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Comparison of the effects of two drying methods on polymorphism of theophylline

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Standard

Comparison of the effects of two drying methods on polymorphism of theophylline. / Airaksinen, Sari; Karjalainen, Milja; Räsänen, Eetu; Rantanen, Jukka; Yliruusi, Jouko.

I: International Journal of Pharmaceutics, Bind 276, Nr. 1-2, 19.05.2004, s. 129-41.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Harvard

Airaksinen, S, Karjalainen, M, Räsänen, E, Rantanen, J & Yliruusi, J 2004, 'Comparison of the effects of two drying methods on polymorphism of theophylline', International Journal of Pharmaceutics, bind 276, nr. 1-2, s. 129-41. https://doi.org/10.1016/j.ijpharm.2004.02.017

APA

Airaksinen, S., Karjalainen, M., Räsänen, E., Rantanen, J., & Yliruusi, J. (2004). Comparison of the effects of two drying methods on polymorphism of theophylline. International Journal of Pharmaceutics, 276(1-2), 129-41. https://doi.org/10.1016/j.ijpharm.2004.02.017

Vancouver

Airaksinen S, Karjalainen M, Räsänen E, Rantanen J, Yliruusi J. Comparison of the effects of two drying methods on polymorphism of theophylline. International Journal of Pharmaceutics. 2004 maj 19;276(1-2):129-41. https://doi.org/10.1016/j.ijpharm.2004.02.017

Author

Airaksinen, Sari ; Karjalainen, Milja ; Räsänen, Eetu ; Rantanen, Jukka ; Yliruusi, Jouko. / Comparison of the effects of two drying methods on polymorphism of theophylline. I: International Journal of Pharmaceutics. 2004 ; Bind 276, Nr. 1-2. s. 129-41.

Bibtex

@article{2d7a9860382a49d68aa1e4f3cfa0aa79,
title = "Comparison of the effects of two drying methods on polymorphism of theophylline",
abstract = "Processing-induced transformations in drug formulation may induce adverse biopharmaceutical changes in the finished product. During the drying phase of wet granulation, theophylline monohydrate transforms either the stable (form I), or a polymorphic, metastable (form I(*)) form of anhydrous theophylline. We investigated the effect of two drying methods (multichamber microscale fluid bed dryer MMFD) or variable temperature X-ray powder diffractometer (VT-XRPD) on the relative amounts of the different theophylline forms remaining in the dried granules. Granules were analyzed using XRPD and near-infrared spectroscopy. Form I(*) was the predominant form of theophylline after drying at 40-50 degrees C with both drying techniques. Although drying at temperatures over 50 degrees C produced mostly form I, more than 20{\%} of form I(*) remained even at 90 degrees C when drying in MMFD. In these conditions, humidity had little influence on the amount of form I(*) in the granules. In contrast, drying in a VT-XRPD at 60 degrees C produced form I already during the first 15min. Using additional drying methods, including MMFD, during the preformulation stage can be more informative about the possible polymorphic transformations and their underlying mechanisms, such as triboelectrification or recrystallization, in drug ingredients during the manufacturing process.",
keywords = "Chemistry, Pharmaceutical, Polymorphism, Genetic, Theophylline, Vasodilator Agents, X-Ray Diffraction",
author = "Sari Airaksinen and Milja Karjalainen and Eetu R{\"a}s{\"a}nen and Jukka Rantanen and Jouko Yliruusi",
year = "2004",
month = "5",
day = "19",
doi = "10.1016/j.ijpharm.2004.02.017",
language = "English",
volume = "276",
pages = "129--41",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

RIS

TY - JOUR

T1 - Comparison of the effects of two drying methods on polymorphism of theophylline

AU - Airaksinen, Sari

AU - Karjalainen, Milja

AU - Räsänen, Eetu

AU - Rantanen, Jukka

AU - Yliruusi, Jouko

PY - 2004/5/19

Y1 - 2004/5/19

N2 - Processing-induced transformations in drug formulation may induce adverse biopharmaceutical changes in the finished product. During the drying phase of wet granulation, theophylline monohydrate transforms either the stable (form I), or a polymorphic, metastable (form I(*)) form of anhydrous theophylline. We investigated the effect of two drying methods (multichamber microscale fluid bed dryer MMFD) or variable temperature X-ray powder diffractometer (VT-XRPD) on the relative amounts of the different theophylline forms remaining in the dried granules. Granules were analyzed using XRPD and near-infrared spectroscopy. Form I(*) was the predominant form of theophylline after drying at 40-50 degrees C with both drying techniques. Although drying at temperatures over 50 degrees C produced mostly form I, more than 20% of form I(*) remained even at 90 degrees C when drying in MMFD. In these conditions, humidity had little influence on the amount of form I(*) in the granules. In contrast, drying in a VT-XRPD at 60 degrees C produced form I already during the first 15min. Using additional drying methods, including MMFD, during the preformulation stage can be more informative about the possible polymorphic transformations and their underlying mechanisms, such as triboelectrification or recrystallization, in drug ingredients during the manufacturing process.

AB - Processing-induced transformations in drug formulation may induce adverse biopharmaceutical changes in the finished product. During the drying phase of wet granulation, theophylline monohydrate transforms either the stable (form I), or a polymorphic, metastable (form I(*)) form of anhydrous theophylline. We investigated the effect of two drying methods (multichamber microscale fluid bed dryer MMFD) or variable temperature X-ray powder diffractometer (VT-XRPD) on the relative amounts of the different theophylline forms remaining in the dried granules. Granules were analyzed using XRPD and near-infrared spectroscopy. Form I(*) was the predominant form of theophylline after drying at 40-50 degrees C with both drying techniques. Although drying at temperatures over 50 degrees C produced mostly form I, more than 20% of form I(*) remained even at 90 degrees C when drying in MMFD. In these conditions, humidity had little influence on the amount of form I(*) in the granules. In contrast, drying in a VT-XRPD at 60 degrees C produced form I already during the first 15min. Using additional drying methods, including MMFD, during the preformulation stage can be more informative about the possible polymorphic transformations and their underlying mechanisms, such as triboelectrification or recrystallization, in drug ingredients during the manufacturing process.

KW - Chemistry, Pharmaceutical

KW - Polymorphism, Genetic

KW - Theophylline

KW - Vasodilator Agents

KW - X-Ray Diffraction

U2 - 10.1016/j.ijpharm.2004.02.017

DO - 10.1016/j.ijpharm.2004.02.017

M3 - Journal article

C2 - 15113621

VL - 276

SP - 129

EP - 141

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

ID: 140622093