical properties of the acitve ingredients.Water extraction part:Fructus Perillae which crashed to coarse powder,Semen Descurainiae and Semen Plantaginis wrapped wit h bag,then decoting mixed with the Pericarpium Trichosanthis, Herba Lycopi and Rhizo ma Glycyrrhizae Radix Et.According to the content of rosmarinic acid,quercetin-3-O-β-D-glucopyranosyl-7-O-β-D-gentiobioside and extract rate to optimize extract techology by orthogonal experiment.Alcohol extraction part:Using the single-factor test and orthogon al test to optimize extract process.The water extraction part concentrated under reduced pressure,then purified with alcohol deposit.To optimize the best alcohol-precipiation pro cedure by orthogonal experiment.Merge the solution,and concentrating it to relative densi tiy to 1.30～1.35(60℃).Adding dextrin to the solution then dryed under reduced pressure. According to moisture rate,granulating conditions shaping rate,select excipients to optim ize the best forming process.Quality Standard Section:The identification methods of the medicines such as Peril la Frutescens seeds, Coptis chinensis, Herba Lycopi, Herba Leonuri, Semen Plantaginis, Radix Glycyrrhizae in the preparation have been established using TLC.The Determinati on method of rosmarinic acid and Berberine has been established using HPLC;Accordin g to the Chinese Pharmacopoeia (edition 2010) general principles for granules, the pilot scale products have been checked. The water content, Dissolubility, granularity, content uniformity, microorganism are all conforms with the regulations.Stablity Section:After the PET/AL/PE packaging, experiment of accelerated and long-ter m stability for six months have been carried out on three batches of pilot scale product.Corresp onding items,which include the character, identification and content determination of the sam ple,have been tested for 6 months according to the product quality standard draft.As a result, pr eparation showed desirable stability during the inspection.Pharmacokinetics Section:Drawing the blood from eyepits of the rats after oral gra nules.Tetermining the content of constituents dissolved in serum of the rats by HPLC-M S/MS.Then analyzed the data by DAS3.2.7 software,then get the c-t profiles and pharma cokinetic parameters.It can provide a reference for the research of XiefeLishui granules.In conclusion,the preparation technology of Xiefei Lishui granules proved reasonabl e and achievable. The quality is controlled and the granules are stable.