[Pharmacokinetics of bromotetrandrin (W198) in rats and beagle dogs].
OBJECTIVE
To study the pharmacokinetics of bromotetrandrine (W198) in rats and beagle dogs.


METHODS
The concentrations of W198 in serum were determined using HPLC method with UV detection.


RESULTS
The pharmacokinetic parameters of W198 after single iv doses of W198 10, 20 and 40 mg x kg(-1) in rats were as follows: T1/2beta were 6.60, 7.36 and 6.77 h, AUC0-24 h were 3.797, 7.371 and 15.192 mg x h x L(-1), Vd were 7.14, 4.33 and 4.13 L x kg(-1), CL were 2.83, 2.60 and 2.71 L x (kg x h)(-1), respectively. The T1/2beta and AUCo-24 h of W198 after single im dose of W198 20 mg x kg(-1) in rats were 11.61 h and 12.646 mg x h x L(-1). The im bioavailability of W198 in rats was 56.9%. The T1/2beta, AUC0-24 h, Vd and CL of W198 after single iv dose of W198 5 mg x kg(-1) in beagle dogs were 11.72 h, 12.646 mg x h x L(-1), 0.70 L x kg(-1) and 0.46 L x (kg x h)(-1), respectively. The plasma protein binding ratio of W198 with human serum protein was 78.0%.


CONCLUSIONS
The absorption of W198 in rats was of first order kinetics.
Xiao
Shu-huai
SH
Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China. xsh26@hotmail.com
Wei
Guang-li
GL
Lu
Rong
R
Liu
Chang-xiao
CX
Wang
Feng-peng
FP
D000470:Alkaloids / Q000378:metabolism / Q000493:pharmacokinetics*; D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism / Q000493:pharmacokinetics*; D019540:Area Under Curve; D044182:Benzylisoquinolines / Q000378:metabolism / Q000493:pharmacokinetics*; D001682:Biological Availability; D001798:Blood Proteins / Q000378:metabolism; D004285:Dogs; D004365:Drugs, Chinese Herbal / Q000378:metabolism / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D008297:Male; D011485:Protein Binding; D051381:Rats; D017208:Rats, Wistar; D013045:Species Specificity
D000470:Alkaloids; D000970:Antineoplastic Agents; D044182:Benzylisoquinolines; D001798:Blood Proteins; D004365:Drugs, Chinese Herbal; C009438:tetrandrine