الفهرس | Only 14 pages are availabe for public view |
Abstract Pantoprazole sodium, a proton pump inhibitor (PPI), exhibits potent and long lasting inhibition of gastric acid secretion. Pantoprazole sodium like other proton pump inhibitors degrades at pH 1-2, within minutes. Thus the aim of this thesis is to formulate pantoprazole sodium in tablet dosage forms for trans-mucosal delivery through buccal and sublingual mucosae in the oral cavity, this gives rapid systemic absorption and avoids gastric degradation as well as first pass metabolism in the liver. Pantoprazole sodium buccoadhesive tablets were prepared by direct compression technique using different bioadhesive polymers. The effects of varying the bioadhesive polymer and the drug:polymer ratio were studied. The formulae were evaluated concerning their mucoadhesive force, swelling ability and in-vitro drug release. The best formula, showing the highest mucoadhesive force (24.4x103dyne/cm2) and optimum drug release after 6 hrs. (91.3%), was the one consisting of a polymer combination of sodium alginate high viscosity and chitosan; with 1:3, D:P ratio. this formula was selected for further in-vivo studies. Pantoprazole sodium was also formulated as sublingual tablet by direct compression technique. The effect of microcrystalline cellulose concentration (16 and 33% w/w), superdisintegrant type (Ac-Di-Sol, Explotab and Crospovidone) and Superdisintegrant concentration (5,10 and 15% w/w) on the disintegration time and drug dissolution from sublingual tablet formulations were investigated. The best formula, showing the lowest disintegration time (1.86 min.) and the highest percent of drug dissolved after 5 mins. (95.6%), was the one consisting of 5% Ac-Di-Sol, 16% microcrystalline cellulose and mannitol 45%. This formula was selected for further in-vivo studies. The anti-ulcer activity of selected pantoprazole sodium buccoadhesive and sublingual tablets was done by evaluating their ability to protect guinea pigs from experimentally induced gastric ulcers using ulcer index method. Finally the selected buccoadhesive and sublingual pantoprazole sodium tablets proved to be promising for oral trans-mucosal delivery of pantoprazole. |