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Mani Ganesh(마니 가니쉬),Mei Mei Peng(팽메이메이),Aziz Abidov(아비도프 아지즈),Han Seok Oh(오한석),Min Cheol Shin(신민철),Won Geun Joo(주원근),Da Sol Shin(신다솔),Han Gyu Lee(이한규),Tae Jun Park(박태준),Hyun Tae Jang(장현태) 한국산학기술학회 2015 한국산학기술학회 학술대회 Vol.2015 No.1
This work is to develop once daily ace-clofenac controlled drug release formulations by the incorporation of aceclofenac cocrystals in alginate beads (modified release super-saturated drug delivery system). To achieve this goal, aceclofenac cocrystals were prepared using chitosan as a co-former. The synthesized materials were characterized by FT-IR, SEM and XRD technique. Enhancement of dissolution rate was assessed in simulated gastric fluid (pH 1.2). Enhanced oral bioavailability of aceclofenac has been achieved using chitosan cocrystals of aceclofenac and its entrapment into alginate matrix a super saturated drug delivery system (SDDS). Prepared SDDS were evaluated by various physiochemical and pharmacological methods. The result revealed that theprimary cocrystals enhanced the solubility of the drug and the thick gelled polymer matrix that formed from swelling of calcium alginate beads makes it to release the drug in continuous and sustained manner by supersaturated drug diffusion. The Cmax, Tmax and relative bioavailability for aceclofenac cocrystal and aceclofenac SDDS were 2.06 ± 0.42 µg/ml, 1 h, 159.72 ± 10.84 and 2.01 µg/ml, 1 h, 352.76 ± 12.91, respectively. Anti-inflammatory activity of aceclofenac was significantly improved with the SDDS. With respect to the results, it revealed that the SDDS described herein might be a promising tool for the oral sustained release of aceclofenac and likely for that of various other poorly soluble drugs.