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        Sustained delivery of cefdinir to upper gastrointestinal tract using calcium alginate beads: a formulation by design

        Radhakrishnan Praveen,Sandeep Kumar Singh,Priya Ranjan Prasad Verma,Jerome Karippamattom George 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.6

        The present research demonstrates the developmentand characterization of alginate based multiunitfloating dosage form for sustained delivery of cefdinir tothe upper gastrointestinal tract. The method involved ionicgelation of sodium alginate solution containing suspendeddrug and myristyl alcohol (release modifier and buoyancyregulator) by calcium ions followed by freeze drying. Fourier transform infrared spectroscopy and differentialscanning calorimetry studies revealed that there were noincompatibilities between drug and excipients. The effectof various process variables; amount of sodium alginate,myristyl alcohol and cefdinir; on critical parameters likedrug loading, particle size and mean dissolution time(MDT) was modelled using Box–Behnken design andstudied using response surface plots and regression equations. The observed and predicted r2 values were inagreement in case of all the responses which marks thevalidity of developed model. The particle size, drug loadingand MDT were found to be strongly dependent on thevariables studied. The beads showed high drug loading upto 65.41 % and extended drug release up to 24 h in 0.1 Nhydrochloric acid. The beads exhibited 100 % buoyancywithout any lag time up to 24 h despite of the high drugloading. The mechanism of drug release was found to beFickian diffusion.

      • KCI등재

        Cross linked alginate gel beads as floating drug delivery system for cefdinir: optimization using Box–Behnken design

        Radhakrishnan Praveen,Priya Ranjan Prasad Verma,Sandeep Kumar Singh,Jerome Karippamattom George 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.2

        Regional absorption of several drugs necessitatesthe continuous monitoring of the movement of dosageform through gastro-intestinal tract. Sometimes it isimportant to deliver the drug at a particular physiologicalregion of the gastrointestinal tract for better effects. Floating delivery system is a prominent approach to releasethe drug in the gastric fluid. The objective of present studywas to formulate, evaluate and optimize cefdinir loadedintra-gastric floating beads of sodium alginate. Floatingalginate beads were prepared by ionic gelation methodaccording to Box–Behnken design with three factors variedat three levels. Uniform beads buoyant up to 24 h wereformed with rough surface and porous internal structure. Characterization by Fourier transform infrared spectroscopy,differential scanning calorimetry, thermo-gravimetricanalysis and powder x-ray diffractometry suggested anexcellent compatibility of drug with excipients and formulationprocess. The effect of selected independentvariables [amount of sodium alginate (X1), myristyl alcohol(X2) and cefdinir (X3) each at three levels] on thedependent variables [density (Y1), entrapment efficiency(Y2), time to release 20 % (Y3), cumulative percentage ofcefdinir released at 12th hour (Y4) and dissolution efficiency(Y5)] were studied using regression equations andresponse surface plots. The predicted and adjusted r² valueswere in reasonable agreement and the models weresignificant with p<0.05. Criteria were set for eachresponses and optimized formulation was preparedaccording to the software determined levels. The predictedand observed responses were in good agreement with lowpercent bias errors (<10 %), marking the validity of thedeveloped model. Thus, cefdinir loaded, extended release,intra-gastric floating gel beads of calcium alginate wereformulated and optimized.

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