The Effect of Food Thickeners on the Bitterness and Dissolution of Amlodipine Besilate Loaded Oral Disintegration Tablets: Assessment of Potential Suitability for Patients with Dysphagia

The purpose of this research was to evaluate the effect of starch- and xanthan gum-based food thickeners on the bitterness and dissolution of amlodipine besilate (AMPB) loaded orally disintegrating tablets (ODT) for potential use with patients with dysphagia. A conventional dissolution test simulating the oral cavity was performed and the taste sensor output of the dissolved sample was evaluated over a 60-seconds period. When four types of AMPB loaded ODTs were tested alone, at 60 seconds, branded product (A) was the least bitter, followed by generic product (B)/generic product (C) which were equal, and finally generic product (D) which was the most bitter. Inhibition of bitterness of AMPB loaded ODTs mixed thickeners, 1.0 (w/v) % xanthan gum-based food thickener solution was significantly strong. The 7.1 (w/v) % and 4.7 (w/v) % starch-based food thickeners solution also effective in bitterness inhibition compared to the 2.4 (w/v) % starch-based food thickener solution. The dissolution test under pH 1.2 in related to 7.1 (w/v) % and 4.7 (w/v) % starch-based thickener contained each of AMPB loaded ODTs were associated with an almost complete amlodipine (AMP) dissolution (almost 90% at 10 minutes), whereas the 1.0, 2.0, 3.0 (w/v) % xanthan gum-based food thickener solution containing AMPB loaded ODTs did not show complete AMP dissolution and there were large variations in the initial dissolution stage. This suggests that a mixture of xanthan gum-based thickener and AMPB loaded ODT poses a risk of reduction of bioavailability. In conclusion, a mixture of 4.7 (w/v) % or 7.1 (w/v) % starch-based thickener with ODTs provides complete release of AMP and superior bitterness inhibition, so is the best choice for administration to patients with dysphagia.

Optimization of Jiawei Qing'e Oral Fast Disintegrating Tablets Based on Response Surface-Central Composite Design

Abstract: Objective To apply the response surface-central composite design to developing and optimizing the oral fastdisintegrating tablets (ODT) formulation for Jiawei Qing’e, a kind of prescription of Chinese herbal medicine.Methods The bitterness of Jiawei Qing’e was masked using Eudragit E-100 by solvent evaporation technique.Response surface approach was applied to investigating the interaction of formulation parameters in optimizing theformulation. The independent variables were Eudragit E-100/drug ratio (X1), amount of disintegrants (X2), and theamount of diluents (X3). The disintegration time (Y1), hardness (Y2), and weight variations of the tablets werecharacterized. Results The models predicted levels of X1= 4.63%, X2= 5.25%, and X3= 34.33%, for the optimalformulation having a hardness of 3.0 kg with the disintegration time of 30 s within experimental region. The observedresponse of Y1= 26.5 s and Y2= 3.14 kg reasonably agreed with the predicted response. Conclusion Responsesurface methodology shows the good predictability and reliability in optimizing the formulation. The optimized ODTof Jiawei Qing’e has acceptable taste, rapid disintegrating ability, and good mechanical strength.