Abstract
The pharmacokinetics in rats of gentiopicroside (GPS) from orally administered decoctions ofRadix Gentianae (DRG) andGentiana macrophlla (DGM) were compared with that of GPS alone administered at 150 mg/kg orally and 30 mg/kg intravenously. The metabolic profile of GPS after intravenous injection could be fitted to two-compartment model whereas oral administration decoctions DRG or DGM, or GPS alone, could all be fitted to a one-compartment model. After oral administration of GPS alone, GPS was absorbed quickly and reached a maximum plasma concentration (Cmax) value, 5.78 ± 2.24 ¼g/mL within 0.75 ± 0.62 h. The plasma level of GPS declined with a T1/2ke, 3.35 ± 0.76 h. After oral administration of decoctions DRG and DGM, GPS was absorbed and reached significantly higher maximum concentrations of 10.53 ± 3.20 ¼g/mL (p<0.01) and 7.43 ± 1.64 ng/mL (p < 0.05) at later time points 1.60 ± 0.76 (p < 0.01 ) and 2.08±0.74 h (p < 0.05), for DRG and DGM respectively, compared with oral GPS alone. Significantly larger AUC values were found for decoctions of GPS (83.49 ± 20.8 ¼g·h/mL for DRG and 59.43 ± 12.9 ¼g·h/mL for DGM) compared with oral GPS alone (32.67 ± 12.9 ¼g·h/mL). The results demonstrate that the bioavailability of GPS was markedly improved when administered as a decoction than as purified GPS. The decoction fromRadix Gentianae provided 2.5 times better bioavailability and that fromGentiana macrophlla 1.8 times higher. The study confirms the importance of careful pharmacokinetic analysis in the characterization of herbal medicines when applied for future clinical applications.
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References
Calliste, C. A., Trouillas, P., Allais, D. P., Simon, A., and Duroux, J. L., Free radical scavenging activities measured by electron spin resonance spectroscopy and B16 antiproliferative behaviors of seven plants.J. Agric. Food. Chem., 49, 3321- 3327 (2001).
el-Sedawy, A. I., Hattori, M., Kobashi, K., and Namba, T., Metabolism of gentiopicroside (gentiopicrin) by human intestinal bacteria.Biol. Pharm. Bull., 37, 2435–2437 (1989).
Huh, H., Kim, H. K., and Lee, H. K., PAF antagonistic activity of 2-hydroxy-3-methoxybenzoic acid glucose from Gentiana scabra.Arch. Pharm. Res., 21, 436–439 (1998).
Jiang, S. H., Kang, L. J., Jiang, Y., Yao, S. K., and Liu, W. N., Studies on pharmacokinetics of gentiopicrin in longdan and its compound preparation in rats.Chin. Pharm. J., 40, 212–215 (2005).
Kondo, Y., Takano, F., and Hojo, H., Suppression of chemically and immunologically induced hepatic injuries by gentiopicroside in mice.Planta Med., 60, 414–416 (1994).
Li, Y. Q., Zhao, D. H., Pan, B. R., Li, B. G., Sun, W. J., Tian, Q., and Jia, M., Effect of gentiopicroside on liver injury of rats.J. Fourth Mil. Med. Univ., 22, 1645–1649 (2001).
Liu, Y. H., Li., X. C., Liu, Y. Q., and Yang, C. R., 1994. Iridoid glycosides from gentiana macrophylla.Acta Botanica Yunnanica, 16, 85–89 (1994).
Liu, Z. W., Chen, C. X., and Jin, R. M., Studies on liver- protecting and bilesecretion-promoting effects of gentiopicroside.Chinese Traditional and Herbal Drugs, 33, 47–50 (2002).
Liu, Z. Q., Zhou, H., Liu, L., Jiang, Z. H., Wong, Y. F., Xie, Y., Cai, X., Xu, H. X., and Chan, K., Influence of co-administrated sinomenine on pharmacokinetic fate of paeoniflorin in unrestrained conscious rats.J. Ethnopharmacol., 99, 61–67 (2005).
Rojas, A., Bah, M., Rojas, J. I., and Gutierrez, D. M., Smooth muscle relaxing activity of gentiopicroside isolated from Gentiana spathacea. Planta Med., 66, 765–767 (2000).
Song, Q. S., Gao, K. B., and Fu, K. Z., Isolation and identification of gentiopicroside from the roots ofGentiana triflora Pall.Zhong Yao Tong Bao, 12, 36–37 (1987).
Song, C. Q., Yang, X. F., and Hu, Z. B., The metabolism of gentiopicroside by human intestinal bacteria.Lishizhen Medicine and Materia Medica Research, 12, 1–2 (2001).
Tan, R. X. and Kong, L. D., Secoiridoids from Gentiana siphonantha.Phytochemistry, 46, 1035–1038 (1997).
Thrivikraman, K. V., Huot, R. L., and Plotsky, P. M., Jugular vein catheterization for repeated blood sampling in the unrestrained conscious rat.Brain Res. Protoc., 10, 84–94 (2002).
Wang, C. H., Wang, Z. T., S W Annie Bligh, White, K.N., and White, C. J., Pharmacokinetics and tissue distribution of gentiopicroside following oral and intravenous administration in mice.Eur. J. of Drug Metab. and Pharmacokinet, 29, 199- 203 (2004).
Yang, X. F. and Song, C. Q., Studies on the metabolism of gentiopicroside by rat intestinal flora.China Journal of Chinese Materia Medica, 25, 673–676 (2000).
Zhang, J. Q. and Zhou, Y. P., Inhibition of aldose reductase from rat lens by some Chinese herbs and their components.China Journal of Chinese Materia Medica, 14, 557–559 (1989).
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Wang, C.h., Cheng, X.m., He, Yq. et al. Pharmacokinetic behavior of gentiopicroside from decoction of radix gentianae, gentiana macrophylla after oral administration in rats: A pharmacokinetic comaprison with gentiopicroside after oral and intravenous administration alone. Arch Pharm Res 30, 1149–1154 (2007). https://doi.org/10.1007/BF02980251
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DOI: https://doi.org/10.1007/BF02980251