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sustained release and enhanced oral bioavailability of rivaroxaban by plga nanoparticles with no food effect
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نویسنده
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anwer md. khalid ,mohammad muqtader ,iqbal muzaffar ,ansari mohd nazam ,ezzeldin essam ,fatima farhat ,alshahrani saad m. ,aldawsari mohammed f. ,alalaiwe ahmed ,alzahrani aiman a. ,aldayel abdullah m.
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منبع
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journal of thrombosis and thrombolysis - 2020 - دوره : 49 - شماره : 3 - صفحه:404 -412
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چکیده
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The purpose of the currents study was to enhance bioavailability of rivaroxaban (rxb) and reduce the food effect. rxb loaded plga nanoparticles (rxb-plga-nps) were prepared by emulsion solvent evaporation method and optimized using central composite design (cdd). the optimized rxb-plga-nps (f8) with composition, plga (125 mg), pva (0.5%w/w) and rxb (20 mg) was found optimum with particle size (496 ± 8.5 nm), pdi (0.607), zp (− 18.41 ± 3.14 mv), %ee (87.9 ± 8.6) and %dl (9.5 ± 1.6). the optimized nps (f8) was further evaluated in vitro for dsc, ftir, sem and in vitro release studies. a comparative pharmacokinetic studies with commercial tablet (xarelto®) were conducted on fasted and fed state rats. compared to commercial tablet (xarelto®), the rxb-plga-nps (f8) exhibited a significant enhancement of bioavailability in both fasted and fed state. in addition, the bioavailability of rxb from nps (f8) was found unaffected in the presence of food.
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کلیدواژه
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rivaroxaban ,plga ,nanoparticles ,bioavailability ,food effect
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آدرس
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prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, king saud university, college of pharmacy, department of pharmaceutical chemistry, bioavailability laboratory, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmacology, saudi arabia, king saud university, college of pharmacy, department of pharmaceutical chemistry, bioavailability laboratory, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia, prince sattam bin abdulaziz university, college of pharmacy, department of pharmaceutics, saudi arabia
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Authors
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