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        Design, optimization and pharmacokinetics of novel prolonged gastroretentive drug delivery system of quetiapine fumarate

        Dharmik M. Mehta,Punit B. Parejiya,Hetal K. Patel,Palak J. Trivedi,Disha D. Suthar,Pragna K. Shelat 한국약제학회 2016 Journal of Pharmaceutical Investigation Vol.46 No.5

        Present study attempts to overcome pH-dependent solubility, a limitation for oral delivery of poorly soluble BCS class-II drugs. A pH independent, patient compliant, dual working gastroretentive drug delivery system of model drug quetiapine fumarate (QF) was fabricated by unique combination approach of mucoadhesion and floating. Bilayer tablets comprising floating adhesive layer (FL) and matrix layer (ML) was systematically optimized by applying 32 full factorial experimental designs. Selected variables for FL: Polyox 303WSR (X1FL) and alginate beads (X2FL), and for ML: HPMC K100M (X1ML) and fumaric acid (X2ML) were studied against responses for FL: floating lag time (R1FL), total floating time (R2FL) and adhesion force (R3FL) and for ML: percentage drug released at 2 h—Q2h (R1ML), 8 h—Q8h (R2ML), and 18 h—Q18h (R3ML), respectively. Optimized batch (OP) showed floating lag time (6.5 h), total floating time (14 h), adhesion force (0.82 N) and Q18h ([90 %). Pharmacokinetic study of OP and immediate release market product demonstrated improved bioavailability (*12 % higher AUC0–?) of OP. In a nutshell, developed drug delivery system can be fabricated as a platform for QF and similar BCS class-II drugs with pH dependent solubility.

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