Study On The Pharmacokinetics And Antitumor In Vitro Of Matrine Microemulsion

Objective:We do the experiment's aim is to study the pharmacokinetic and antitumor activity in vitro of matrine microemulsion,evaluate the hepatic targeting and antitumor activity of matrine microemulsion.Methods: In order to compare the pharmacokinetic parameters of matrine microemulsion and matrine,we administered the rats orally and we used high performance liquid chromatography to determine the plasma concentration of matrine.We used the DAS2.0 software to analyze data.We used HPLC to determine the concentration of matrine in the heart,liver,spleen,lung,kidney and brain tissue.We used SPSS16.0 software to analyze the data obtained to compare the distribution of matrine microemulsion and matrine in vivo.The rats were fed with Matrine microemulsion and matrine to prepare the drug containing seru.We compared the effects of different matrine containing serum on proliferation,cell cycle and apoptosis of hepatoma Hep G2 cells by MTT assay and flow cytometry.Results: The pharmacokinetic process of matrine microemulsion in vivo is a two-compartment model.The Cmax of matrine microemulsion group is 7.487,The AUC0-t of matrine microemulsion group is 50.65,The AUC0-? of matrine microemulsion group is 51.49 and the t1/2Z of matrine microemulsion group is 3.845.The Cmax of matrine group is 3.678,The AUC0-t of matrine group is 23.022,The AUC0-? of matrine group is 23.321 and the t1/2Z of matrine group is 3.655.The number of the matrine microemulsion group were significantly higher than those in the matrine group.The absorption of matrine microemulsion was good and the elimination was slow.After the rats were fed with matrine microemulsion,the matrine was most distributed in the liver.The relative uptake rate of the liver was 1.73.The peak concentration ratio Ce is 1.85.Matrine microemulsion has good liver targeting property.We used MTT method to detect the effect of matrine microemulsion on cell viability.We give the drug 24 h,20% matrine microemuulsion containing medicine serum inhibition rate was 25.631% and 30% matrine microemulsion containing medicine serum inhibition rate was 57.625%,20% matrine containing medicine serum inhibition rate was 12.096% and 30% matrine containing medicine serum inhibition rate was 32.180%.We give the drug 48 h,20% matrine microemuulsion containing medicine serum inhibition rate was 27.811% and 30% matrine microemulsion containing medicine serum inhibition rate was 63.677%,20% matrine containing medicine serum inhibition rate was 18.420% and 30% matrine containing medicine serum inhibition rate was 44.972%.We examined the effect of matrine microemulsion on apoptosis.When the matrine microemulsion group with 20% medicated serum intervened Hep G2 cell,the apoptosis rate were 55.41%.When the matrine microemulsion group with 30% medicated serum intervened Hep G2 cell,the apoptosis rate were 69.92%.When the matrine group with 20% medicated serum intervened Hep G2 cell,the apoptosis rate were 31.97%.When the matrine group with 30% medicated serum intervened Hep G2 cell,the apoptosis rate were 47.53%.Since the microemulsion group with 20% serum contained Hep G2 cells,the proportion of S phase were 11.42%.Since the matrine group with 30% serum contained Hep G2 cells,the proportion of S phase were 13.11%.Conclusion: Matrine microemulsion has a certain liver targeting and antitumor activity in vitro.