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The
disposition
and pharmacokinetics of Dioscorea nipponica Makino
extract
in rats
Hong Ren1,
Jian Ping Chen1,2*,
Bin Yan Tan1, Dong Mei Wang1,
Shu Hai Lin1,
Y. P. Zhang2,
D. P. Yang1,
T. Y. Wings Loo3, H. S. Barry Yeung4,
Miaozhen Jin5 and Xiaofang Li5
1Sun
Yat-sen University, Guangzhou,
China.
2School
of Chinese
Medicine, University of Hong Kong, China.
3Department
of Pathology,
Tohoku University
School of Medicine,
Sendai,
Japan.
4Department
of Microbiology, Immunology, and Molecular Genetics,
University of California, Los Angeles, USA.
5Guangdong
College of Pharmacy, China.
*Corresponding author. E-mail:
wtyloo@hotmail.com.
Tel: (852)
2589-0479. Fax: (852)
2872-5476.
Accepted 8 October, 2008 |
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This
study was aimed to
investigate
the disposition and pharmacokinetics of the total saponins of dioscorea (TSD) in rats. Male Sprague-Dawley
rats were
orally
administrated with 3H labeled
TSD
at a single dose ratio of
80 mg
TSD per 1
kg rat.
Blood samples and feces were collected at different time
points to measure the level of TSD activity.
At the final time
point,
determination of the disposition
of TSD
in lung,
kidney, heart, liver, adrenal, and small intestine were performed. From the blood
samples’ emission of radioactivity, pharmacokinetic
parameters
were
derived as T1/2 = 33.33 ± 4.48 h, Tmax = 6.5 ±
0.71 h, AUC = 119400 ± 421097.67, and Cmax =
2643.33 ± 192.26 dpm/ml. There
was
51.609%
of
3H
labeled substance excreted in 24 h. These results suggested
that
blood concentration of
3H-TSD
was
extremely low
and
the majority of TSD was
excreted in the feces. The TSD
was
extensively distributed
to
multi-tissues. The
radioactivity level
was measured to be the
highest in the liver, adrenal gland,
and wall of the gastrointestinal tract.
The radioactivity of TSD was still being detected in blood after 96 h.
This showed TSD
was
excreted in vivo very slowly.
Key
words:
Total saponins of dioscorea,
disposition,
pharmacokinetics,
3H labeled. |
