Abstract

Dexibuprofen is practically water-insoluble (non-steroidal anti-inflammatory) drug which has a better anti-inflammatory effect than ibuprofen. The aim of the present work was to apply a coating mixture of pectin and rutin to dexibuprofen by utilizing air suspension technique for decreasing its ulcerogenic activity and improving its bioavailability in rats. The bioavailability of the uncoated and coated drug as well as the effect of the coat on the histopathological features of gastric mucosa was determined using male albino rats. Uncoated dexibuprofen administered to rats, histopathological examination revealed that all the animals showed pronounced necrotic gastric mucosa with severe dilated congested blood vessels. However, microencapsulation of dexibuprofen with pectin and rutin mixture had increased the dissolution rate of the drug by about 38% in acidic and 82% in alkaline pH compared to the uncoated drug. Coating the drug with pectin-rutin mixture significantly reduced ulcer incidence as well as ulcer index (p< 0.05) as compared with a free form of the drug in animals administered the same doses. Encapsulating the drug in a carrier with slowing its diffusion into the mucosal media could alleviate the problem of gastric ulceration. Dexibuprofen coated with pectin-rutin mixture administered to rats, histopathological examination revealed that stomach tissue of animals showed normal gastric mucosa. Therefore, Pectin and rutin with dexibuprofen shows higher dissolution as well as higher bioavailability than the free form. Beside that the encapsulated dexibuprofen were found to have lower ulcergenoic activity than the free form of the drug.

keywords Microencapsulation; Rutin and pectin; Non-steroidal anti-inflammatory drugs; Fluidized bed technique; Dexibuprofen