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In order to study the excretion of genistein (GEN) capsule, an estrogen drugs, in human, 30 healthy volunteers were selected and orally administered 50, 100, and 300 mg genistein in an parallel study. Genistein were determined in urine by LC-MS/MS and glucuronidated genistein (GENG) were indirectly determined with enzymatic hydrolysis in urine by LC-MS/MS, and the pharmacokinetic parameters were analyzed by DAS software (ver 2.0). The result showed that the concentrations of genistein in human urine were less than 1% of the GENG, and the cumulative excretion of GEN in 48 h were 0.037, 0.134, and 0.142 mg, separately, and the urinary excretion percentage were only 0.07%, 0.13%, and 0.05%, separately. But the cumulative excretion of GENG in 48 h was 5.3, 13.8, and 15.4 mg, separately, and the urinary excretion percentage were 10.6%, 13.8%, and 5.1%, separately, and the max urinary excretive rate was 0.4, 1.0, and 1.4 mg x h(-1), separately (tmax were 6 h). Studies showed that part of drug excreted through kidney in a form of GENG in human, and the cumulative urinary excretion and the maximum excretion rate of GENG showed a proportional increase conditioned with the dose in the range of 50-100 mg, but showed non-linear increase feature in 300 mg.
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Objective To establish the method of liquid chromatography-mass spectrum for the determination of /Ginsenoside-Rd in human urine. Methods With the gentiopicroside as internal standard, the dilution method was adopted to treat the urine samples. Electrospmy ionization(ESI)source was applied and operated in the positive ion mode. Multiple reaction monitoring(MRM)mode was used to detect Ginsenoside-Rd content. Results By this method the linearity limit of Ginsenoside-Rd is 30.3～ 10 100 ng? mL-1, the lower quantitative limit is (30.3? 2.16) ng? mL-1, and the inter-and intra-day precision (RSD) was less than 10 % . Conclusions This is an accurate, sensitive, specific and convenient method, which can be used for the determination of Ginsenoside-Rdin urine of the healthy human.
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Objective To establish a HPLC/MS/MS method for the determinati on of gentiopicroside in human urine.Methods The urine sample was treated by solid-phase extraction with internal standard of caffeine;The RESCEK C8 colum n(150mm?2.1mm,5 ?m) was used as the analytical column with a mobilep hase consisting of methanol-10mmol? L-1 NH4AC buffer(pH=6.5)-acetonit rile(50∶40∶10,V/V),the flow rate was 0.2 mL? min-1;A triple quadruple tandem mass spectrometer was used as the detector,Electrospray ioniza tion source was applied and operated in positiveion mode.Gentiopicroside and caffeine were detected by monitoring the ion transition of m/z 374.1→ 195.2 and m/z 195.2→ 138.2 respectively.Results The linear range was 30～ 9000 ng?mL-1(r=0.9980) for gentiopicroside in human urine.The recovery was 91.10% ～ 9 6.21 %,The absolute recovery was 100.52% ～ 103.83%,The within-day and between-day precisions were less than 10 %.Conclusion The method is proved to be sensitive,accurate,rapid,specific.
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Object To study the correlativity between the in vivo release of healthy volunteers and the in vitro dissolution of XIANGHE SUPPOSITORY(XS). Methods The electromagnetic stirring method was used to determine the in vitro dissolution of XS, and the in vivo release was got by the indirect method, assaying the content of the left XS after it had released in administering system, HPLC was used for the determination of XS with the index of variant content of berberine hydrochloride. Results A good correlativity was shown between the percentage of in vivo release and in vitro dissolution of XS. Conclusion In vitro dissolution test under the given conditions could indicate the in vivo absorption of XS.
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Objective To select the herba anti- human papillomavirus (HPV) active fraction from herba Arnebia. Methods The fractions from herba Arnebia. were separated with systematic solvents including petroleum arieal part of benzin, n- butanol , ethanol and distilled water, and their effects on HPV- DNA were evaluated by fluorescence quantitative polymerase chain reaction (FQ- PCR) technique. Results Only the water- extract of.this drug showed in- vitro inhibitory effect on HPV- DNA and its minimum effective concentration is 0.08g/mL. Conclusion Herba Arnebia. has in- vitro inhibitory effect on HPV- DNA and the active components exists in the water- extract.