| AIM:This paper established and evaluated primary dysmenorrhea model rat induced by combining estradiol benzoate with oxytocin,and based on the model we focused on researching pharmacokinetic characteristics of four surrogate compounds absorbed into blood after single oral administration of SGT.Revealed the change of the main transitional components in the blood which provided the technique support and experiment basis for the intra-corporal process of efficacious substance foundation of TCM.METHODS:Primary dysmenorrhea model of rats were duplicated by combining estradiol benzoate with oxytocin,and using the traditional biochemical indicator detection and animal behavior researching,on the other hand provided the real-time monitoring of weight.Evaluating the model of primary dysmenorrhea and based on the model we focused on researching pharmacokinetic characteristics of four surrogate compounds absorbed into blood after single oral administration of SGT.We developed and validated a UPLC-MS/MS method into quantitative analysis of themain components in biological analysis.The biosamples were extracted by three-volume ofmethanol,and the separation of components was achieved on a UPLC HSS C18 column with a mobile phase consisting of 0.1%formic acid-acetonitrile and 0.1%formic acid-water at a flow rate of 0.5 mL/minby linear gradient elution.The MS/MS detection was carried out in the model of MRM.Pharmacokinetic parameters were calc?lated by using noncompartment model of WinNonlin6.1 software.RES?LTS:1.Establishment and evaluation of rats of primary dysmenorrhea modelWe selected combining estradiol benzoate with oxytocin in the method being used to copy the model of primary dysmenorrhea.The detection of biochemical index was carried out on the 15th day.The level of ET?E2?PGF2a?PGE2 were increased significantly,and the level of NO??-EP?P were decreased obviously.Female model group were injected into oxytocin appeared twisting at a rate of 100%compared with male model group in 30 minutes.The weight of control group and male model group slowly rising,while the female model group were detected on a declining curve.It was shown that estrogen had an impact on the state of rats.It provided that combining estradiol benzoate with oxytocin to copy the model of primary dysmenorrhea successf?lly.2.Study on the pharmacokinetic characteristics of SGT based on the primary dysmenorrhea model of ratsBased on primary dysmenorrhea model,we selected main components in blood which had good behavioral characteristic,such as liquiritin?isoliquiritigenin?gallic acid and formononetin.The pharmacokinetic res?lts showed a rapid absorption phase with the mean Tmax of 0.3-1h.The largest Cmax of the 4 main components in vivo of SGT in thesequence is formononetin,next is gallic acid and isoliquiritigenin,last is liquiritin.The Cmax and AUC of gallic acid was much higher than others.And the MRT of 5components were all longer than 2.4h.The pharmacokinetic study found that the main invivo components of SGT have rapid distribution,large area under the curve and slowelimination characters in rats.CONSLUSIONS:This paper carried out a method to make a copy of primary dysmenorrhea model.Biochemical index was valuated according to combine estradiol benzoate with oxytocin.The res?lt showed that female model group were injected into oxytocin appeared twisting at a rate of 100%compared with male model group in 30 minutes and the weight was lighter than other two groups.We co?ld make sure that in this method can make a copy of primary dysmenorrhea successf?lly.This paper demonstrated that the four main componentsof SGT in vivo hadrapid distribution,large area under the curve and slow elimination characters in blood.So this research showed intracorporalprocess of transitional ingredients in vivo of TCMform?lar-SGT,which provided thetechnique support and experiment basis for the intracorporal process of efficacious substancefoundation of TCM. |
PDF Full Text Request