[Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs].
OBJECTIVE
To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs.


METHODS
Applying to double cycle self crossover design, a single oral or intravenous dose of 10 mg x kg(-1) sinomenine was given to 10 beagle dogs. Drug concentrations in plasma were determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program.


RESULTS
The concentration-time curves of oral administration fitted to one compartment model in the beagle dogs. The T(max), C(max), t1/2 and AUC(0-T) was (82.5 +/- 13.9) min, (0.15 +/- 0.027) mg x L(-1), (87.6 +/- 28.3) min and (28.43 +/- 3.48) mg x min x L(-1), respectively. The concentration -time curves of i.v. fitted to two compartment model in the beagle dogs. The t1/2beta and AUC(0-T) was (106.7 +/- 120.2) min and (93.32 +/- 82.08) mg x min x L(-1). The absolute bioavailability for oral use was (30.46 +/- 4.24)%.


CONCLUSIONS
The absolute bioavailability of sinomenine is low, and the elimination of sinomenine tablet is fast.
Chen
Wanyi
W
Department of Clinical Pharmacology, First Affiliated Hospital of Chongqing University of Medical Sciences, Chongqing 400016, China. chenwanyi1005@163.com
Zhou
Yuanda
Y
Kang
Jiping
J
Li
Qiubo
Q
Feng
Xiaoke
X
D000818:Animals; D001682:Biological Availability; D004285:Dogs; D004365:Drugs, Chinese Herbal / Q000493:pharmacokinetics; D005260:Female; D007275:Injections, Intravenous; D008297:Male; D009019:Morphinans / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D004365:Drugs, Chinese Herbal; D009019:Morphinans; C009271:sinomenine