Evaluation of Local Anesthesia Provided by Transdermal Patches Containing Different Formulations of Tetracaine

Topical formulations of tetracaine in vehicles of propylene glycol and saline are tested on human volunteers with standard occlusive, adhesive, transdermal patches.The effects of formulation composition, dose, and onset time are investigated.Dose-response studies indicate that the optimum formulatio...

Full description

Saved in:
Bibliographic Details
Published in:Journal of pharmaceutical sciences 1993-11, Vol.82 (11), p.1123-1125
Main Authors: Miller, K.J., Goodwin, S.R., Westermann-Clark, G.B., Shah, D.O.
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Analgesics
Anesthesia, Local
Biological and medical sciences
Dose-Response Relationship, Drug
Double-Blind Method
Humans
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Skin - metabolism
Tetracaine - administration & dosage
Tetracaine - pharmacokinetics
Time Factors
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Topical formulations of tetracaine in vehicles of propylene glycol and saline are tested on human volunteers with standard occlusive, adhesive, transdermal patches.The effects of formulation composition, dose, and onset time are investigated.Dose-response studies indicate that the optimum formulation for the diffusion of tetracaine in vivo is 60% free base and 40% acid salt (w/w) in 40% propylene glycol and 60% saline (v/v). A concentration of 0.3M [8.3% (w/v)] tetracaine is sufficient to reach the dose plateau.Time-response studies indicate that high concentrations of tetracaine in the optimum formulation [1.1 and 1.8 M, 30 and 50% (w/v), respectively] can produce statistically significant analgesia relative to a placebo after 45 min.Comparison of these in vivo data with earlier in vitro data indicate that the optimum formulation with regard to clinical studies is identical to that for in vitro diffusion through hairless mouse skin [60% free base and 40% acid salt (w/w) in 40% propylene glycol and 60% saline].
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600821111