Studies on the pharmacokinetics of lidamycin in mice and dogs using bioassay / 药学学报
Acta Pharmaceutica Sinica
; (12): 700-704, 2004.
Article
in Zh
| WPRIM
| ID: wpr-302733
Responsible library:
WPRO
ABSTRACT
<p><b>AIM</b>A bioassay method was established for the determination of active concentrations of lidamycin and studied its pharmacokinetics in mice and dogs.</p><p><b>METHODS</b>Cytotoxicity of lidamycin in vitro was used to determine drug serum concentrations in vivo.</p><p><b>RESULTS</b>Validity of methodology met the requirements of pharmacokinetic study. The concentration-time profile in mice after iv lidamycin of 100, 50 and 10 microg x kg(-1) was best fitted with 2-compartmental model with T1/2alpha and T1/2beta of 0.77-1.8 min and 5.6-7.2 min, respectively. The AUC were 2851.3, 887.8 and 166.4 microg x min x L(-1), respectively and increased with dose nonlinearly. There were similar trends between AUC and the potency of tumor growth inhibition. After iv lidamycin of 12 microg x kg(-1) in dogs, the concentrations of lidamycin decreased rapidly and the AUC was 16 microg x min x L(-1), which were lower and quicker than those in mice. The levels in serum after second administration at day 15, were lower than those of the first.</p><p><b>CONCLUSION</b>Active concentrations and pharmacokinetics of lidamycin were obtained by bioassay method successfully. There are species differences and single and multi-dosing differences in the pharmacokinetics of lidamycin.</p>
Full text:
1
Index:
WPRIM
Main subject:
Pathology
/
Pharmacology
/
Sarcoma 180
/
Species Specificity
/
Biological Assay
/
Blood
/
Pharmacokinetics
/
KB Cells
/
Area Under Curve
/
Enediynes
Type of study:
Prognostic_studies
Limits:
Animals
/
Female
/
Humans
/
Male
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2004
Type:
Article