title: Influence of non-water-soluble placebo pellets of different sizes on the characteristics of orally disintegrating tablets manufactured by freeze-drying.
abstract: The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL mannitol or sucrose solution. Particle size distributions were 200-355 µm for Cellets 200 (C200) and 500-710 µm for Cellets 500 (C500). An examination of the tablets revealed that the particles could not be sufficiently embedded in mannitol because of its crystalline nature. The tablet hardness was also inadequate. In contrast, the hardness of sucrose tablets was increased by the addition of Cellets 500. Therefore, the sucrose-based formulation was studied further. Binders [hydroxyethylstarch, sodium alginate, methylcellulose (MC), and gelatin] were added in different concentrations, and tablets were made either with or without placebo pellets. A positive effect of the Cellets on the hardness of tablets was identified. Furthermore, disintegration time could be clearly reduced by Cellets for tablets made from 100 mg/mL sucrose with addition of 10 mg/mL MC, 20 or 40 mg/mL gelatin. The freeze-dried tablet index revealed that the formulations of sucrose with 50 mg/mL hydroxyethylstarch or 20 mg/mL gelatin were particularly advantageous.
authors.affiliation: Division of Pharmaceutics, Freeze Drying Focus Group, University of Erlangen, Cauerstraße 4, Erlangen 91058, Germany.
authors.forename: Ulrike
authors.initials: U
authors.lastname: Stange
authors.affiliation: Niederbronner Pharmacy, Mommsenstraße 22, Nuremberg 90491, Germany.
authors.forename: Christian
authors.initials: C
authors.lastname: Führling
authors.affiliation: Division of Pharmaceutics, Freeze Drying Focus Group, University of Erlangen, Cauerstraße 4, Erlangen 91058, Germany; GILYOS GmbH, Friedrich-Bergius-Ring 15, Würzburg 97076, Germany. Electronic address: info@gilyos.com.
authors.forename: Henning
authors.initials: H
authors.lastname: Gieseler
mesh_terms: D000284:Administration, Oral; D004337:Drug Carriers / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry; D005612:Freeze Drying; D006244:Hardness; D008353:Mannitol / Q000737:chemistry; D010316:Particle Size; D012995:Solubility; D013395:Sucrose / Q000737:chemistry; D013607:Tablets / Q000737:chemistry*; D014867:Water / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D005079:Excipients; D013607:Tablets; D014867:Water; D008353:Mannitol; D013395:Sucrose