Studies On Quality Standards And Preparations Of Total Flavonoids From Cudrania Tricuspidata

Cudrania species(Moraceae),a rich source of prenylated xanthones and flavonoids,have been investigated phytochemically and biologically.Its roots are applied in clinic for the treatment of digestive apparatus tumor,especially gastric carcinoma,and are also used as Chinese folk medicine "Chuan-po-shi" together with the roots of C.cochinchinensis(Lour) against gonorrhea,rheumatism,jaundice,boils, scabies,bruising,and dysmenorrhea.In early 1980s,Zhemu syrups was made from it's root extract for the treatment of gastrointestinal cancer.But its active ingredients were not clear and quality was instable.Our preliminary research showed that prenylated xanthones such as cudratricusxanthones B,D and macluraxanthone B were anti-tumor active ingredients,and also the extraction and purification process of the total flavonoids of C.tricuspidata(CTP) has been investigated.The pharmacological studies showed that CTP had significant anti-tumor activity,and the effect could be improved remarkably combined with chemotherapy drugs.Therefore, on the basis of the previous results,the present study focuses on the quality standards of CTP and its preparations.1 Researches on the quality standard of CTPIn accordance with Chinese Pharmacopoeia 2005(VolumeⅠ),the quality standard of CTP was researched.CTP was identified by chemical reaction and thin layer chromatography(TLC).General testing methods had been carried out,such as limit test for heavy metals and arsenic,determination of loss on drying and water,etc. The contents of total flavonoids and three prenylated xanthones were determined. Total flavonoids,calculated as cudratricusxanthone B,was determined by colourimetry.Three prenylated xanthones,cudratricusxanthones B,D and macluraxanthone B,were determined by HPLC.According to the experimental results,the quality standard of CTP has been drafted.The results of the stability experiments showed that CTP was stable under the conditions of 60℃,RH 92.5%and 4500 Lx±500 Lx for at least 10 days, respectively.And CTP was stable after being placed at 40℃,RH 75%and at room temperature for 3 months. 2 Researches on CTP tabletsThe formulation of CTP tablets was optimized by single factor and central composite design-response surface methodology.Optimal formulation was proposed to contain CTP 100 g,MCC 40 g,lactose 70 g,PS 60 g,PVPP 30 g,4%PVP 33 mL, and MS 1.5 g.After optimizing,tablets hardness was more than 70 N,disintegration time was less than 1 min,and dissolution of cudratricusxanthones B,D and macluraxanthone B at 45 min were all more than 70%.The quality standard of CTP tablets was established,including identification (chemical reaction and TLC),inspection(weight variation,hardness,disintegration time,and dissolution),and determination of three prenylated xanthones and total flavonoids.The results of the stability experiments showed that CTP tablets were stable under the accelerated conditions and room temperature,etc.3 Researches on CTP solid dispersion capsulesPVP was chosen as solid dispersion carrier by single factor experiment,and the preparation methods of solvent melting and solvent evaporation were compared.The dissolution rate was accelerated significantly after CTP was prepared to solid dispersion,and the dissolution of cudratricusxanthones B,D and macluraxanthone B at 45 min were also increased remarkably.The quality standard of CTP solid dispersion capsules was established,including identification(chemical reaction and TLC),inspection(water determination,filling variation,and dissolution),and determination of three prenylated xanthones and total flavonoids.The results of the stability experiments showed that CTP solid dispersion capsules were stable under the accelerated conditions and room temperature,etc.4 ReviewIn the end,a review on application of the technology of solid dispersions in the preparations of traditional Chinese medicine is presented.