Elucidation of Compression-Induced Surface Crystallization in Amorphous Tablets Using Sum Frequency Generation (SFG) Microscopy

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Mah , P T , Novakovic , D , Saarinen , J , Landeghem , S V , Peltonen , L , Laaksonen , T , Isomäki , A & Strachan , C J 2017 , ' Elucidation of Compression-Induced Surface Crystallization in Amorphous Tablets Using Sum Frequency Generation (SFG) Microscopy ' , Pharmaceutical Research , vol. 34 , no. 5 , pp. 957-970 . https://doi.org/10.1007/s11095-016-2046-6

Title: Elucidation of Compression-Induced Surface Crystallization in Amorphous Tablets Using Sum Frequency Generation (SFG) Microscopy
Author: Mah, Pei T.; Novakovic, Dunja; Saarinen, Jukka; Landeghem, Stijn Van; Peltonen, Leena; Laaksonen, Timo; Isomäki, Antti; Strachan, Clare J.
Contributor organization: Faculty of Pharmacy
Division of Pharmaceutical Chemistry and Technology
Preclinical Drug Formulation and Analysis group
Nanobio Pharmaceutics
Department of Anatomy
Medicum
Clare Strachan / Research Group
Formulation and industrial pharmacy
Drug Research Program
Date: 2017
Language: eng
Number of pages: 14
Belongs to series: Pharmaceutical Research
ISSN: 0724-8741
DOI: https://doi.org/10.1007/s11095-016-2046-6
URI: http://hdl.handle.net/10138/234766
Abstract: Purpose To investigate the effect of compression on the crystallization behavior in amorphous tablets using sum frequency generation (SFG) microscopy imaging and more established analytical methods. Method Tablets containing neat amorphous griseofulvin with/without excipients (silica, hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC) and polyethylene glycol (PEG)) were prepared. They were analyzed upon preparation and storage using attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, scanning electron microscopy (SEM) and SFG microscopy. Results Compression-induced crystallization occurred predominantly on the surface of the neat amorphous griseofulvin tablets, with minimal crystallinity being detected in the core of the tablets. The presence of various types of excipients was not able to mitigate the compression-induced surface crystallization of the amorphous griseofulvin tablets. However, the excipients affected the crystallization rate of amorphous griseofulvin in the core of the tablet upon compression and storage. Conclusion SFG microscopy can be used in combination with ATR-FTIR spectroscopy and SEM to understand the crystallization behaviour of amorphous tablets upon compression and storage. When selecting excipients for amorphous formulations, it is important to consider the effect of the excipients on the physical stability of the amorphous formulations.
Subject: 317 Pharmacy
amorphous
attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy
compression
crystallization
griseofulvin
scanning electron microscopy (SEM)
sum frequency generation (SFG) microscopy
Peer reviewed: Yes
Rights: unspecified
Usage restriction: openAccess
Self-archived version: publishedVersion


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