Sodium diclofenac, delivery

Gonzalez-Rodriguez M, Maestrelli F. Mura P. Rabasco AM. In vitro release of sodium diclofenac from a central core matrix tablet aimed for colonic drug delivery. Eur J Hiarm Sci 2003 20 125-31. 

Egito and colleagues have been working for over a decade on the extraction of xylan from corn cobs and its use for the development of microparticles as drug carriers for colon-specific delivery of anti-inflammatory and toxic drugs, such as sodium diclofenac (SD], 5-aminosalycilic acid [5-ASA], and usnic acid (UA). Xylan-coated microparticles have also been developed by Egito and co-workers in order to deliver magnetite particles [44]. Different microencapsulation techniques have been used for... 

M. Cohen-Avrahami, A. Aserin, N. Garti, Hn mesophase and peptide cell-penetrating enhancers for improved transdermal delivery of sodium diclofenac. Colloids Surf. B 77, 131-138 (2010)... 

Most drags do not penetrate epithelial barriers at rates sufficient for clinical usefulness without permeability enhancers, chemicals that are routinely added to dermal drag delivery products [17]. For example, using human skin in an in vitro study, it was demonstrated that sodium diclofenac = 0.70) permeability was enhanced by a mixture containing the hpophiles oleic acid = 7.64) and o-limonene = 4.57) [18]. 

Datta, M., Kaur, M., 2014. In vitro release of sodium diclofenac from poloxamer 188 modified montmorillonite as an oral drug delivery vehicle. luL J. Pharm. Pharm. Sci. 6 (5), 100-110. 

The buccal permeability of the non-steroidal antiinflammatory drug, diclofenac sodium, has been evaluated in a dog model. The dog was selected because of the similarity of its buccal mucosa to that of man. Analysis of the buccal data indicated that diclofenac sodium permeability followed an essentially zero-order kinetic process with a minimal lag phase. Permeability of the drug was estimated to be 3 mg/cm2.h but significant differences were observed between animals. The absorption rate with the transbuccal delivery device decreased with time whereas the corresponding rate with a saturated solution was constant. This difference was attributed to the time dependency of drug delivery from the device and was modeled on the basis of release from a membrane-dispersed monolith combined with constant buccal permeability. The predictions of the model showed excellent agreement with the experimental data. 

The cumulative release profile for diclofenac sodium from the transbuccal delivery device exhibited a square root of time dependency over approximately 80% of the total release process (Figure 3). In view of the drug s solubility within the hydrogel ( 16 mg/cc) and the total loading (-420 mg/cc), dyjg2release was modelled as a dispersed monolith and a 3.19 x 10 cm /h diffusion coefficient was calculated. 

Figure 3. In vitro delivery of diclofenac sodium from a buccal drug delivery device (details of the dissolution method are given in the text). ...

Plasma concentrations of diclofenac sodium after application of the transbuccal delivery device (Figure 6) followed a different time course to that observed with the saturated solution. Plasma concentrations of the drug increased rapidly over the initial phase and achieved peak values of 2400-4000 ng/ml at 1 h after system application. Thereafter, the levels decreased slowly and converged to a mean value of 2250 ng/ml before the system was removed. Based on depletion analysis, 7.8 mg was delivered on average from the hydrogel discs over 4 h. 

Figure 6. Plasma concentrations of diclofenac sodium after application of a buccal drug delivery device to the mucosa of 4 Beagle dogs.

In several investigations the feasibility of development of a sustained-release form for diclofenac sodium was studied. Matrix-type formulation was designed, which appears to be a very attractive approach from process development and scale up points of view. HPMC is the most important hydrophilic polymer used for the preparation of oral controlled-release drug-delivery systems. - One of the most important characteristics of HPMC is the high swellability, which has a considerable effect on the release kinetics of the incorporated drug. 

Bv B, RD, S B, Abraham S, Furtado S, V M. Hollow microspheres of diclofenac sodium— Agastroreten-tive controlled delivery system. Pakistan Journal of Pharmaceutical Sciences. October 2008 21(4) 451— 454. PubMed PMID 18930869. 

Dutta R. K., Sahu S. (2012a). Development of diclofenac sodium loaded magnetic nanocarriers of pectin interacted with chitosan for targeted and sustained drug delivery. CoHoid ur ce 97,19-26. 

A controlled release preparation of diclofenac sodium, a non-steroidal anti-inflammatory agent, was developed for transdennal administration. PVAl and PVAl/polyacrylic acid(PAA) alloy membranes were prepared from a solvent-casting technique using different PVAl/PAA v/v ratios. The release of the drug from the membrane was evaluated under in viti o conditions at pH 7.4. The delivery system provided linear release without time lag, burst effect and boundary layer resistance. The effects of such variables as film thickness and PVAl/PAA ratio on the permeation behaviour of the polymeric membranes are discussed. The optimal PVAl/PAA was found to be 50/ 50. 48 refs. 

Chitosan has also been found to be beneficial in formulation development of delivery systems for local or systemic administration of drug through the rectal route. Chitosan microspheres encapsulating diclofenac sodium incorporated in hydrogels have been designed for efficient rectal administration [126]. Quaternized derivative of chitosan. 

Rosin biomaterial has film-forming ability, utilized in the development of film-based drug delivery systems and dosage forms. Sustained release of the drug has been achieved with rosin-coated pellets prepared using diclofenac sodium as a model drug. Therefore, rosins can be used in the development of transdermal drug delivery systems. 

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