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

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.

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Article information: Karolina Dziemidowicz, Felipe L. Lopez, Ben J. Bowles, Andrew J. Edwards, Terry B. Ernest,
Mine Orlu, and Catherine Tuleu. AAPS PharmSciTech. DOI: 10.1208/s12249-018-1104-2

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Materials: The co-processed excipients investigated in this study were Avicel® HFE-102 (FMC biopolymers, Philadelphia, Pennsylvania, USA), CombiLac® and MicroceLac® (Meggle Pharma, Wasserburg, Germany), F-Melt® type C and F-Melt® type M (Fuji Health Science, Toyama, Japan), Ludiflash® (BASF, Lampertheim, Germany), Pharmaburst® 500 (SPI Pharma, Septemes Les Vallons, France) and SmartEx® QD100 (ShinEtsu, Tokyo, Japan). Avicel® PH-102 (FMC biopolymers) was tested as a comparator against the co-processed excipients since it is a highly compressible non-co-processed excipient. All samples were kindly provided by the manufacturers. The individual constituents for each excipient are presented in Table I.