Human transbuccal absorption of diclofenac sodium from a prototype hydrogel delivery device.
The buccal delivery of the nonsteroidal antiinflammatory drug, diclofenac sodium (Voltaren), from a prototype hydrogel was studied in man in a randomized crossover design of buccal delivery and i.v. infusion. After a 30-min delay, plasma levels of diclofenac increased to near steady-state levels of 100 ng/ml by 3 hr. With each subject serving as his own control, the i.v. infusion data facilitated the calculation of a mean steady-state flux of diclofenac sodium of 2.1 +/- 0.6 mg/cm2-hr across human buccal mucosa and a time lag of 1.0 +/- 0.5 hr. The large flux of this ionized species indicates that the traditional lipoidal model of buccal permeation based on the partition coefficient is inadequate.
Cassidy
J
J
Pharmaceuticals Division, CIBA-GEIGY Corp., Ardsley, New York 10502.
Berner
B
B
Chan
K
K
John
V
V
Toon
S
S
Holt
B
B
Rowland
M
M
D000042:Absorption; D000278:Administration, Buccal; D000328:Adult; D004008:Diclofenac / Q000008:administration & dosage / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D006801:Humans; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D008297:Male; D008954:Models, Biological; D009061:Mouth Mucosa / Q000378:metabolism; D011092:Polyethylene Glycols
D004008:Diclofenac; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D011092:Polyethylene Glycols