Bioavailability

Penetration and permeation of Diclofenac Spray Gel vs. Voltaren Emulgel in human skin biopsies, 1997; 96014

Design: open, intraindividual comparative in-vitro study on abdominal human skin without subcutaneous fat over 8 hours.

Methodology: Application of samples in equivalent dosages (10 mg) on skin biopsies. Evaluation of drug deposition of diclofenac in stratum corneum by stripping with sticky tape and skin tissues (cutis and lumen) without fat tissue as well as determination in acceptor medium with student`s t-test in 2 subjects for each preperation.

Results: Deposition in skin and permeation of Diclofenac sodium 4% Spray Gel (DicloFlex®) through the skin is up to 20 - times higher than with Voltaren Emulgel. After 8 hours 78% of Voltaren Emulgel had still not left the stratum corneum.


Favourable dermal penetration of diclofenac after administration to the skin using a novel spray gel formulation, Brunner M. et al, Br J Clin Pharmacol, 1-5, 2005 (9605)

Bioavailability of Diclofenac sodium 4% Spray Gel (DicloFlex®) vs. Voltaren 50 mg tablets in humans assessed by microdialysis

Design: Open fixed sequential study design.

Methodology: 12 healthy male volunteers received on 3 consecutive days each 48 mg of Diclofenac sodium 4% Spray Gel (DicloFlex®) t.i.d onto a defined skin area. After a 14 day wash- out-period volunteers received 50 mg oral Voltaren coated tablets t.i.d. Microdialysis probes were inserted in target tissues and dialysates were collected immediately after the final dose in both treatment regimens and 48 hrs later. Plasma samples were taken simultaneously.

Results: Bioavailability of Diclofenac sodium 4% Spray Gel (DicloFlex®) in target tissues is significantly higher compared with oral.

First time that a topical product achieved higher subcutaneous tissue and muscle concentration vs. oral treatment!