Investigation of solid phase composition on tablet surfaces by grazing incidence X-ray diffraction

Vishal Shamji Koradia; Mikko Tenho; Heidi Lopez de Diego; Michiel  Ringkjøbing-Elma; Jørn Sonnergaard; Jamo Salonen; Vesa-Pekka Lehto; Jukka Rantanen

doi:10.1007/s11095-011-0520-8

Investigation of solid phase composition on tablet surfaces by grazing incidence X-ray diffraction

Vishal Shamji Koradia, Mikko Tenho, Heidi Lopez de Diego, Michiel Ringkjøbing-Elma, Jørn Sonnergaard, Jamo Salonen, Vesa-Pekka Lehto, Jukka Rantanen

9 Citationer (Scopus)

Abstract

Purpose: To investigate solid state transformations of drug substances during compaction using grazing incidence X-ray diffraction (GIXD). Methods: The solid forms of three model drugs-theophylline (TP), nitrofurantoin (NF) and amlodipine besylate (AMB)-were compacted at different pressures (from 100 to 1000 MPa); prepared tablets were measured using GIXD. After the initial measurements of freshly compacted tablets, tablets were subjected to suitable recrystallization treatment, and analogous measurements were performed. Results: Solid forms of TP, NF and AMB showed partial amorphization as well as crystal disordering during compaction; the extent of these effects generally increased as a function of pressure. The changes were most pronounced at the outer surface region. The different solid forms showed difference in the formation of amorphicity/crystal disordering. Dehydration due to compaction was observed for the TP monohydrate, whereas hydrates of NF and AMB were stable towards dehydration. Conclusions: With GIXD measurements, it was possible to probe the solid form composition at the different depths of the tablet surfaces and to obtain depth-dependent information on the compaction-induced amorphization, crystal disordering and dehydration.

Originalsprog	Engelsk
Tidsskrift	Pharmaceutical Research
Vol/bind	29
Udgave nummer	1
Sider (fra-til)	134-144
ISSN	0724-8741
DOI	https://doi.org/10.1007/s11095-011-0520-8
Status	Udgivet - jan. 2012

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10.1007/s11095-011-0520-8

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title = "Investigation of solid phase composition on tablet surfaces by grazing incidence X-ray diffraction",

abstract = "Purpose: To investigate solid state transformations of drug substances during compaction using grazing incidence X-ray diffraction (GIXD). Methods: The solid forms of three model drugs-theophylline (TP), nitrofurantoin (NF) and amlodipine besylate (AMB)-were compacted at different pressures (from 100 to 1000 MPa); prepared tablets were measured using GIXD. After the initial measurements of freshly compacted tablets, tablets were subjected to suitable recrystallization treatment, and analogous measurements were performed. Results: Solid forms of TP, NF and AMB showed partial amorphization as well as crystal disordering during compaction; the extent of these effects generally increased as a function of pressure. The changes were most pronounced at the outer surface region. The different solid forms showed difference in the formation of amorphicity/crystal disordering. Dehydration due to compaction was observed for the TP monohydrate, whereas hydrates of NF and AMB were stable towards dehydration. Conclusions: With GIXD measurements, it was possible to probe the solid form composition at the different depths of the tablet surfaces and to obtain depth-dependent information on the compaction-induced amorphization, crystal disordering and dehydration.",

keywords = "Former Faculty of Pharmaceutical Sciences",

author = "Koradia, {Vishal Shamji} and Mikko Tenho and Diego, {Heidi Lopez de} and Michiel Ringkj{\o}bing-Elma and J{\o}rn Sonnergaard and Jamo Salonen and Vesa-Pekka Lehto and Jukka Rantanen",

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doi = "10.1007/s11095-011-0520-8",

language = "English",

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T1 - Investigation of solid phase composition on tablet surfaces by grazing incidence X-ray diffraction

AU - Koradia, Vishal Shamji

AU - Tenho, Mikko

AU - Diego, Heidi Lopez de

AU - Ringkjøbing-Elma, Michiel

AU - Sonnergaard, Jørn

AU - Salonen, Jamo

AU - Lehto, Vesa-Pekka

AU - Rantanen, Jukka

PY - 2012/1

Y1 - 2012/1

N2 - Purpose: To investigate solid state transformations of drug substances during compaction using grazing incidence X-ray diffraction (GIXD). Methods: The solid forms of three model drugs-theophylline (TP), nitrofurantoin (NF) and amlodipine besylate (AMB)-were compacted at different pressures (from 100 to 1000 MPa); prepared tablets were measured using GIXD. After the initial measurements of freshly compacted tablets, tablets were subjected to suitable recrystallization treatment, and analogous measurements were performed. Results: Solid forms of TP, NF and AMB showed partial amorphization as well as crystal disordering during compaction; the extent of these effects generally increased as a function of pressure. The changes were most pronounced at the outer surface region. The different solid forms showed difference in the formation of amorphicity/crystal disordering. Dehydration due to compaction was observed for the TP monohydrate, whereas hydrates of NF and AMB were stable towards dehydration. Conclusions: With GIXD measurements, it was possible to probe the solid form composition at the different depths of the tablet surfaces and to obtain depth-dependent information on the compaction-induced amorphization, crystal disordering and dehydration.

AB - Purpose: To investigate solid state transformations of drug substances during compaction using grazing incidence X-ray diffraction (GIXD). Methods: The solid forms of three model drugs-theophylline (TP), nitrofurantoin (NF) and amlodipine besylate (AMB)-were compacted at different pressures (from 100 to 1000 MPa); prepared tablets were measured using GIXD. After the initial measurements of freshly compacted tablets, tablets were subjected to suitable recrystallization treatment, and analogous measurements were performed. Results: Solid forms of TP, NF and AMB showed partial amorphization as well as crystal disordering during compaction; the extent of these effects generally increased as a function of pressure. The changes were most pronounced at the outer surface region. The different solid forms showed difference in the formation of amorphicity/crystal disordering. Dehydration due to compaction was observed for the TP monohydrate, whereas hydrates of NF and AMB were stable towards dehydration. Conclusions: With GIXD measurements, it was possible to probe the solid form composition at the different depths of the tablet surfaces and to obtain depth-dependent information on the compaction-induced amorphization, crystal disordering and dehydration.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1007/s11095-011-0520-8

DO - 10.1007/s11095-011-0520-8

M3 - Journal article

C2 - 21744172

SN - 0724-8741

VL - 29

SP - 134

EP - 144

JO - Pharmaceutical Research

JF - Pharmaceutical Research

IS - 1

ER -

Investigation of solid phase composition on tablet surfaces by grazing incidence X-ray diffraction

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