Preparation and characterization of multi-component tablets containing co-amorphous salts : Combining multimodal non-linear optical imaging with established analytical methods

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http://hdl.handle.net/10138/308342

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Ojarinta , R , Saarinen , J , Strachan , C J , Korhonen , O & Laitinen , R 2018 , ' Preparation and characterization of multi-component tablets containing co-amorphous salts : Combining multimodal non-linear optical imaging with established analytical methods ' , European Journal of Pharmaceutics and Biopharmaceutics , vol. 132 , pp. 112-126 . https://doi.org/10.1016/j.ejpb.2018.09.013

Title: Preparation and characterization of multi-component tablets containing co-amorphous salts : Combining multimodal non-linear optical imaging with established analytical methods
Author: Ojarinta, Rami; Saarinen, Jukka; Strachan, Clare J.; Korhonen, Ossi; Laitinen, Riikka
Contributor: University of Helsinki, Division of Pharmaceutical Chemistry and Technology
University of Helsinki, Preclinical Drug Formulation and Analysis group
Date: 2018-11
Language: eng
Number of pages: 15
Belongs to series: European Journal of Pharmaceutics and Biopharmaceutics
ISSN: 0939-6411
URI: http://hdl.handle.net/10138/308342
Abstract: Co-amorphous mixtures have rarely been formulated as oral dosage forms, even though they have been shown to stabilize amorphous drugs in the solid state and enhance the dissolution properties of poorly soluble drugs. In the present study we formulated tablets consisting of either spray dried co-amorphous ibuprofen-arginine or indomethacin-arginine, mannitol or xylitol and polyvinylpyrrolidone K30 (PVP). Experimental design was used for the selection of tablet compositions, and the effect of tablet composition on tablet characteristics was modelled. Multimodal non-linear imaging, including coherent anti-Stokes Raman scattering (CARS) and sum frequency/second harmonic generation (SFG/SHG) microscopies, as well as scanning electron microscopy, X-ray diffractometry and Fourier-transform infrared spectroscopy were utilized to characterize the tablets. The tablets possessed sufficient strength, but modelling produced no clear evidence about the compaction characteristics of co-amorphous salts. However, co-amorphous drug-arginine mixtures resulted in enhanced dissolution behaviour, and the PVP in the tableting mixture stabilized the supersaturation. The co-amorphous mixtures were physically stable during compaction, but the excipient selection affected the long term stability of the ibuprofen-arginine mixture. CARS and SFG/SHG proved feasible techniques in imaging the component distribution on the tablet surfaces, but possibly due to the limited imaging area, recrystallization detected with xray diffraction was not detected.
Subject: Co-amorphous
Amino acid
Tablet
Deformation
Dissolution
Multimodal
non-linear imaging
CARS
SFG
SHG
WATER-SOLUBLE DRUGS
IBUPROFEN-POLYVINYLPYRROLIDONE DISPERSIONS
SOLID-STATE PROPERTIES
HOT-MELT EXTRUSION
AMINO-ACIDS
INDOMETHACIN-ARGININE
COMPACTION PROPERTIES
DISSOLUTION BEHAVIOR
DELIVERY SYSTEMS
MICROCRYSTALLINE CELLULOSE
317 Pharmacy
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