Formulation and in vitro evaluation of transdermal matrix patches of Diclofenac sodium (original) (raw)
Related papers
Drug Development and Industrial Pharmacy, 1999
A transdermal delivery system containing the anti-inflammatory analgesic diclofenac diethyl ammonium in an ethyl hexyl acrylate and vinyl acetate pressure-sensitive adhesive system was developed for percutaneous absorption. These patches were subjected to in vitro permeation and permeation enhancement studies through rat skin using a specially designed diffusion cell. Further, the work deals with percutaneous absorption studies carried out on both animals and human volunteers. The pharmacokinetic parameters calculated from the blood levels of the drug reveal a profile typical of a sustained-release formulation, with the ability to maintain adequate plasma levels for 24 hr (i.e., up to the next application). (Area under the curve [AUC]: 4.356 Ϯ 1.3 mcg/ml.hr in animals and 0.442 Ϯ 0.053 mcg/ml.hr in humans; T max was 8 hr in both the cases, whereas C max was 0.288 Ϯ 0.088 mcg/ml in animals and 0.034 Ϯ .008 mcg/ml in human volunteers.) The amount of the drug bioavailable for targeting the sites of action is lower than via the oral route, but the absorbed dose appears to be adequate for therapeutic use, particularly because of the absence of side effects.
Formulation and Evaluation of Diclofenac Transdermal Gel
2013
INTRODUCTION The Transdermal drug delivery systems are selfcontained, discrete dosage forms which when applied to intact skin deliver the drug through the skin at a controlled rate to the systemic circulation[1].At present, the most common form of delivery of drugs is the oral route. While this has the notable advantages of easy administration, it also has significant drawbacks namely poor bioavailability due to hepatic metabolism (first pass) and the tendency to produce rapid blood level spikes leading to a need for high and /or frequent dosing, which can be both cost prohibitive and involvement[2].To overcome these difficulties there is a need for the development of new drug delivery system; which will improve the therapeutic efficacy and safety of drugs by more precise (i.e. site specific), spatial and temporal placement within the body thereby reducing both size and number of doses. One of the methods most often utilized has been Transdermal delivery. This delivery transport the...
Development and evaluation of transdermal patches of aceclofenac
2014
The aim of this study was to develop and evaluate matrix-type transdermal therapeutic system containing aceclofenac with different ratios of hydrophilic polymers (hydroxylpropyl methylcellulose, sodium carboxy methylcellulose) and a hydrophobic polymer (ethyl cellulose).Thirteen aceclofenac transdermal patch formulations consisting of hydroxyl propyl methyl cellulose, ethyl cellulose and sodium carboxy methyl cellulose polymeric combinations were prepared by solvent casting. These prepared transdermal patches were evaluated for in vitro release, weight variation, moisture content, folding endurance, thickness, drug content and swelling studies. The diffusion studies were performed by using modified Franz diffusion cell. The formulation, F10 showed the maximum release of 98.18 % in 4 h, where as F2 showed the maximum release of 93.22 % in 8 h. Formulation, F9 showed the minimum release of 41.4 % in 8 h. Hence F2 (ethylcellulose: hydroxylpropyl methylcellulose ratio 3:2), exhibited go...
Asian Journal of Pharmaceutical and Clinical Research, 2018
Objective: The aim of this study was to investigate diclofenac sodium patches using chitosan (Ch) and polyvinyl (PVA) alcohol cross-linked tripolyphosphate sodium (TPP) to increased transdermal permeation of the drug from the matrix system across rabbit skin.Materials and Methods: The chemical characterization of diclofenac sodium was done by ultraviolet-visible spectrophotometry. Formulation of diclofenac sodium patches using solvent evaporation method with cross-link technique. Evaluation of physical character of the film includes organoleptic observation, weight test, thickness, % moisture absorption, fold resistance, interaction between materials used Fourier transform infrared (FTIR), and active substance levels. The drug release was determined using Franz diffusion cells in phosphate buffer (pH 7.4).Results: The result of physiochemical parameters of the transdermal patch were found satisfactory. Formula F1, F2, F3, and F4 produce patches with fine texture, F5 and F6 formulas ...
Formulation and evaluation of transdermal patch of aceclofenac
International Journal of Drug Delivery, 2009
The objective of present study is to determine the permeation of Pregabalin from transdermal patch into microcirculation of skin. Matrix type transdermal drug delivery system (TDDS) of Pregabalin was prepared by the solvent evaporation technique. Several batches were prepared by using combination of HPMC and PVP; PVA and PVP; Eudragit RL-100 and Eudragit RS-100; HPMC and EC in different ratios. Propylene glycol was used as plasticizer and DMSO was incorporated as a permeation enhancer. Formulated transdermal patches were charachterised for their physicochemical parameters like thickness, weight variation, flatness, tensile strength, folding endurance, moisture content, moisture uptake and drug content uniformity. Patches were evaluated for their in-vitro drug release profile and ex-vivo skin permeation studies. Patches were also subjected to stability studies and skin irritation studies to determine their compatibility with skin. Formulation P 1 containing HPMC and PVP in the ratio of 3:1 and propylene glycol, 5%w/v and DMSO, 6%w/v was found to be the most optimum formulation. P 1 was also found to exhibit maximum in -vitro %drug release of about 81.70%. Result of evaluation studies revealed that Pregabalin can be administered as a controlled drug delivery system to reduce frequency of drug administration. But this hypothesis requires further confirmation via in-vivo pharmacodynamic and pharmacokinetic studies in animal and human models.
Journal of Pharmaceutical Sciences, 2002
In this study, matrix-type transdermal patches containing diclofenac diethylamine were prepared using different ratios of polyvinylpyrrolidone (PVP) and ethylcellulose (EC) by solvent evaporation technique. The drug matrix film of PVP and EC was casted on a polyvinylalcohol backing membrane. All the prepared formulations were subjected to physical studies (moisture content, moisture uptake, and flatness), in vitro release studies and in vitro skin permeation studies. In vitro permeation studies were performed across cadaver skin using a modified diffusion cell. Variations in drug release profiles among the formulations studied were observed. Based on a physicochemical and in vitro skin permeation study, formulation PA4 (PVP/EC, 1:2) and PA5 (PVP/EC, 1:5) were chosen for further in vivo experiments. The antiinflammatory effect and a sustaining action of diclofenac diethylamine from the two transdermal patches selected were studied by inducing paw edema in rats with 1% w/v carrageenan solution. When the patches were applied half an hour before the subplantar injection of carrageenan in the hind paw of male Wistar rats, it was observed that formulation PA4 produced 100% inhibition of paw edema in rats 12 h after carrageenan insult, whereas in the case of formulation PA5, 4% mean paw edema was obtained half an hour after the carrageenan injection and the value became 19.23% 12 h after the carrageenan insult. The efficacy of transdermal patches was also compared with the marketed Voveran 1 gel and it was found that PA4 transdermal patches produced a better result as compared with the Voveran 1 gel. Hence, it can be reasonably concluded that diclofenac diethylamine can be formulated into the transdermal matrix type patches to sustain its release characteristics and the polymeric composition (PVP/EC, 1:2) was found to be the best choice for manufacturing transdermal patches of diclofenac diethylamine among the formulations studied. ß
DESIGN AND INVITRO EVALUATION OF DICLOFENAC-PARACETAMOL DUAL RELEASE TRANSDERMAL PATCH
International Journal of Pharmacy & Therapeutics
The plan of this current study is to design the dual release transdermal patches (Dual Trans) and to perform the physiochemical and invitro evaluation studies for it. The present study proved that Transdermal patch containing two drugs i.e., Diclofenac potassium (Diclo) and Paracetamol (Para) follows simultaneous release pattern of drug without interacting the release of each other and also it focus its effect on chronic pain associated with skeleton-muscular disorders such as Rheumatoid arthritis. In this study Diclo-Para Dual Trans was prepared by solvent evaporation method using different polymer like Ethyl Cellulose, HPMC with varying proportions, Dimethyl Sulfoxide (DMSO) as a skin permeation enhancers and Polyethylene Glycol is used as a plasticizer. The prepared patches were evaluated for its thickness, weight variation, folding endurance, moisture content, drug content uniformity and also taken for invitro permeation study, invitro release kinetics studies and skin irritation studies. A drug polymer interaction was studied by FTIR. Invitro release and permeation studies were performed by using Franz-diffusion cell. The Results shows that patches prepared with HPMC and DMSO showed higher % moisture transmission and desired % drug release of both the drugs Diclofenac and Paracetamol. Also the study reveals that the formulation containing HPMC (with drug and polymer ratio 1:1) has ideal zero-order release kinetics and best fit for Peppa’s fitting curve.
Development and evaluation of aceclofenac transdermal patches with different permeation enhancers
2015
This research work was an attempt to formulate and evaluate matrix-type transdermal therapeutic system containing Aceclofenac with different permeation enhancers (in different 3 ratios) by the solvent evaporation technique and explores the effect of permeation enhancers on the in vitro permeability of aceclofenac across excised goat skin. Matrix transdermal patches were prepared by using hydroxyl propyl methyl cellulose (HPMC) by incorporating dibutyl phthalate incorporated as plasticizer and oleic acid, peppermint oil and iso-propyl myristrate (IPM) as permeation enhancers in different 3 ratios 2%, 4% and 6% v/v in whole formula. Permeation studies were performed using modified Franz diffusion cell. All the patches were uniform with respect to physiochemical evaluation. The in-vitro permeation study indicate that formulation ATP-3(6% v/v oleic acid) showed maximum release of 74.513% in 12 hrs emerging to be ideal formulation. The developed transdermal patches increase the efficacy ...
Biochimica et Biophysica Acta (BBA) - Biomembranes, 2001
Transfenac, a lotion-like formulation of diclofenac, is described. It consists of pharmaceutically acceptable ingredients and mediates the agent transport through intact skin and into the target tissues. Therapeutically meaningful drug concentrations in the target tissue are reached even when the administered drug dose in Transfenac is below 0.5 mg/kg body weight. Ultradeformable agent carriers, called Transfersomes, form the basis of Transfenac. These Transfersomes are proposed to cross the skin spontaneously under the influence of transepidermal water activity gradient (see [Biochim. Biophys. Acta 1104 (1992) 226]). Diclofenac association with ultradeformable carriers permits it to have a longer effect and to reach 10-times higher concentrations in the tissues under the skin in comparison with the drug from a commercial hydrogel. For example, Transfenac achieves intramuscular agent concentrations between 0.5 and 2 Wg/g and 2 and 20 Wg/g at t = 12 h, depending on the tissue depth, when it is administered in the dose range 0.25^2 mg/kg of rat body weight. A much higher drug concentration in a hydrogel (1.25^10 mg/kg body weight) creates the drug level of only 6 0.5 Wg/g in the muscle. The drug concentration in the rat patella for these two types of formulation is between 1 Wg/g and 5 Wg/g or 0.4 Wg/g, respectively. The relative advantage of diclofenac delivery by means of ultradeformable carriers increases with the treated muscle thickness and with decreasing drug dose, as seen in mice, rats and pigs; this can be explained by assuming that the drug associated with carriers is cleared less efficiently by the dermal capillary plexus. In pigs it suffices to use 0.3 mg of diclofenac in highly deformable vesicles per kg body weight, spread over an area of 25 cm 2 , to ensure therapeutic drug concentration in a 5-cm thick muscle specimen, collected under the agent application site. When the drug is used in a hydrogel at 8 times higher dose, the average intramuscular concentration is at least three times lower and subtherapeutic. This suggests that diclofenac in Transfersomes has the potential to replace combined oral/topical diclofenac administration in humans. ß 2001 Published by Elsevier Science B.V.