Bakhsh S., Khan G.M., Menaa F., Khan B.A.
Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, KPK, Pakistan; Department of Pharmacy, Quaid-e-Azam University, Islamabad, Pakistan; Department of Pharmaceutical Sciences, Medicine and Nanotechnology, Fluorotronics USA, Inc., Global Innovation and Trade, Inc., San Diego, CA, United States; School of Pharmacy, Kampala International University, Western Campus, Uganda
Bakhsh, S., Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, KPK, Pakistan; Khan, G.M., Department of Pharmacy, Quaid-e-Azam University, Islamabad, Pakistan; Menaa, F., Department of Pharmaceutical Sciences, Medicine and Nanotechnology, Fluorotronics USA, Inc., Global Innovation and Trade, Inc., San Diego, CA, United States; Khan, B.A., Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, KPK, Pakistan, School of Pharmacy, Kampala International University, Western Campus, Uganda
The present study was conducted to formulate controlled release dosage forms containing Ibuprofen with Eudragit® S 100 polymer. The tablets were formulated at three different ratios with the polymer to investigate the effect of different concentrations of polymer on in vitro drug release patterns/kinetics and in vivo absorption/pharmacokinetics. Pre-formulation studies were conducted including bulk density, tapped density, compressibility index, Hausner ratio and angle of repose. In vitro studies were conducted using phosphate buffer (pH 7.4) as dissolution medium. In vivo performance was evaluated using albino rabbits. Physico-chemical characteristics (i.e. dimensional tests, weight variation, hardness, friability and drug content determination) fell in the USP acceptable limits. The compressibility index was found to range between 12.02±0.01% and 18.66±0.03%, the Hausner ratio varied between 1.02±0.01 and 1.19±0.10 and the angle of repose ranged from 15.19±0.01 to 24.52±0.10, all indicating better flow properties than the bulk-reference standard. Both bulk and tapped densities also fell in the USP acceptable range. Ibuprofen market tablets showed Tmax of 2.1±0.4h, which was significantly (P-value <0.05) lower compared to that of the reference standard (i.e. 4.09±1.3h). Ibuprofen test formulation has a half-life (t<inf>1/2</inf>) of 16.9±2.5h, which was significantly (P-value<0.001) higher compared to that of the reference standard (i.e. 9.23±2.9h). Eudragit® S 100 polymers can be used efficiently to develop directly compressed prolonged release tablets.
eudragit; excipient; ibuprofen; phosphate; delayed release formulation; ibuprofen; methylmethacrylate-methacrylic acid copolymer; nonsteroid antiinflammatory agent; polymethacrylic acid derivative; albino rabbit; angle of repose; animal experiment; Article; bulk density; controlled release formulation; dissolution; drug blood level; drug formulation; drug half life; drug marketing; drug screening; Hausner ratio; hydrophilicity; in vitro study; in vivo study; matrix tablet; maximum plasma concentration; nonhuman; pH; physical chemistry; plasma concentration-time curve; preformulation; reproducibility; tablet compression; tablet formulation; tablet friability; tablet hardness; time to maximum plasma concentration; weight variation; animal; chemical phenomena; delayed release formulation; rabbit; Animals; Anti-Inflammatory Agents, Non-Steroidal; Delayed-Action Preparations; Excipients; Hydrophobic and Hydrophilic Interactions; Ibuprofen; Polymethacrylic Acids; Rabbits