Chapter 1: History and present progress of the classification, activities, metabolism are briefly introduced. Furthermore analytical methods on ginsenosides are reviewed.Chapter 2: The aim is to establish a specific method for determination of total ginsenosides in panax Ginseng saponin G for injection. The total ginsenosides was determined by ice acetic acid-perchloric acid based colorimetric method. A soxhlet extraction method is applied to eliminate interferences from cremophor, a solubilization agent, which has the potential to react with the color agent. The linear response of the method ranged from 42.9 to 369ug of ginsenosides (r=0.9999);and the average of recovery was 99.9% with a relative standard deviation (RSD) of 0.09% (n=6). The method is proved to be suitable for the quality control of the total ginsenosides in panax Ginseng saponin G for injection and offers advantages of simple, specificity, and accurate over the previously reported methods.Chapter 3: C-K is a kind of rare saponin which has been shown inhibitive activities of tumor cells, so lots of people has been interested in it for many years. The chapter includes how C-K was founded and developed. Furthermore, the activity of C-K is reviewed.Chapter 4: Preclinical pharmacokinetics study is important in evaluating a novel drug. The chapter involves the basic principle of preclinicalpharmacokinetics and the characteristics of the LC/MS/MS.Chapter 5: A new LC/MS/MS method for determination of C-K in rat plasma was developed and validated and successfully used in the preclinical pharmacokinetics study. A highly sensitive and rapid method using reversed-phase liquid Chromatography combined with tandem mass spectrometry has been developed for the quantitative analysis of C-K in rats plasma. Glycyrrhetinic acid, a structurally related analog of C-K, was used as the internal standard. An small volume of plasma was processed using liquid-liquid extraction. The extract was separated on a Century SIL BDS C)8 column. The mobile phase consisted of acetonitrile/methanol (3:2)-10mM aqueous ammonium acetate (87: 13: 1, v/v), at a flow rate of 0.25 mL-min"1, and the column temperature is 40°C.An API 4000 tandem mass spectrometer equipped with ESI (electrosprary ionization) was used as detector and was operated in the negative ion mode. Multiply reaction monitoring (MRM) using the precursor/product ion combinations of m/z 621.4-*-161.1 (C-K) and m/z 469.3-* 425.2 (internal standard, glycyrrhetinic acid) was used to quantify C-K. The assay was reproducible and linear for C-K in the range of 4.00-4.00 X 103ng ? mL"1 in rat plasma. The lower limit of quantification was 4.00ng ? mL"1. Each sample was separated only 5 min. The precision was within 8% and RE value was within the range of ± 10%.The preclinical pharmacokinetics of C-K was systematically studied by the validated LC/MS/MS method. Following an intravenous administration of C-K to rats in three doses, the plasma concentrations of C-K were determined by the validated LC/MS/MS method. The pharmacokinetics parameters were assessed using DAS 2.0 (Drug and Statistics ver 2.0). Cmax, AUCo-t were all dose proportional in rats. The concentration in plasma-time curves after an i.v. administration to rats was all fitted to three-compartmentmodels.Chapter 6: A new LC/MS/MS method for determination of C-K in dog plasma was developed and validated and successfully used in the preclinical pharmacokinetics study. A highly sensitive and rapid method using reversed-phase liquid Chromatography combined with tandem mass spectrometry has been developed for the quantitative analysis of C-K in dogs plasma. Glycyrrhetinic acid, a structurally related analog of C-K, was used as the internal standard. A small volume of plasma was processed using liquid-liquid extraction. The extract was separated on a Century SIL BDS C|8 column. The mobile phase consisted of acetonitrile/methanol (3:2)-10mM aqueous ammonium acetate (87: 13: 1, v/v), at a flow rate of 0.25 mL-min"1, and the column temperature is 40°C.A API 4000 tandem mass spectrometer equipped with ESI (electrosprary ionization) was used as detector and was operated in the negative ion mode. Multiply reaction monitoring (MRM) using the precursor/product ion combinations of m/z 621.4-* 161.1 (C-K) and m/z 469.3-* 425.2 (internal standard, glycyrrhetinic acid) was used to quantify C-K. The assay was reproducible and linear for C-K in the range of 2.00-2.00 X 103ng 'mL"1 in dog plasma. The lower limit of quantification was 2.00ng ? ml/1. Each sample was separated only 5 min. The precision was within 6% and RE value was within the range of± 10%.The preclinical pharmacokinetics of C-K was systematically studied by the validated LC/MS/MS method. Following an intravenous administration of C-K to dogs in three doses, the plasma concentrations of C-K were determined by the validated LC/MS/MS method. The pharmacokinetics parameters were assessed using DAS 2.0 (Drug and Statistics). Cmax, AUC0-t were all dose proportional in dogs . The concentration in plasma-time curves after an i.v. administration to dogs was all fitted to three-compartment models.