Arzneimittelforschung 2011; 61(8): 435-438
DOI: 10.1055/s-0031-1296224
CNS-active Drugs · Hypnotics · Psychotropics · Sedatives
Editio Cantor Verlag Aulendorf (Germany)

Dose-dependent pharmacokinetics of tyrosol galactoside as an anti-fatigue drug in rats

Deng Yating
1   Department of Pharmacology, Fourth Military Medical University, Xi’an, PR China
,
Wang Qingwei
2   Department of Pharmacy, The Second Affiliated Hospital, Fourth Military Medical University, Xi’an, PR China
,
Liu Xueying
3   Department of Medicinal Chemistry, Fourth Military Medical University, Xi’an, PR China
,
Wang Yu
3   Department of Medicinal Chemistry, Fourth Military Medical University, Xi’an, PR China
,
Ding Zijie
3   Department of Medicinal Chemistry, Fourth Military Medical University, Xi’an, PR China
› Author Affiliations
Further Information

Publication History

Publication Date:
27 November 2011 (online)

Abstract

Tyrosol galactoside (TG) is a new candidate anti-fatigue agent under development. In order to have a good understanding of its pharmacokinetic characters, the paper describes the dose-dependent pharmacokinetics of TG in rats after oral and intravenous administration. TG was rapidly absorbed after oral administration and cleared with first-order rate, for the plasma half-life was independent of dose. Cmax and AUCo–∞ after both intravenous and oral dosing were all linearly correlated with the dose, as the regression correlation coefficient (R) was 0.998, 0.989 and 0.994 for AUCo–∞ (i. v., P < 0.01) AUCo–∞(i. g., P < 0.01) and Cmax (i. g., P < 0.01), respectively. However, these parameters increased less than proportionally with increasing dose. In addition, the apparent volume of distribution (Vd) and the apparent clearance (Cl) seemed to be affected by the dose.

 
  • References

  • 1 Nozaki S, Mizuma H, Tanaka M, Jin G, Tahara T, Mizuno K et al Thiamine tetrahydrofurfuryl disulfide improves energy metabolism and physical performance during physical-fatigue loading in rats. Nutr Res. 2009; 29: 867-72
  • 2 Escalante CP, Manzullo EF. Cancer-related fatigue: the approach and treatment. J Gen Intern Med. 2009; 24: 412-6
  • 3 Rabkin JG, McElhiney MC, Rabkin R, McGrath PJ. Modafi-nil treatment for fatigue in HIV/AIDS: a randomized placebo-controlled study. J Clin Psychiatry. 2010; 71: 707-15
  • 4 Dworzanska E, Mitosek-Szewczyk K, Stelmasiak Z. Fatigue in multiple sclerosis. Neurol Neurochir Pol. 2009; 43: 71-76
  • 5 Abbas G, Jorgensen RA, Lindor KD. Fatigue in primary biliary cirrhosis. Nat Rev Gastroenterol Hepatol. 2010; 7: 313-9
  • 6 Friedman JH. Fatigue in Parkinson’s disease patients. Curr Treat Options Neurol. 2009; 11: 186-90
  • 7 Jean-Pierre P, Morrow GR, Roscoe JA, Heckler C, Mohile S, Janelsins M et al A phase 3 randomized, placebo-controlled, double-blind, clinical trial of the effect of modafinil on cancer-related fatigue among 631 patients receiving chemotherapy: a University of Rochester Cancer Center Community Clinical Oncology Program Research base study. Cancer. 2010; 116: 3513-20
  • 8 Lou JS, Dimitrova DM, Park BS, Johnson SC, Eaton R, Arnold G et al Using modafinil to treat fatigue in Parkinson disease: a double-blind, placebo-controlled pilot study. Clin Neuropharmacol. 2009; 32: 305-10
  • 9 Hu Y, Tian W. Research progress in anti-fatigue effects of traditional Chinese medicine. Med J Natl Defending Forces in Southwest China. 2010; 20: 345-7
  • 10 Chang Y, Yao H, Hsieh S, Lu T, Teng-KuangYeh T. Quantitative determination of salidroside in rat plasma by on-line solid-phase extraction integrated with high-performance liquid chromatography/electrospray ionization tandem mass spectrometry. J Chromatogr B. 2007; 857: 164-9