Formulation and evaluation of ketorolac transdermal systems.
The effects of pressure-sensitive adhesives and vehicles on the in vitro permeation of ketorolac and in vivo pharmacokinetics were studied. Duro-Tak 87-2196 showed the highest in vitro permeation profiles, and propylene glycol monolaurate-diethylene glycol monoethyl ether (DGME) (60:40, v/v) and propylene glycol monocaprylate-DGME (60:40, v/v) revealed the most favorable in vitro and in vivo results. The decreased Cmax and prolonged Tmax and half-life were obtained with the ketorolac transdermal systems compared with oral administration, indicating that the ketorolac transdermal systems may have a prolonged effect with reduced toxic event. There was an excellent relationship found between in vitro permeation flux and in vivo AUC0-infinity.
Choi
Jun Shik
JS
College of Pharmacy, Chosun University, Gwangju, Korea.
Cho
Young Ah
YA
Chun
In Koo
IK
Jung
Sun Young
SY
Gwak
Hye Sun
HS
D000269:Adhesives; D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D004355:Drug Stability; D006207:Half-Life; D020910:Ketorolac / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D019999:Pharmaceutical Solutions; D014677:Pharmaceutical Vehicles; D011312:Pressure; D019946:Propylene Glycol / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley
D000269:Adhesives; D000894:Anti-Inflammatory Agents, Non-Steroidal; D019999:Pharmaceutical Solutions; D014677:Pharmaceutical Vehicles; D019946:Propylene Glycol; D020910:Ketorolac