Physicochemical qualities and ingestibility of high value-added amlodipine besilate formulations

Abstract

Objectives The physicochemical qualities and ingestibility of high value-added amlodipine besilate formulations were evaluated using one brand name and four generic orally disintegrating tablets (formulations A, B, C, D, and E) and a generic orally disintegrating film (formulation F). Methods Pushing out from a press-through package, tablet strength, and hydrophilia were examined for the aforementioned formulations A–E, and sensory characteristics according to the disintegration time, taste, and palatability in healthy subjects were evaluated for formulations A–F. Results The strength required for pushing out from a press-through package for formulations A, B, C, D, and E was approximately 20 N, indicating ease of opening for most users. Moreover, hardness and friability of formulations A, B, C, D, and E were more than 0.03 kg/mg and less than 1%, respectively. Thus, all formulations had sufficient tablet strength to endure fall impact in the automatic packing machine and vibration when carrying them from one place to another. The wetting time of formulation E (9 s) was significantly shorter than that of formulations A (27 s), B (34 s), C (28 s), and D (29 s), indicating that with the exception of hydrophilia, the physicochemical qualities of the five aforementioned formulations of orally disintegrating tablets were equivalent. The disintegration time of formulations E (15 s) and F (15 s) in the oral cavity was significantly shorter than that of formulations A (23 s), B (26 s), C (25 s), and D (22 s). Moreover, more than 50% of subjects reported strong or weak bitterness for formulations B, C, D, E, and F. Finally, more than 80% of subjects described formulations A, E, and F as easy to take, indicating good palatability. Conclusions This study provides useful information for selecting high value-added amlodipine besilate formulations for individualized treatments.