title: Formulation of paracetamol-containing pastilles with in situ coating technology.
abstract: The focus of this research was to apply the in situ coating technology for producing paracetamol- (PCT-) containing pastilles for paediatric use from a eutectic of two sugar alcohols (sorbitol, xylitol) in one step. This type of melt-technology is more cost-efficient and simpler than other conventional tableting technologies, whereby the formation of the pastilles and their coating occur upon the same fabrication step. We managed to produce pastilles having a softer core and a harder, resistant shell in one cooling step. Adding polyethylene glycol (PEG) 2000 or 6000 to the PCT-containing eutectic, the dissolution rate of PCT could be considerably increased, especially when using PEG 2000, reaching equal dissolution characteristics both under mouth- and gastric-specific conditions. Distributions of the components within the pastilles have been determined by X-ray scattering and Raman spectroscopy. Physico-chemical parameters of the xylitol-sorbitol eutectic and their changes upon adding PCT and PEGs have been determined, and it has been revealed that xylitol and sorbitol form a new entity with a distinguished crystal structure. The significant changes in viscosity were explained and the interaction in the eutectic mixture was investigated using Fourier transform infrared spectroscopy (FT-IR). The uniformity of the physical parameters of the pastilles (including size, weight and drug content) also demonstrates the feasibility of using the cost-efficient and simple one-step eutectic-cooling technology for manufacturing pastilles.
authors: Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary; Richter Gedeon Plc., Budapest, Gyömrői út 19-21, H-1103 Budapest, Hungary.
authors: Gábor
authors: G
authors: Katona
authors: Institute of Biophysics, Biological Research Centre of the Hungarian Academy of Sciences, Temesvári krt. 62, H-6701 Szeged, Hungary.
authors: Balázs
authors: B
authors: Szalontai
authors: Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
authors: Mária
authors: M
authors: Budai-Szűcs
authors: Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
authors: Erzsébet
authors: E
authors: Csányi
authors: Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary. Electronic address: revesz@pharm.u-szeged.hu.
authors: Piroska
authors: P
authors: Szabó-Révész
authors: Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
authors: Orsolya
authors: O
authors: Jójárt-Laczkovich
mesh_terms: D000082:Acetaminophen / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D012995:Solubility; D013402:Sugar Alcohols / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013608:Tablets, Enteric-Coated; D013678:Technology, Pharmaceutical / Q000379:methods*; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D013402:Sugar Alcohols; D013608:Tablets, Enteric-Coated; D000082:Acetaminophen
keywords: Dissolution rate; Eutectic; Paracetamol; Pastillization process; Peg; Raman; Sugar alcohols