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Voltaren gel absorption

E Folzer, D Gonzalez, R Singh, H Derendorf
Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug (NSAID) widely used in humans and animals. There are limited published studies evaluating diclofenac's skin permeation following topical administration. The aim of our study was to evaluate and compare the in vitro permeation of three different diclofenac-containing formulations (patch, gel, solution) over 24 hours. These formulations were applied (n = 6 per formulation) to pig skin sandwiched between the two chambers in a static Franz diffusion cell and aliquots from the receptor medium were sampled at pre-defined time points...
January 2014: Die Pharmazie
Martin Brunner, David Davies, Wolfgang Martin, Chiara Leuratti, Edith Lackner, Markus Müller
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: • Therapy with topical non-steroidal anti-inflammatory drugs (NSAIDs) relies on the ability of the active drug to penetrate the skin in sufficiently high amounts to exert a clinical effect, which is linked to the specific galenic properties of the formulation. WHAT THIS STUDY ADDS: • This phase 1 study characterizes the transdermal penetration and plasma exposure of different dose levels with galenic differences of a novel topical diclofenac formulation under development and indicates greater diclofenac penetration through the skin when compared with a commercially available formulation...
June 2011: British Journal of Clinical Pharmacology
Amnon C Sintov, Shafir Botner
The objective of this study was to evaluate the transdermal delivery potential of diclofenac-containing microemulsion system in vivo and in vitro. It was found that the transdermal administration of the microemulsion to rats resulted in 8-fold higher drug plasma levels than those obtained after application of Voltaren Emulgel. After s.c. administration (3.5 mg/kg), the plasma levels of diclofenac reached a peak of 0.94 microg/ml at t=1 h and decreased rapidly to 0.19 microg/ml at t=6 h, while transdermal administration of the drug in microemulsion maintained constant levels of 0...
March 27, 2006: International Journal of Pharmaceutics
Martin Brunner, Pejman Dehghanyar, Bernd Seigfried, Wolfgang Martin, Georg Menke, Markus Müller
AIMS: The study was designed to evaluate the relative bioavailability of diclofenac in plasma, subcutaneous adipose and skeletal muscle tissue after repeated topical administration using MIKA Diclofenac Spray Gel (4%), a novel formulation, and after oral dosing using VOLTAREN 50 mg enteric coated tablets. METHODS: Diclofenac (48 mg) was administered topically three times daily for 3 days onto a defined area of the thigh of 12 healthy males. After a 14-day wash out period, subjects were orally treated with 50 mg diclofenac three times daily for 3 days...
November 2005: British Journal of Clinical Pharmacology
Giovana C Rosim, Cláudio Henrique Barbieri, Fernando Mauro Lanças, Nilton Mazzer
A quantitative study of sodium diclofenac (Voltaren Emulgel, Novartis) phonophoresis was undertaken in humans. Fourteen healthy human volunteers were submitted to ultrasound irradiation on two 225-cm2 areas on the dorsum (group A), followed by the application of the medication gel, and the plasma diclofenac mass was measured at 1, 2 and 3 h later by high performance liquid chromatography. The same procedure was repeated one month later with the same volunteers but with the ultrasound equipment switched off for the control group (group B)...
March 2005: Ultrasound in Medicine & Biology
J Zimmerman, J Siguencia, E Tsvang
We present four cases of upper gastrointestinal hemorrhage associated with the cutaneous application of diclofenac (Voltaren Emulgel). The patients' ages ranged from 24 to 85 yr. Three of the patients had used the medication three times daily for at least 2 wk before the onset of bleeding. In two cases, the treatment was indicated for backache which, retrospectively, was attributable to a peptic ulcer. In those two patients, the hemorrhage was massive, requiring blood transfusions. Because systemic absorption of nonsteroidal anti-inflammatory drugs from topical formulations has been documented, caution should be exercised when prescribing these formulations to patients with a history of peptic ulcer...
November 1995: American Journal of Gastroenterology
W Riess, K Schmid, L Botta, K Kobayashi, J Moppert, W Schneider, A Sioufi, A Strusberg, M Tomasi
The percutaneous absorption of diclofenac diethylammonium 1.16% (w/w) in a combination of emulsion cream and gel (Voltaren Emulgel) and of diclofenac sodium 1% (w/w) in a cream formulation (Voltaren cream) was investigated in guinea-pig, rabbit and man. The percutaneous absorption of diclofenac sodium in guinea-pig was 3 to 6% of the dose when the cream formulation in doses of 320, 100 or 40 mg was applied on 10 cm2 of occluded skin and left in place for 6 h. The transdermal delivery of 14C-labelled diclofenac yielded plateau plasma concentrations of radiotracer from 1...
July 1986: Arzneimittel-Forschung
Y Hiramatsu, S Akita, P A Salamin, R Maier
Four commercial gel preparations of topical anti-inflammatory agents have been assessed in six animal models commonly used to determine the biological activity of non-steroidal anti-inflammatory agents for systemic administration. Only UV-induced erythema of the skin, adjuvant induced arthritis and the measurement of vascular permeability proved suitable for differentiation of the potency of the four topical agents. Carrageenin-induced paw oedema, the cotton pellet test and the assessment of the pain threshold according to Randall and Selitto were of little value...
October 1990: Arzneimittel-Forschung
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