Pharmacokinetic characteristics of fentanyl iontophoretic trandermal system over a range of applied current.
OBJECTIVE
To evaluate the pharmacokinetic (PK) characteristics of a modified fentanyl iontophoretic transdermal system (ITS).


METHODS
This was a prospective, open-label, single-center, randomized, 3-period, 5-treatment, 6-sequence study. Each subject was randomly assigned to receive three treatments in a sequence consisting of intravenous fentanyl citrate, fentanyl ITS at 170 μA, and then one of three other fentanyl ITS treatments at 140, 200 or 230 μA.


METHODS
The following PK parameters were determined: Cmax, tmax, t1/2, AUC23 - 25 and amount of fentanyl absorbed into systemic circulation (i.e., Dose Absorbed).


RESULTS
Fifty-two subjects received at least one fentanyl treatment. Serum exposure (Cmax and AUC23 - 25) and Dose Absorbed increased with increasing current. The median tmax ranged from 23.0 to 23.2 h across the 4 ITS groups. Mean t1/2 values ranged from 11.0 to 13.0 h. The Dose Absorbed from the fentanyl ITS at 170 μA met bioequivalence criteria when compared to data from an earlier version of the fentanyl ITS.


CONCLUSIONS
Exposure of fentanyl and the amount of fentanyl absorbed increased with the magnitude of applied current with the ITS. The fentanyl ITS at 170 μA is bioequivalent to an earlier version of the system.
The Medicines Company , 900 Saginaw Drive, Suite 200, Redwood City, CA 94063 , USA +1 650 241 6811 ; +1 650 241 6895 ; jbradley.phipps@THEMEDCO.com.
J Brad
JB
Phipps
Nitin
N
Joshi
Kelly A
KA
Regal
Jinfang
J
Li
Raymond S
RS
Sinatra
D000279:Administration, Cutaneous; D000328:Adult; D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D005260:Female; D005283:Fentanyl / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D007478:Iontophoresis; D008297:Male; D011446:Prospective Studies; D013810:Therapeutic Equivalency
D000701:Analgesics, Opioid; D005283:Fentanyl
fentanyl; iontophoretic transdermal system; patient-controlled analgesia; pharmacokinetic