Plasma protein binding of celecoxib in mice, rat, rabbit, dog and human.
Biopharm Drug Dispos
; 20(6): 293-9, 1999 Sep.
Article
in En
| MEDLINE
| ID: mdl-10701700
ABSTRACT
The plasma protein binding of celecoxib was determined for animals and humans using in vitro and ex vivo methods. Eight, healthy, human volunteers (three male, five female, 20-39 years) received celecoxib (600 mg) BID for 7 days, blood samples were collected and concentrations of bound and unbound celecoxib determined. The fraction of bound drug in the volunteers was constant (97.4 +/- 0.1%) at total celecoxib plasma concentrations ranging from 0.01 to 4.02 microg/mL. The ex vivo plasma protein binding of celecoxib in the animals was concentration-independent up to approximately 12, 8 and 10 microg/mL for mouse, rat and dog, respectively. The plasma protein binding of celecoxib after a single oral dose of 10 and 300 mg/kg to mice was 98.3 +/- 0.2%, of 1 and 400 mg/kg to rats was 98.3 +/- 0.2% and of 1 and 100 mg/kg to dogs was 98.5 +/- 0.1%. The percent binding of celecoxib to plasma proteins in vitro was slightly lower than those values determined ex vivo. The in vitro binding of celecoxib to plasma protein was constant over the concentrations of 0.1-10 microg/mL for all species, except rat.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Sulfonamides
/
Blood Proteins
/
Anti-Inflammatory Agents, Non-Steroidal
/
Cyclooxygenase Inhibitors
Limits:
Adult
/
Animals
/
Female
/
Humans
/
Male
Language:
En
Journal:
Biopharm Drug Dispos
Year:
1999
Type:
Article
Affiliation country:
United States