Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures |
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Authors: | Yangjie Wei Michael P. Nedley Sarit B. Bhaduri Xavier Bredzinski Sai H. S. Boddu |
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Affiliation: | .College of Pharmacy and Pharmaceutical Sciences, The University of Toledo HSC, 3000 Arlington Ave. (MS1013), Toledo, Ohio 43614 USA ;.Division of Dentistry, The University of Toledo, Toledo, Ohio 43614 USA ;.Department of Mechanical, Industrial and Manufacturing Engineering, The University of Toledo, Toledo, Ohio USA ;.Alpha Mos America, Inc., 7502 Connelley Drive, Suite 110, Hanover, Maryland 21076 USA |
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Abstract: | Several attempts have been made to mask the bitter taste of oral formulations, but none have been made for injectable formulations. This study aims to mask the bitter taste of dental lidocaine HCl (LID) injection using hydroxypropyl-β-cyclodextrin (HP-β-CD) and sodium saccharin. Inclusion complexes of LID and HP-β-CD were prepared by the solution method in 1:1 and 1:2 M ratios. Inclusion complexes in solution were studied using phase solubility in phosphate buffer solutions (pH 8, 9, and 10). Freeze-dried inclusion complexes were characterized using differential scanning calorimetry (DSC), X-ray, Fourier transform infrared (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 and for taste using an Alpha MOS ASTREE electronic tongue (ETongue). The association constants of HP-β-CD with lidocaine-free base and its ionized form were found to be 26.23 ± 0.00025 and 0.8694 ± 0.00045 M−1, respectively. Characterization studies confirmed the formation of stable inclusion complexes of LID and HP-β-CD. Injectable formulations were found to be stable for up to 6 months at 4°C, 25°C, and 40°C. The taste evaluation study indicated that HP-β-CD (1:1 and 1:2 M ratios) significantly improved the bitter taste of LID injectable formulation. In conclusion, inclusion complex in the 1:1 M ratio with 0.09% sodium saccharin was considered to be optimum in masking the bitter taste of LID.KEY WORDS: bitter taste, HP-β-CD, inclusion complex, injectable, lidocaine HCl, taste masking |
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