Formulation and comparative evaluation of bioadhesive containing diclofenac sodium and commercial enteric coated tablets in-vitro and in dogs

• Published in: International journal of pharmaceutics Vol. 133; no. 1; pp. 149 - 153
• Main Author: Hosny, Ehab A.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 14-05-1996; Elsevier
• Subjects: Bioadhesive tablets; Biological and medical sciences; Diclofenac sodium; Dogs; Enteric coated tablets; Formulation; General pharmacology; In-vitro; In-vivo; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Bioadhesive tablets; Enteric coated tablets; Formulation; Dogs; Diclofenac sodium; In-vivo; In-vitro; Fissipedia; Carnivora; Digestive system; Enteric coating; In vitro; Property formulation relationship; Non steroidal antiinflammatory agent; In vivo; Vertebrata; Mammalia; Animal; Dosage form; Tablet; Dog
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/0378-5173(95)04426-4

Polycarbophil containing diclofenac sodium tablets were formulated using two different size of granules. The granules were obtained by evaporation under reduced pressure of polycarbophil particles loaded with alcoholic solution of the drug. The in-vitro release of these bioadhesive containing tablets was evaluated together with that of Ciba-Geigy commercially available enteric coated tablets ‘Voltaren’ in simulated gastric fluid for 2 h followed by another 2 h in simulated intestinal fluid. The Voltaren tablets released no drug in simulated gastric fluid but released all their drug contents within 1 h in simulated intestinal fluid. The tablets formulated using polycarbophil granules of smaller size (0.18-0.313 mm) released about 13% of their drug contents in simulated gastric fluid and released the remaining drug in simulated intestinal fluid within 0.5 h of dissolution, while tablets formulated with larger granules size (0.5-0.8 mm) released 10% of their drug contents in the first medium and released the remaining drug within 2 h in the second. The in-vivo evaluation in dogs of these two tablet formulations of polycarbophil and that of entericcoated Voltaren tablets each containing 50 mg drug revealed that the bioadhesive tablets formulated with smaller granules size were bioequivalent to Voltaren tablets producing a non-significantly different (
P > 0.05)
C
max,
T
max and AUC. The results also indicated the effect of bioadhesive granules size on rate and extent of absorption where tablets formulated with smaller granules size showed higher
C
max, shorter
T
max, larger AUC and higher relative bioavailability compared with those tablets formulated with larger granules size.