Titre du document / Document title

Transbuccal permeation, anti-inflammatory activity and clinical efficacy of diroxicam formulated in different gels

Auteur(s) / Author(s)

ATTI M. A. ⁽¹⁾ ; EL-GIBALY I. ⁽¹⁾ ; SHALTOUT S. E. ⁽²⁾ ; FETIH G. N. ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Pharmaceutics, Faculty of Pharmacy, Assim University, Assiut, EGYPTE
⁽²⁾ Oral and Maxillofacial Surgery Section, Faculty of Medicine, Assiut University Hospital, Assiut University, Assiut, EGYPTE

Résumé / Abstract

In attempts to avoid the systemic side effects of piroxicam (PC) (e.g. gastrotoxicity), several buccal gel formulations containing PC were prepared and their effects on the characteristics of the drug permeation through rabbit buccal mucosa in-vitro were evaluated using a Franz-type diffusion cell. The general rank order of the total flux of 0.5% PC from gels was found to be: hydroxypropylmethylcellulose (HPMC, 2.5%) > hydroxypropylcellulose (HPC, 2.5%) > sodium alginate (Na alg., 7%) > methylcellulose (MC, 3%) > hydroxyethylcellulose (HEC, 1.5%) > carbopol 934 (Carb. 934, 1%) ≥ sodium carboxymethylcellulose (NaCMC, 2%) > pluronic F-127 (PF-127, 20%) > polyvinyl alcohol (PVA, 10%). The effect of various penetration enhancers 1% sodium lauryl sulphate (NaLS), 3% sodium deoxycholate (NaDC), 3% sodium tauroglycocholate (NaTGC) on the rate of permeation across the excised buccal mucosa (of 0.5% PC in gels prepared using 3% MC, 2.5% HPMC or 7% Na alg. base) and histology of the buccal epithelium was also investigated. Pharmacodynamic evaluation of the anti-inflammatory activity of PC in these gel formulations (containing 3% NaDC as an enhancer) was carried out using the kaolin-induced rat paw oedema method. The results obtained indicated that PC administered in 7% Na alg. or 2.5% HPMC gel bases was significantly more effective than the 3% MC gel and oral drug solution in suppressing oedema formation in rats. Comparative clinical studies were conducted in patients with post-operative dental pain and oedema following maxillofacial operations. The results revealed that 7% Na alg. and 2.5% HPMC gel formulations applied to the buccal mucosa were slightly better than or equally effective to the orally administered commercial product (Feldene Flash® tablet) in reducing pain level, swelling and tenderness within a period of 4 days. These findings suggest that PC (0.5%) administered in the buccal gel may present a potential therapeutical use as a strong anti-inflammatory and analgesic agent.

Revue / Journal Title

International journal of pharmaceutics   ISSN 0378-5173   CODEN IJPHDE 

Source / Source

2004, vol. 276, n^o1-2, pp. 11-28 [18 page(s) (article)] (1 p.1/4)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1978) (Revue)

Mots-clés anglais / English Keywords

Enzyme ; Oxidoreductases ; Prostaglandin-endoperoxide synthase ; Oxicam derivatives ; Enzyme inhibitor ; Rodentia ; Vertebrata ; Mammalia ; Lagomorpha ; Analgesic ; Antipyretic ; Rat ; Penetration ; Permeability ; Mucosa ; Rabbit ; Animal ; Piroxicam ; Colloidal gel ; Non steroidal antiinflammatory agent ; Permeation ;

Mots-clés français / French Keywords

Enzyme ; Oxidoreductases ; Prostaglandin-endoperoxide synthase ; Oxicam dérivé ; Inhibiteur enzyme ; Rodentia ; Vertebrata ; Mammalia ; Lagomorpha ; Analgésique ; Antipyrétique ; Rat ; Pénétration ; Perméabilité ; Muqueuse ; Lapin ; Animal ; Piroxicam ; Gel colloïdal ; Antiinflammatoire non stéroïde ; Perméation ;

Mots-clés espagnols / Spanish Keywords

Enzima ; Oxidoreductases ; Prostaglandin-endoperoxide synthase ; Oxicam derivado ; Inhibidor enzima ; Rodentia ; Vertebrata ; Mammalia ; Lagomorpha ; Analgésico ; Antipirético ; Rata ; Penetración ; Permeabilidad ; Mucosa ; Conejo ; Animal ; Piroxicam ; Gel coloidal ; Antiinflamatorio no esteroide ; Permeación ;

Mots-clés d'auteur / Author Keywords

Piroxicam ; Rabbit buccal mucosa ; Buccal permeability ; Penetration enhancer ; Rat paw oedema ;

Localisation / Location

INIST-CNRS, Cote INIST : 16510, 35400011001907.0020