Enhanced efficacy by percutaneous absorption of piroxicam from the poloxamer gel in rats.
The pharmacokinetics and anti-inflammatory activity of piroxicam from the poloxamer 407 gel were determined to investigate percutaneous absorption of piroxicam from poloxamer gels in rats. The poloxamer 407 gel containing 1% piroxicam showed significant inhibition of carragenin-induced rat foot swelling when compared to the control group. The extent of inhibition of swelling (%) showed a linear relationship with the logarithm of piroxicam dose within approximately 0.4-3.2 mg/kg. The enhancing effect of polyoxyethylene-2-oleyl ether, non-ionic surfactant on the percutaneous absorption of piroxicam from poloxamer 407 gel was evaluated in rats. The piroxicam gel containing polyoxyethylene-2-oleyl ether increaesd the relative bioavailability approximately 1.8-fold compared with the gel without enhancer. Percutaneous administration of piroxicam gel containing polyoxyethylene-2-oleyl ether to rats showed a relatively constant, sustained blood concentration with minimal fluctuation.
Shin
S
S
College of Pharmacy, Chonnam National University, Kwangju, South Korea.
Cho
C
C
Oh
I
I
D000465:Algorithms; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001702:Biopharmaceutics; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005782:Gels; D007509:Irritants; D010894:Piroxicam / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics*; D020442:Poloxamer / Q000009:adverse effects / Q000494:pharmacology*; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*; D013268:Stimulation, Chemical; D013501:Surface-Active Agents / Q000009:adverse effects / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005782:Gels; D007509:Irritants; D013501:Surface-Active Agents; D020442:Poloxamer; D010894:Piroxicam; D002351:Carrageenan