Planta Med 2004; 70(12): 1161-1165
DOI: 10.1055/s-2004-835845
Original Paper
Biochemistry and Molecular Biology
© Georg Thieme Verlag KG Stuttgart · New York

Pharmacokinetic and Metabolic Studies of Retrojusticidin B, a Potential Anti-Viral Lignan, in Rats

Chen-Yu Wang1 , Shao-Wen Sun1 , Shoei-Sheng Lee1
  • 1School of Pharmacy, College of Medicine, National Taiwan University, Taipei, Taiwan 100, Republic of China
Weitere Informationen

Publikationsverlauf

Received: February 23, 2004

Accepted: June 26, 2004

Publikationsdatum:
10. Januar 2005 (online)

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Abstract

The pharmacokinetics and metabolism of retrojusticidin B, an anti-HIV reverse transcriptase agent isolated from Phyllanthus myritifolius, were studied in rats. The phase II conjugated metabolites were characterized after solvolysis and enzymatic hydrolysis. The oral bioavailabilities of retrojusticidin B, suspended in Tween 80 and in corn oil, were found to be 22.1 % and 33.1 %, respectively. The elimination half-lives (T1/2) were 22.9 and 36.2 minutes, respectively. The T1/2, clearance, and the volume of distribution (Vz) of retrojusticidin B estimated from i. v. measurements were 24.5 min, 2.6 ± 0.4 L/min, and 90.6 ± 6.4 L, respectively. 9,9′-Secoretrojusticidin B was shown to be phase I metabolite.

Abbreviations

AUC:area under the plasma level-time curve

Vz:apparent volume of distribution of the central compartment

Cl:clearance

Cmax:maximum peak concentration

Tmax:the time to achieve Cmax

References

Dr. Shoei-Sheng Lee

School of Pharmacy

College of Medicine

National Taiwan University

Taipei 100

Taiwan

R.O.C.

Telefon: +886-2-2312-3456 ext. 8405

Fax: +886-2-2321-1127

eMail: shoeilee@ha.mc.ntu.edu.tw