Melt-in-Mouth Pellets of Fexofenadine Hydrochloride Using Crospovidone as an Extrusion–Spheronisation Aid

Abstract

Abstract. Microcrystalline cellulose (MCC) is well established as an extrusion spheronisation aid for the preparation of pellets. Crospovidone (Polyplasdone® XL-10) is compared with microcrystalline cellulose for the preparation of melt-in-mouth pellets. Taste-masked fexofenadine hydrochloride was incorporated in the melt-in-mouth formulation. Crospovidone was found to be well suited as extrusion-spheronisation aid for the preparation of melt-in-mouth pellets. The great advantage of crospovidone is, however, the disintegrating properties of the pellets after only a short time of exposure to liquid. Crospovidone was successfully employed as an extrusion-spheronisation aid to produce melt-in-mouth pellets obviating the need of a traditional extrusion-spheronisation aid, MCC. Dual properties of Crospovidone were explored viz. as an extrusion-spheronisation aid and a disintegrant.

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“…Finally, dried pellets were shifted to collect 16/20 mesh fractions and were used for further coating. [14] Coating of pellets with effervescent layer and gas entrapment layer…”

Contrasting the crospovidones functionality as excipients for direct compression

“…The cross-linked structure of crospovidone behaves as a mesh to prevent the loss of water trapped within the internal pores; its mechanism of action resembles the sponge model proposed for microcrystalline cellulose (Jain et al, 2010).…”

“…Polyplasdone crospovidones are considered free-flowing materials and the CI has been reported for Polyplasdone XL as 29% (Fujii et al, 2005), 22% (Quadir, Kolter, 2006) and 33% (Bühler, 2005), while Polyplasdone XL10 was reported to have a CI of 31% (Quadir, Kolter, 2006), 29.9% (Jain et al, 2010) and 40% (Polyplasdone, 2013). These different results have been found in the literature or calculated from published data for bulk and tapped densities and vary because of the different methods used to assess the data or due to changes in the excipient properties between different batches.…”

A Quality by Experimental Design Approach to Assess the Effect of Formulation and Process Variables on the Extrusion and Spheronization of Drug-Loaded Pellets Containing Polyplasdone® XL-10

“…Polyplasdone ® XL-10 has been included as an extrusion aid at 25% w/w of the powder blend with lactose α-monohydrate as the remaining material [11,[15][16][17], at 25% w/w with lactose α-monohydrate and drug as the remaining material [18], or at 10-90% w/w polymer with drug as the remaining material in order to expand the influence of the polymer on the pellet characteristics [19]. It should be noted that lactose can dissolve in the water added during the wet mixing step and this can easily influence the product from extrusion-spheronization processing, including formation of liquid bridges in the wetted mass that contribute to the cohesive nature of the mass and the extrudate and that dry to form solid bridges in the dry pellet.…”

“…Kollidon ® CL-SF, which is reported to have a particle size similar to that of Polyplasdone ® XL-10 and INF-10 [20], failed as an extrusion-spheronization aid, whereas a micronized particle grade, Kollidon ® CL-M, was successful. Jain et al focused on the use of Polyplasdone ® XL-10 as an extrusionspheronization aid in the preparation of fexofenadine hydrochloride pellets at no more than 25% of the pellet content [18]. The authors noted that higher quality pellets could be produced with a smaller median particle diameter or a higher particle size distribution of the powder blend that leads to denser packing of the particles.…”