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Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures

Wei, Yangjie
http://rave.ohiolink.edu/etdc/view?acc_num=mco1404694762

Abstract Details

2014, Master of Science (MS), University of Toledo, College of Pharmacy.
Lidocaine HCl (LID), an amino amide-type local anesthetic, is a bitter drug that is widely used in dental procedures. It is administered in the form of injections in the oral cavity. This study aims to mask the bitter taste of injectable LID formulation using hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and sodium saccharin. Inclusion complexes of LID and HP-ß-CD were prepared by the solution method in 1:1 and 1:2 molar ratios. Inclusion complexes in solution were studied using phase solubility in phosphate buffer solutions (50 mM, pH 8, 9, and 10). Freeze dried inclusion complexes were characterized using differential scanning calorimetry (DSC), X-ray analysis (X-ray), Fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), and in vitro release. Injectable formulations were prepared using inclusion complexes and characterized for stability using HPLC and for taste using an Alpha MOS ASTREE ETongue. The association constants of HP-ß-CD with lidocaine free base and its ionized form were found to be 26.23 ± 0.00025 M-1 and 0.8694 ± 0.00045 M-1, respectively. Results obtained from the DSC, X-ray, FT-IR, and SEM confirmed the inclusion of LID within the non-polar cavity of HP-ß-CD. HP-ß-CD did not show a significant decrease in the release of LID at the 1:1 molar ratio, but slightly delayed its release at the 1:2 molar ratio. The drug content of LID in inclusion complexes was found to be stable for up to 6 months when stored at 4°C, 25°C, and 40°C. The taste evaluation study indicated that HP-ß-CD (1:1 and 1:2 molar ratio) significantly improved the bitter taste of LID injectable formulation. In conclusion, inclusion complex in the 1:1 molar ratio with 0.09% sodium saccharin was considered to be optimum in masking the bitter taste of LID.
Sai Boddu (Advisor)
Kenneth Alexander (Committee Member)
Jerry Nesamony (Committee Member)
Pharmaceuticals; Pharmacy Sciences

Recommended Citations

Citations

  • Wei, Y. (2014). Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures [Master's thesis, University of Toledo]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=mco1404694762

    APA Style (7th edition)

  • Wei, Yangjie. Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures. 2014. University of Toledo, Master's thesis. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=mco1404694762.

    MLA Style (8th edition)

  • Wei, Yangjie. "Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures." Master's thesis, University of Toledo, 2014. http://rave.ohiolink.edu/etdc/view?acc_num=mco1404694762

    Chicago Manual of Style (17th edition)

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This open access ETD is published by University of Toledo Health Science Campus and OhioLINK.