A pharmaceutical study on an antidepressant drug / Nabil Ashraf Ibrahim Shoman ; Supervised Mohamed Ahmed Elnabarawi , Bhaskara Jasti , Mahmoud Hassan Teaima

Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutics

This thesis aims to formulate, evaluate two satiety-enhancing gastroretentive floating dosage forms of bupropion hydrochloride (BUP): floating raft systems (FRS), and floating tablets (FT). BUP is a highly water-soluble antidepressant drug that mediates weight loss, subsequently, these swellable FRS and FT can increase satiety and provide promising outcomes for treating depression with comorbid binge eating disorder (BED), through retaining as buoyant in the stomach and sustaining the BUP release. BED recently become a global health care issue for clinicians with detrimental effects on all organ systems. A multidisciplinary strategy including pharmacotherapy is required for its management. For BUP FRS, sixteen formulations with in-situ gelling and floating properties were prepared. These liquid solutions incorporate effervescent agent (calcium carbonate) with different concentrations of glyceride lipids (Compritol® 888 ATO & Precirol® ATO 5) and with gel-forming polymers (pectin or alginate) to retard the drug release rate. Design Expert® software was applied in a 24 full factorial design to study the effect of different formulation variables (A: Type of in situ gel-forming polymer, B: Type of glyceride lipid, C: Lipid concentration, and D: CaCO3 concentration) on their relevant responses (Gelation lag time (Y1), Floating lag time (Y2), drug release percent after 1 h (Y3) and after 8 h (Y4)). The optimal FRS (3% alginate, 2% precirol®, and 2% CaCO3) was further investigated for compatibility, and bioavailability study in healthy volunteers relative to the marketed Wellbutrin® SR tablets. This system provided an optimum viscosity that allowed rapid gelation in the stomach, excellent floating, and controlled BUP release with a comparable bioavailability. In conclusion, this FRS would be a novel especially designed liquid form to improve patient compliance and drug efficacy through controlling BUP release, to treat depression associated with eating disorders or dysphagia

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