| Saxifraga stolonifera(L.) Meerb is a Miao-nationality herbal medicine which has been used to treat otitis media, erysipelas, and hemoptysis for centries. It was indicated that S. stolonifera could be used to cure BPH with less sideeffects in clinical. Lots of studies were done to learn about the efficacy material basement of S. stolonifera against BPH. Chlorogenic acid, Quercetin-3-O-β-L-rhamnopyranoside, Gallic Acid, Bergenin and Quercetin-5-O-β-D-glucopyranoside were the main components among what were responding to the activity against BPH according to the chromatographic fingerprint and profile-effect study on S. stolonifera. Hower, how did these ‘bioactive ingredients’ move in boby and whether these ‘bioactive ingredients’ could reach the target tissue is unclear. For the perpose to clearify its characteristics of motion in rat, systematical study on the absorption, distribution, metabolism, and excretion(ADME) of the bioactive compounds in rat after oral administration of S. stolonifera was conducted.1. Pharmacokinetics of S. stolonifera extracted with water in rat A sensitive and selective UHPLC-MS/MS method was estabilished and validated for simultaneous determination of Gallic acid(GA), Bergnin(BG) and(QR) in rat plasma. The established UHPLC-MS/MS method was applied to the pharmacokinetics of GA, BG and QR in male rats after three dosage of intragastric(2.16, 4.32, and 8.64 g/kg) administration of S. stolonifera, respectively. The results showed that variations of S. stolonifera extract doses altered the contents of GA, BG and QR in rat blood. GA, BG and QR could be rapidly absorbed into the circulation. The AUC0-t of three compounds increased with the dose of S. stolonifera extract which indicated that absobtion of GA, BG, and QR showed a linear dynamics.2. Pharmacokinetics of S. stolonifera extracted with ethyl alcohol,single and blend compounds in ratThe pharmacokinetics of GA, BG, CA, QR and QG in male rats wasconducted after oral administration of S. stolonifera extracted with ethylalcohol, pure GA, pure BG, pure CA and the blend of GA,BG and CA,respectively. The results of GA and BG showed that the Cmax of GA andBG were 3 and 5 times, respectively, as the one which was administratedthe aqeus extract of S. stolonifera; The paremeters of CA afteradministration of S. stolonifera extracted with ethyl alcohol and theblend of GA, BG and CA showed a differernt behavior with thesegained after administrated pure CA in T1/2, Cmax and Tmax. The T1/2 of QRadvanced 2 h and the Cmax was about 3 times compared with the onewhich was administrated the aqeus extract of S. stolonifera. Thepharmacokinetics paremeters of QG were achieved for the first time andit could be quickly absorbed in rat.3. Distribution study of S. stolonifera in ratSimple and effective UHPLC-MS/MS methods were developed to thedetermination of GA, BG, CA, QR and QG in rat liver, heart, spleen,lung, kidney, brain and prostate. The established method was applied tothe distribution of GA, BG, CA, QR and QG in rat heart, liver, spleen,lung, kidney, brain and prostate after oral administration of S.stolonifera(17.28 g/kg). The results indicated that all analytesdistributed in prostate with high concentration after 0.75 and 3 h whichwas consistent with the activity against BPH of S. stolonifera. 4. Excretion study of S. stolonifera extracted with ethyl alcohol in rat Simple and effective UHPLC-MS/MS methods were developed and validated to the determination of t GA, BG, CA, QR and QG in rat feces and urine. The assays were successfully applied to the excretion study of GA, BG, CA, QR and QG in feces and urine. After oral administration of 8.64 and 17.28 g/kg S. stolonifera, the excretion rate of GA, BG, CA, QR and QG in feces were all lower than 2.1% which surposed that most of those analytes might be extensively metabolized in rat. |
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