Abstract
The aim of this study was to prepare diphenhydramine hydrochloride (DPH)-loaded orally fast-disintegrating mini-tablets (OFDMTs) containing either L-aspartic acid (Asp) or L-glutamic acid (Glu) as bitterness-suppressant, to characterize the prepared tablets and to evaluate their bitterness under conditions mimicking those of the oral cavity. The preparation of five formulation batches of the OFDMTs involved mixing DPH, with or without two different concentrations of Asp or Glu, and a premix containing a disintegrating agent. When all ingredients were well mixed, the mixture was directly compacted to form small (4 mm diameter) DPH-loaded OFDMTs. There were only small differences between the tablets with respect to mass, diameter, width and hardness. The disintegration times of the five formulation batches of DPH-loaded OFDMTs were measured using the OD-mate, a disintegration test apparatus in which conditions resemble those of the oral cavity. The disintegration times were all within 10 s of exposure to a medium representing the inside of the oral cavity. Rapid release profiles were observed for DPH, Asp and Glu in these dissolution tests. The taste sensor outputs of samples taken at different times (5 - 30 s) from the dissolution test solutions of the four DPH-loaded OFDMTs containing Asp or Glu were significantly inhibited compared with those of control DPH-loaded OFDMT. These results suggest that the inclusion of Asp or Glu in DPH-loaded OFDMTs is sufficient to mask bitterness in the oral cavity for the first 30 s after the tablet is placed in the mouth. It is anticipated that swallowing will have taken place within 30 s.
Highlights
The palatability of oral formulations is critical for good adherence, especially in pediatric and geriatric patients
The aim of this study was to prepare diphenhydramine hydrochloride (DPH)loaded orally fast-disintegrating mini-tablets (OFDMTs) containing either Laspartic acid (Asp) or L-glutamic acid (Glu) as bitterness-suppressant, to characterize the prepared tablets and to evaluate their bitterness under conditions mimicking those of the oral cavity
These results suggest that the inclusion of Asp or Glu in DPH-loaded OFDMTs is sufficient to mask bitterness in the oral cavity for the first 30 s after the tablet is placed in the mouth
Summary
The palatability of oral formulations is critical for good adherence, especially in pediatric and geriatric patients. Diphenhydramine hydrochloride (DPH) was chosen as a model drug as it is already widely used in pediatric and geriatric patients This drug is known to have a bitter taste [5] so the addition of a bitterness suppressant is essential when the OFDMTs containing DPH are expected to disintegrate rapidly in the oral cavity, resulting in high concentrations of DPH being exposed to bitterness receptors on the tongue. Such a level of bitterness would greatly decrease adherence. A safe and efficient bitterness suppressant must be incorporated in the DPH-loaded OFDMTs
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