Preparation And Quality Control Of Jianpifang Granules

Objective: According to the requirements of preclinical pharmaceutical research of new traditional Chinese medicine,modern pharmaceutical technology was used to develop Jianpi Fang(JPF)granules,a new traditional Chinese medicine compound with exact curative effect,controllable quality and convenient carrying.Method: The quality inspection of Citri Reticulatae Pericarpium(Chenpi),Dioscoreae rhizoma(Shanyao),Hordei fructus Germainatus(Maiya)and Oryzae fructus Germainatus(Daoya)has been carried out and all these four herbs have been used to study the extraction and preparation of JPF and the molding process of its granules.Three batches of JPF granules in pilotscale experiments have been prepared to validate the preparation process of JPF granules.The quality standard and stability of JPF granules were investigated for its new drugs application.Result: 1.Refer to the provisions of Chinese Pharmacopoeia,Chenpi,Shanyao,Daoya and Maiya,which we purchased were processed Chinese herbal pieces,and the quality meets the requirements,which can be used for the preparation of JPF granule.The optimized preparation process was as follows: Chenpi was weighed according to the proportion of prescription,adding 8 times the amount of 60% ethanol solution and reflux extracting for 2 times(1.5 hour each time).The filtrate was combined,filtered,ethanol was recovered and dried under reduced pressure to obtain the extract.And the other three traditional Chinese medicines(Shanyao,Daoya and Maiya)was decocting twice(1 hour each time)with 10 times the amount of water.The decoction was combined,filtered and concentrated,and dried under pressure to obtain the extract.The extract powder was mixed with dextrin and 60% ethanol was used as binder for one-step granulation.2.Quality standard study of JPF granule: A method for qualitative identification of hesperidin in JPF granules was established by using TLC.And Methods for the determination of hesperidin and allantoin in JPF granules has also been established.And the contents of hesperidin and allantoin in JPF granule were 13.01-13.51 mg/g and 1.39-1.42 mg/g,respectively.Therefore,the content of hesperidin and allantoin in JPF granules is not less than 10 mg/g and 1.0 mg/g respectively.Fingerprint chromatography study of JPF granule has also been established.The fingerprint of JPF granule contains 14 characteristic peaks in common and seven characteristic common peaks has been identified by comparing with the reference substance,such as allantoin(1),narirutin(7),hesperidin(8),nobiletin(11),3,5,6,7,8,3’,4’-heptamethoxyflavone(12),tangeretin(13),isosinensetin(14).And the fingerprints of Jianpi decoction prepared by different methods were different,which indicating this method could be used to distinguish different samples prepared by various of extraction methods.3.Multi-component content determination method study of JPF granule: a new method for simultaneously determine the content of 7 components(allantoin,hesperidin,narirutin,isosinensetin,nobiletin,3,5,6,7,8,3’,4’-heptamethoxyflavone,tangeretin)in JPF granule would be established.And the method has been used to analyze the content of effective components in the extract of Jianpi formula prepared by different extraction processes,and the results indicated allantoin,hesperidin and narirutin was major components in all JPF decoction samples.But the content of allantoin in JPF decoction by water extraction was highest,which was 1.21 times than that in JPF decoction by 60% ethanol reflux,while the content of hesperidin was higher than that of Jianpi decoction by water extraction,which was3.49 times than that in JPF decoction by water extraction.And the contents of narirutin,isosinensetin,nobiletin,3,5,6,7,8,3’,4’-heptamethoxyflavone and tangeretin in JPF decoction by 60% ethanol reflux were higher than that of JPF decoction by water extraction.Furthermore,the rationality of the extraction process of Chenpi,Shanyao,Daoya and Maiya from Jianpi Recipe by ethanol reflux method and water decoction method was verified.The established method can be used to analyze the chemical constituents of different Jianpi prescriptions.Conclusion: The above results show that the preparation process of Jianpi Granule is simple,the quality is stable,and it has the potential to be developed into a new drug for the treatment of functional activity disorder in the elderly.