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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2012, Vol. 17 ›› Issue (12): 1378-1383.

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Pharmacokinetic and absolute bioavailability study of Guanfu Base A hydrochloride in Beagle dogs

SUN Jian-guo1, XIAO Ya-nang1, PENG Ying1, ZHANG Xue-yuan1, WU Hui1, YU Guang-wei1, LIU Jing-han2, WU Ming-shu1, 3, A Ji-ye1, WANG Guang-ji1   

  1. 1Key Lab of Drug Metabolism and Pharmacokinetics, 2Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, Jiangsu,China;
    3Acta Pharmacologica Sinica, Shanghai 200031,China
  • Received:2012-10-17 Revised:2012-11-14 Published:2012-12-31

Abstract: AIM: An LC-MS method was developed and validated for the analysis of Guanfu Base A in dog plasma to support the pharmacokinetic study. METHODS: Blood was withdrawn at different times and absolute bioavailability was studied by LC-MS at dosage of 4 mg/kg in 6 beagle dogs. RESULTS: The pharmacokinetic of Guanfu Base A in Beagle dogs fits best to two compartment model with AUC0-48 h, Cmax, tmax and half life t1/2 of (17623.9±7006.4) ng·mL-1·h, (1988±972)ng/mL, (0.8±0.7) h, and (11.2±1.6) h, respectively. Compared with i.v administration, the absolute bioavailability of Guanfu Base A was(99.0±11.2)%, with absorption rate (K01)at (7.563±4.612)/h.CONCLUSION: After oral administration, GFA can be rapidly and completely absorbed by Beagle dogs, which suggested that oral administration of Guanfu Base A could be a substitute way for anti-arrhythmic treatment.

Key words: Guanfu Base A hydrochloride, LC-MS, Pharmacokinetics, Beagle dogs

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