Comparative Evaluation of Pellet Cushioning Agents by Various Imaging Techniques and Dissolution Studies

Abstract

Most of the commercially available pharmaceutical products for oral administration route are marketed in the tablet dosage forms. However, compression of multiparticulate systems is a challenge for the pharmaceutical research and industry, especially if the individual unit is a coated particle, as the release of the active ingredient depends on the integrity of the coating. In the present study, polymer-coated pellets tableted with different types of excipients (powder, granules, pellets) then were investigated by various tablet-destructive (microscopic) and tablet non-destructive (microfocus X-ray; microCT) imaging methods. The information obtained from the independent evaluation of the in vitro drug release profiles model is confirmed by the results obtained by image analysis, regardless of whether X-ray or stereomicroscopic images of the coated, tableted pellets were used for image analysis. The results of this study show that the novel easy-to-use, fast, and non-destructive MFX method is a good alternative to the already used microscopic image analysis methods regarding the characterization of particulates, compressed into tablets.

Review on Starter Pellets: Inert and Functional Cores

“…Several factors must be considered when preparing pellet-containing tablets (modifiedrelease or orodispersible tablets). In addition to the excipient factors (e.g., cushioning agents, excipient-pellet ratio) and tableting parameters (compression force, compression speed), the size of the API-loaded pellet must be appropriate [62][63][64][65][66]. The ideal pellet size for tableting, including the active ingredient and the film coating is considered to be a fraction between 500 and 800 µm (Figure 4).…”

Cushion-coated pellets for tableting without external excipients

“…The main strategy to avoid damage to the starting pellets when they are subjected to tableting and to have a prompt disintegration of the resulting dosage form involves the use of cushioning excipients previously mixed with or, in few cases, layered on the surface of the subunits (Abdul et al, 2010;Chen et al, 2017;Hosseini et al, 2013;Sántha et al, 2021). To reduce the risk of deformation, breakage or fusion of the original pellets, the proposed excipients are typically selected among those having good compaction properties, which would ultimately limit any direct contact of the units with each other while allowing for rapid disintegration of the tablet (Csobán et al, 2016;De Alencar et al, 2017;Gómez-Carracedo et al, 2008;Stange et al, 2013).…”

“…The pellet-to-excipient ratio is an important parameter that influences the mechanical strength, disintegration time, mass and drug content uniformity of the resulting tablets, as well as the integrity of the tableted subunits (Bianchini et al, 1992;Debunne et al, 2004;Pinto et al, 1997aPinto et al, , 1997b. To address the risk of segregation in the mixtures of pellets and cushioning excipients, the use of fillers with a relatively large particle size or of placebo pellets was proposed, meeting most of the desired requirements (Beckert et al, 1998;Elsergany et al, 2020;Lundqvist et al, 1998;Lundqvist and Podczeck, 1997;Sántha et al, 2021;Wagner et al, 1999).…”

Development and Dissolution Study of a β-Galactosidase Containing Drinking Straw

“…Oral administration of the active ingredients is still the most commonly used route of administration [1,2]. Many oral formulations are commercially available not only in various strengths, but also in several dosage forms.…”