79 Notes Sweroside (C 16 H 22 O 9 , molecular weight 358.344), an iridoid glycoside, belongs to a large group of natural monoterpenoids with a glucose moiety attached to C-1 in the pyrane ring. It widely exists in plants of many families [1][2][3] and shows a wide variety of biological activities such as hepatoprotective effect, antitumor, antibacterial, antifungal.
4-7)Sweroside is also the main ingredient of purified herbal extracts from the flower buds of Lonicera japonica THUNB. (IGEs-1) which were demonstrated to possess perfect hepatoprotective effect in our preliminary experiments. Since sweroside and its correlative plant extracts have exhibited these pharmacological effects, it would be hopeful that sweroside and IGEs-1 to be developed to some promising preparations of herbal medicinal products (HMPs).Recently, HMPs are getting more common in the main stream in previously skeptical markets such as the United States and United Kingdom. 8) Establishing the pharmacological basis for efficacy of HMPs is a constant challenge. Of particular interest is the question of bioavailability to assess to what degree and how fast compounds are absorbed after administration of HMPs. Of further interest are the elucidation of metabolic pathways, and the assessment of elimination routes and their kinetics. These data become an important issue to link data from pharmacological assays and clinical effects. A better understanding of the pharmacokinetics and bioavailability of HMPs can also help in designing rational dosage regimens. Despite a wide range of research in either sweroside or L. japonica, 9,10) to our best knowledge, there is no information available on the pharmacokinetics of sweroside orally and intravenously administered to investigate its oral bioavailability and hepatobiliary excretion. Moreover, no report has been published to elucidate the metabolites and the metabolic pathways of sweroside.Furthermore, the development of sampling technique has been a focus in vivo experiment.11) Microdialysis system is a sampling technique that can reduce endogenous interference and can be easy to couple with detector for on-line analysis. A series of papers reported the successful application of microdialysis system to pharmacokinetic study.12-15) However, there is no paper to present the application of microdialysis for the preparation of bile samples of sweroside in rat.In the present study, a simple, stable and accurate HPLC-UV method was developed to determine sweroside in rat plasma, urine, feces and bile simultaneously. The method was applied to basic pharmacokinetic and oral bioavailability studies after intravenous administration of sweroside and oral administration of sweroside and IGEs-1. A sampling method through a validated bile microdialysis system coupled with this HPLC-UV determination was developed to evaluate the hepatobiliary excretion of sweroside in rat.
ExperimentalPreparation of IGEs-1 and Sweroside The flower buds of Lonicera japonica THUNB. were collected at the middle of May from Mi county, Hena...