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Development and Evaluation of a Biopolymer based Ceftriaxone Sodium Oral Formulation

Patel, Nachiket

Abstract Details

2014, Master of Science (MS), University of Toledo, Pharmaceutical Sciences (Industrial Pharmacy).
Ceftriaxone sodium (CS) is a third-generation cephalosporin and belongs to BCS Class III. This antibiotic cannot be absorbed orally owing to its poor permeability through GI epithelia and its acid labile nature. The purpose of present investigation was to develop and evaluate a multiparticulate system exploiting pH-sensitive property and specific biodegradability of calcium alginate beads, for intestinal delivery of CS. Beads of CS entrapped in sodium alginate consisting of different polymers such as sodium carboxymethylcellulose, acacia, HPMC K4M and HPMC K15M as drug release modifiers were prepared by ionotropic gelation method using calcium chloride as a cross-linking agent followed by enteric coating with cellulose acetate phthalate. Sustained-release polymeric beads were then evaluated for entrapment efficiency using HPLC, in vitro drug release examined in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8), swellability, particle size and surface morphology using optical microscopy and Scanning Electron Microscopy (SEM), and surface characterization using Atomic Force Microscopy (AFM). Thermal Gravimetric Analysis (TGA) was utilized to check the strength of the polymer matrix and thermal stability of the prepared formulations. The drug entrapment efficiency for the optimized formulation was determined to be 74.66 ± 4.99%. Swelling properties of drug-loaded beads were found to be in range from 0.859 to 3.35. Beads coated with cellulose acetate phthalate and carboxymethylcellulose aqueous polymer dispersion exhibited sustained release and followed first-order kinetics and the mechanism of diffusion was anomalous or non-Fickian (diffusion and erosion dependent swelling mechanism). The particle size of the beads was between 1.039 ± 0.197 mm to 2.146 ± 0.357 mm. TGA demonstrated the cross-linking efficiency and thermal stability of the beads. SEM images demonstrated the structure and surface of the beads. AFM images demonstrated composition and polymer dependent variations in surface structure, morphology, and roughness.
Jerry Nesamony (Committee Chair)
Sai Hanuman Sagar Boddu (Committee Member)
Zahoor Shah (Committee Member)
110 p.

Recommended Citations

Citations

  • Patel, N. (2014). Development and Evaluation of a Biopolymer based Ceftriaxone Sodium Oral Formulation [Master's thesis, University of Toledo]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=mco1404772298

    APA Style (7th edition)

  • Patel, Nachiket. Development and Evaluation of a Biopolymer based Ceftriaxone Sodium Oral Formulation. 2014. University of Toledo, Master's thesis. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=mco1404772298.

    MLA Style (8th edition)

  • Patel, Nachiket. "Development and Evaluation of a Biopolymer based Ceftriaxone Sodium Oral Formulation." Master's thesis, University of Toledo, 2014. http://rave.ohiolink.edu/etdc/view?acc_num=mco1404772298

    Chicago Manual of Style (17th edition)