Oral bioavailability and intestinal disposition of dehydroandrographolide in rats / 南方医科大学学报
Journal of Southern Medical University
;
(12): 1074-1081, 2012.
Article
in Chinese
| WPRIM
| ID: wpr-315530
ABSTRACT
<p><b>OBJECTIVE</b>Dehydroandrographolide (DP) from Andrographis paniculata (Burm. F.) Nees is a potential anticancer agent. This study aimed to investigate the oral bioavailability and intestinal disposition of DP to provide useful information for the development of DP as a new candidate anticancer drug.</p><p><b>METHODS</b>The pharmacokinetics of DP was evaluated in rats, and its intestinal disposition was determined using cultured Caco-2 cells and a single-pass rat intestinal perfusion model.</p><p><b>RESULTS</b>The oral bioavailability of DP was 11.92% in rats. The apparent permeability coefficient (P(app)) of DP from the basolateral side (B) to the apical side (A) (5.37×10(-5) cm/s) of the Caco-2 model was roughly equal to that from A to B (4.56×10(-5) cm/s), suggesting no involvement of the efflux transporter(s). In the perfusion model, no significant difference was found in the effective permeability (P*(eff)) of DP between the 4 segments of the intestine. No significant metabolism of DP was detected in the intestinal perfusates. The amount of DP found in the bile was only about 0.1% of the absorbed amount. The P*(eff) and bile amounts of DP were not significantly increased by P-glycoprotein (P-gp) inhibitor or breast cancer resistant protein (BCRP) inhibitor (P>0.05).</p><p><b>CONCLUSION</b>The bioavailability of DP was 11.92% in rats. DP has good absorption and metabolism stability in the intestine. The efflux transporters such as P-gp and BCRP do not participate in DP transport.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Biological Transport
/
Pharmacokinetics
/
Biological Availability
/
Administration, Oral
/
Rats, Sprague-Dawley
/
Caco-2 Cells
/
Diterpenes
/
Intestinal Absorption
/
Intestines
/
Metabolism
Limits:
Animals
/
Humans
/
Male
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2012
Type:
Article
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