Co-Processed Excipients for Dispersible Tablets—Part 2: Patient Acceptability

Abstract

Palatability and patient acceptability are critical attributes of dispersible tablet formulation. Co-processed excipients could provide improved organoleptic profile due to rational choice of excipients and manufacturing techniques. The aim of this study was to identify the most suitable co-processed excipient to use within directly compressible dispersible tablet formulations. Nine excipients, selected based on successful manufacturability, were investigated in a randomised, preference and acceptability testing in 24 healthy adult volunteers. Excipients were classified in order of preference as follows (from most preferred): SmartEx QD100 > F-Melt Type C > F-Melt Type M > MicroceLac > Ludiflash > CombiLac > Pharmaburst 500 > Avicel HFE-102 > Avicel PH-102. Broad differences were identified in terms of acceptability, with SmartEx QD100 being 'very acceptable', F-Melt Type C, F-Melt Type M and MicroceLac being 'acceptable', Ludiflash, CombiLac and Pharmaburst 500 being 'neutral' and Avicel products being 'very unacceptable' based on ratings using five-point hedonic scales. Organoleptic differences were ascribed to different composition and physical properties of excipients, resulting in dissimilar taste and mouth-feel. Excipients with particle size in water larger than 200-250 μm were considered poorly acceptable, which supports the use of this value as a threshold for maximum particle size of dispersible formulation. The most promising co-processed excipients for directly compressible dispersible tablets were successfully identified.

Scalable flibanserin nanocrystal-based novel sublingual platform for female hypoactive sexual desire disorder: engineering, optimization adopting the desirability function approach and in vivo pharmacokinetic study

“…The lyophilized nanocrystal formula FLB-NC6 was used in the preparation of FLB sublingual tablets. In addition, Pharmaburst ® (85% D-mannitol, <10% silicon dioxide, <10% sorbitol, 5% crospovidone) (Dziemidowicz et al, 2018 ) was used as superdisintegrant. Pharmaburst provides good patient acceptability and produces tablets with mechanical strength that withstand transportation, storage, and removal from the blister, and at the same time rapidly disintegrates in the mouth after administration (Yousef et al, 2005 ; Tayel et al, 2017 ).…”

Comparison of Flow and Compression Properties of Four Lactose-Based Co-Processed Excipients: Cellactose® 80, CombiLac®, MicroceLac® 100, and StarLac®

“…The residue of insoluble material in the mouth is an important parameter in the acceptability of orodispersible formu- The solubility test simulates conditions in the oral cavity, with the purpose of determining the amount of insoluble material after dispersion of a tablet in water, which may impact the palatability of the product upon administration. The residue of insoluble material in the mouth is an important parameter in the acceptability of orodispersible formulations [44,45]. The total undissolved fraction after 24 h an increased contra α-lactose monohydrate quantity in the order ST < MI < CE < CO (Table 2).…”

Surface Modifiers on Composite Particles for Direct Compaction

“…The co-processed excipients are also popular in direct compaction since they have excellent key direct compaction properties that could effectively improve the direct compaction properties of drug powders. According to the modification alone or in combination with other surface modifiers, it can be divided into unitary modifier, binary modifier, and ternary modifier [ 48 , 49 ]. According to different co-processed methods, this review summarizes the one-component modifier and multi-component modifier, and discusses the corresponding modification mechanism.…”