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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. 2007 Sep; 30(9):1149-54.AP

Abstract

The pharmacokinetics in rats of gentiopicroside (GPS) from orally administered decoctions of Radix Gentianae (DRG) and Gentiana 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 microg/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 microg/mL (p < 0.01) and 7.43 +/- 1.64 microg/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 microgxh/mL for DRG and 59.43 +/- 12.9 microgxh/mL for DGM) compared with oral GPS alone (32.67 +/- 12.9 microgxh/mL). The results demonstrate that the bioavailability of GPS was markedly improved when administered as a decoction than as purified GPS. The decoction from Radix Gentianae provided 2.5 times better bioavailability and that from Gentiana 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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Authors+Show Affiliations

Wang CH
Key Laboratory of Standardization of Chinese Medicines of Ministry of Education, 1200 Cailun Road, Shanghai, China.
Cheng XM
No affiliation info available
He YQ
No affiliation info available
White KN
No affiliation info available
Bligh SW
No affiliation info available
Branford-White CJ
No affiliation info available
Wang ZT
No affiliation info available

MeSH

Administration, OralAnimalsBiological AvailabilityChromatography, High Pressure LiquidFemaleGentianaGlucosidesHumansInjections, IntravenousIridoid GlucosidesIridoidsMalePyransRatsRats, Wistar

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17958334

Citation

Wang, Chang-Hong, 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." Archives of Pharmacal Research, vol. 30, no. 9, 2007, pp. 1149-54.
Wang CH, Cheng XM, 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. 2007;30(9):1149-54.
Wang, C. H., Cheng, X. M., He, Y. Q., White, K. N., Bligh, S. W., Branford-White, C. J., & Wang, Z. T. (2007). 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. Archives of Pharmacal Research, 30(9), 1149-54.
Wang CH, 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. 2007;30(9):1149-54. PubMed PMID: 17958334.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Wang,Chang-Hong, AU - Cheng,Xue-Mei, AU - He,Yu-qi, AU - White,Kenneth N, AU - Bligh,S W Annie, AU - Branford-White,Christopher J, AU - Wang,Zheng-tao, PY - 2007/10/26/pubmed PY - 2007/12/6/medline PY - 2007/10/26/entrez SP - 1149 EP - 54 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 30 IS - 9 N2 - The pharmacokinetics in rats of gentiopicroside (GPS) from orally administered decoctions of Radix Gentianae (DRG) and Gentiana 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 microg/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 microg/mL (p < 0.01) and 7.43 +/- 1.64 microg/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 microgxh/mL for DRG and 59.43 +/- 12.9 microgxh/mL for DGM) compared with oral GPS alone (32.67 +/- 12.9 microgxh/mL). The results demonstrate that the bioavailability of GPS was markedly improved when administered as a decoction than as purified GPS. The decoction from Radix Gentianae provided 2.5 times better bioavailability and that from Gentiana 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. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/17958334/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_ L2 - http://ovidsp.ovid.com/ovidweb.cgi?T=JS&amp;PAGE=linkout&amp;SEARCH=17958334.ui DB - PRIME DP - Unbound Medicine ER -