A microdialysis study of topically applied diclofenac to healthy humans: Passive versus iontophoretic delivery (original) (raw)
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Drug design, development and therapy, 2015
There is scarce information concerning the pharmacodynamic behavior of topical substances used in the physiotherapy setting. The aim of the present study was to estimate the formation and emptying of the diclofenac (DF) skin reservoir after passive, semiocclusive, and electrically assisted applications of DF. Five different groups of healthy volunteers (ntotal=60, 23 male and 37 female), participated in this study. A 1% DF (Voltaren Emulgel) formulation (12 mg) was applied on the volar forearms on randomized defined circular skin areas of 7 cm(2). DF was applied for 20 minutes under three different conditions at the same time. The presence of DF in the skin results in a reduction of the methyl nicotinate (MN) response. To estimate the bioavailability of DF in the skin, MN responses at different times following initial DF application (1.5, 6, 24, 32, 48, 72, 96, and 120 hours) were analyzed. At 1.5 hours after the initial DF application, a significant decrease in MN response was dete...
Aceclofenac topical dosage forms: In vitro and in vivo characterization
Acta Pharmaceutica, 2010
In recent times, topical drug delivery systems have gained on importance for local and sustained action of many therapeutic agents. Topical application of drugs offers potential advantages of delivering the drug directly to the site of action and acting for an extended period of time (1). However, few studies on topical gel formulations reported the therapeutic effects of drugs in a variety of experimental inflammation and inflammatory pain conditions. Aceclofenac is available in the form of 100-mg tablets for oral use. Importance of aceclofenac as a new generation NSAID has inspired development of topical dosage 467
Journal of Pharmaceutical Sciences, 2001
The systemic pharmacokinetics and local drug distribution of sodium diclofenac in skin and underlying tissues was studied. Iontophoresis facilitated local and systemic delivery of diclofenac sodium compared with passive diffusion. The maximum plasma concentration of sodium diclofenac was achieved within 1 h of iontophoresis, and the delivery was proportional to applied current density (371 ± 141 and 132 ± 62 μg/L at 0.5 and 0.2 mA/cm2, respectively). The in vivo delivery efficiency for diclofenac in rabbit was 0.15 mg/mA·h. The concentrations of sodium diclofenac in the skin, subcutanoeus tissue, and muscle beneath the drug application site (cathode) were significantly greater than plasma concentrations and concentrations of drug in similar tissues at the untreated sites. The results thus suggest that the cutaneous microvasculature is not always a perfect “sink” and that transdermal iontophoresis facilitated the direct penetration of diclofenac sodium to deeper tissues. No skin irritation was observed up to 0.5 mA/cm2 current density and 7 mg/mL sodium diclofenac concentration. © 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 90:1269–1276, 2001
A Study Of The Efficacy Of Diclofenac Iontophoresis For Providing Effective Topical Analgesia
The Internet Journal of Pain, Symptom Control and Palliative Care, 2007
Background & Objectives: Iontophoresis has evolved as one of the attractive methods for enhanced drug delivery The purpose of the study was to determine the efficacy of iontophoresis of diclofenac gel in providing topical analgesia Methods : Healthy volunteers were tested using the Iontophor meter. To the right dorsum of the hand of each volunteer, an electrode containing diclofenac gel was applied. No gel was applied to the left dorsum as a control. A current of 0.4 milliamps was applied for ten minutes to the right dorsum. The dorsal surfaces of both hands were tested with an eighteen gauge needle at 0, 5 and 10 minute intervals. The volunteer's response to the pinprick was recorded using the Visual Analogue Scale (VAS). Results: 48 volunteers were tested. The control group had no significant variation from the overall mean pain score during the time of study. However, the mean pain score of the iontophoresis group decreased with time. Multivariate analysis of repeated measures to determine the effect of iontophoresis on the perception of pain showed statistical significance with respect to decrease in pain scores over time (p<0.001). Conclusions: Iontophoresis with diclofenac gel significantly reduces pain for pinprick and may be used as an alternative technique to provide topical analgesia.
Comparison of skin permeability for three diclofenac topical formulations: an in vitro study
Die Pharmazie, 2014
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. An HPLC method with UV detection was developed and validated with the aim of characterizing the transepidermal penetration in the in vitro system. Using this assay to determine the permeation parameters, results at 24 hours showed that the Flector patch released the highest drug amount (54.6%), whereas a lower drug amount was delivered with the Voltaren Emulgel (38.2%) and the solution (34.4...
Journal of clinical and diagnostic research : JCDR, 2015
Different topical formulations of diclofenac have varying skin penetration profile. Recent advances in science and technology has led to the development of many new formulations of drugs for topical drug delivery. One such technological development has led to the innovation of Dynapar QPS, a novel, non-aqueous, quick penetrating solution (QPS) of diclofenac diethylamine. This study was aimed to measure the total exposure from the drug penetrating the skin in healthy human subjects and comparing the relative systemic bioavailability of Dynapar QPS(®) with diclofenac emulgel. A 200 mg of diclofenac from either Dynapar QPS(®) (5 ml) or emulgel (20 g) was applied on back of subject as per the randomisation schedule. Blood samples were collected up to 16 hours post drug application. Plasma concentration of diclofenac was measured by pre-validated HPLC method. Pharmacokinetic (PK) parameters like Cmax, Tmax, t1/2, AUC0-t, AUC0-∞, and Kel, of diclofenac were determined for both the formula...
European Journal of Clinical Pharmacology, 2004
Objectives: Diclofenac is a non-steroidal antiinflammatory drug used for a variety of painful and inflammatory conditions. A new low-dose, topical-gel form of diclofenac sodium (diclofenac-Na) has been developed for pain relief and redness reduction after sunburn. The objective was to compare exposure to oral diclofenac-Na with the systemic exposure to diclofenac after application of the new topical diclofenac-Na 0.1% Emulgel gel (diclofenac-Na gel) to normal skin and to that with ultraviolet-induced erythema relative. Methods: This study was an open, single-centre, threeperiod, non-randomised trial in 18 healthy Caucasian subjects. During the first period, 12.5 g gel (12.5 mg diclofenac-Na) was applied twice on a single day to normal skin. During the second period, a 25-mg diclofenac-Na, enteric-coated tablet was given orally three times in a single day. During the third period, the diclofenac-Na gel was applied, as in the first period, but during the early phase of an erythema induced by three times the ultraviolet minimal erythema dose, i.e. a firstdegree sunburn associated with pain. During each period, venous blood samples were collected over 24 h and urine was collected over 72 h after first administration for the determination of diclofenac in plasma and urine and of 4¢-OH-diclofenac in urine.
CODEN(USA): PCJHBA Short Review on Topical Diclofenac Gel
2016
The purpose of writing this review on pharmaceutical gel was to compile the recent literature with special focus on rational approach to topical formulation and basic components of topical drug delivery systems. Topical application of drugs offers potential advantages of delivering the drug directly to the site of action and acting for an extended period of time. Skin is one of the extensive and readily accessible organs on human body for topical administration and is main route of topical drug delivery system. Diclofenac when it is applied topically to the skin to ease muscular pains, sprains and strains.When diclofenac is applied to the skin as a gel (or a patch containing gel), instead of it having an effect on all of your body, it only works on the area that you have applied it to. Topical gels are intended for skin application or to certain mucosal surfaces for local action or percutaneous penetration of medicament or for their emollient or protective action.