PK of buprenorphine transdermal system (BTDS 10) employing the LPS pyrogen model

R. Noveck, R. Vargas, G. F. McMahon, C. D. Breder, D. A. Spyker, A. Eltahtawy, C. Munera, R. Ganesan, D. Wu, B. E. Reidenberg

Research output: Contribution to journalArticlepeer-review

Abstract

Absorption kinetics of transdermal drugs may be affected by fever, resulting in toxic plasma levels causing adverse events. Purpose: Evaluate PK performance of BTDS during endotoxin induced fever and mild illness. Methods: Randomized single-blind, 2 period crossover [Endotoxin (E) CCRE 2 ng/kg IV vs normal saline placebo (P); given at 24 hrs], PK study. Twenty-two healthy male subjects completed 2×72 h BTDS wear periods with a 10-day interdose interval. PK measures included AUCt, AUC∞, Cmax, AUC(24-32) and apparent 3-day flux. Safety evaluation included physical/lab results and AEs. Results: 19/20 subjects (95%) developed fever in response to E 2-8 h after administration. Normal circadian changes in temp were observed with P. Opioid AE rates were similar, but E produced headache, chills and back pain. Cmax was 117 pg/mL for E and 115 pg/mL for P. Mean difference (E-P) in AUC(24-32) was not statistically different (p>0.05). The 3-day flux was 15.6 μg/hr E vs 14.6 p.g/hr for P. Conclusions: The BTDS poses no special safety concerns during acute fever and mild illness.

Original languageEnglish
Pages (from-to)P3
JournalClinical Pharmacology and Therapeutics
Volume69
Issue number2
StatePublished - 2001

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