Effects of excipients on hydrate formation in wet masses containing theophylline

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Effects of excipients on hydrate formation in wet masses containing theophylline. / Airaksinen, Sari; Luukkonen, Pirjo; Jørgensen, Anna; Karjalainen, Milja; Rantanen, Jukka; Yliruusi, Jouko.

In: Journal of Pharmaceutical Sciences, Vol. 92, No. 3, 03.2003, p. 516-28.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Airaksinen, S, Luukkonen, P, Jørgensen, A, Karjalainen, M, Rantanen, J & Yliruusi, J 2003, 'Effects of excipients on hydrate formation in wet masses containing theophylline', Journal of Pharmaceutical Sciences, vol. 92, no. 3, pp. 516-28. https://doi.org/10.1002/jps.10328

APA

Airaksinen, S., Luukkonen, P., Jørgensen, A., Karjalainen, M., Rantanen, J., & Yliruusi, J. (2003). Effects of excipients on hydrate formation in wet masses containing theophylline. Journal of Pharmaceutical Sciences, 92(3), 516-28. https://doi.org/10.1002/jps.10328

Vancouver

Airaksinen S, Luukkonen P, Jørgensen A, Karjalainen M, Rantanen J, Yliruusi J. Effects of excipients on hydrate formation in wet masses containing theophylline. Journal of Pharmaceutical Sciences. 2003 Mar;92(3):516-28. https://doi.org/10.1002/jps.10328

Author

Airaksinen, Sari ; Luukkonen, Pirjo ; Jørgensen, Anna ; Karjalainen, Milja ; Rantanen, Jukka ; Yliruusi, Jouko. / Effects of excipients on hydrate formation in wet masses containing theophylline. In: Journal of Pharmaceutical Sciences. 2003 ; Vol. 92, No. 3. pp. 516-28.

Bibtex

@article{09050cd8ebf1488dbfdad8bcbffd5696,
title = "Effects of excipients on hydrate formation in wet masses containing theophylline",
abstract = "Transformations between solid phases in dosage forms can lead to instability in drug release. Thus, it is important to understand mechanisms and kinetics of phase transformations and factors that may influence them. During wet granulation theophylline shows pseudopolymorphic changes that may alter its dissolution rate. The aim of this study was to investigate whether excipients, such as alpha-lactose monohydrate or the highly water absorbing silicified microcrystalline cellulose (SMCC) can influence the hydrate formation of theophylline. In particular, the aim was to study if SMCC offers protection against the formation of theophylline monohydrate relative to alpha-lactose monohydrate in wet masses after an overnight equilibration and the stability of final granules during controlled storage. In addition, the aim was to study the use of spectroscopic methods to identify hydrate formation in the formulations containing excipients. Off-line evaluation of materials was performed using X-ray powder diffractometry, near infrared and Raman spectroscopy. alpha-Lactose monohydrate with minimal water absorbing potential was not able to prevent but enhanced hydrate formation of theophylline. Even though SMCC is able to take large amounts of water into its internal structure, it was able to inhibit the formation of theophylline monohydrate only at low moisture contents, not at the amounts of water needed to form granules. Both the spectroscopic methods used could identify the hydrate formation even though there were excipients in the formulation.",
keywords = "Absorption, Chemistry, Pharmaceutical, Excipients, Lactose, Theophylline, Water, Wettability",
author = "Sari Airaksinen and Pirjo Luukkonen and Anna J{\o}rgensen and Milja Karjalainen and Jukka Rantanen and Jouko Yliruusi",
note = "Copyright 2003 Wiley-Liss, Inc. and the American Pharmaceutical Association",
year = "2003",
month = mar,
doi = "10.1002/jps.10328",
language = "English",
volume = "92",
pages = "516--28",
journal = "Journal of Pharmaceutical Sciences",
issn = "0022-3549",
publisher = "Elsevier",
number = "3",

}

RIS

TY - JOUR

T1 - Effects of excipients on hydrate formation in wet masses containing theophylline

AU - Airaksinen, Sari

AU - Luukkonen, Pirjo

AU - Jørgensen, Anna

AU - Karjalainen, Milja

AU - Rantanen, Jukka

AU - Yliruusi, Jouko

N1 - Copyright 2003 Wiley-Liss, Inc. and the American Pharmaceutical Association

PY - 2003/3

Y1 - 2003/3

N2 - Transformations between solid phases in dosage forms can lead to instability in drug release. Thus, it is important to understand mechanisms and kinetics of phase transformations and factors that may influence them. During wet granulation theophylline shows pseudopolymorphic changes that may alter its dissolution rate. The aim of this study was to investigate whether excipients, such as alpha-lactose monohydrate or the highly water absorbing silicified microcrystalline cellulose (SMCC) can influence the hydrate formation of theophylline. In particular, the aim was to study if SMCC offers protection against the formation of theophylline monohydrate relative to alpha-lactose monohydrate in wet masses after an overnight equilibration and the stability of final granules during controlled storage. In addition, the aim was to study the use of spectroscopic methods to identify hydrate formation in the formulations containing excipients. Off-line evaluation of materials was performed using X-ray powder diffractometry, near infrared and Raman spectroscopy. alpha-Lactose monohydrate with minimal water absorbing potential was not able to prevent but enhanced hydrate formation of theophylline. Even though SMCC is able to take large amounts of water into its internal structure, it was able to inhibit the formation of theophylline monohydrate only at low moisture contents, not at the amounts of water needed to form granules. Both the spectroscopic methods used could identify the hydrate formation even though there were excipients in the formulation.

AB - Transformations between solid phases in dosage forms can lead to instability in drug release. Thus, it is important to understand mechanisms and kinetics of phase transformations and factors that may influence them. During wet granulation theophylline shows pseudopolymorphic changes that may alter its dissolution rate. The aim of this study was to investigate whether excipients, such as alpha-lactose monohydrate or the highly water absorbing silicified microcrystalline cellulose (SMCC) can influence the hydrate formation of theophylline. In particular, the aim was to study if SMCC offers protection against the formation of theophylline monohydrate relative to alpha-lactose monohydrate in wet masses after an overnight equilibration and the stability of final granules during controlled storage. In addition, the aim was to study the use of spectroscopic methods to identify hydrate formation in the formulations containing excipients. Off-line evaluation of materials was performed using X-ray powder diffractometry, near infrared and Raman spectroscopy. alpha-Lactose monohydrate with minimal water absorbing potential was not able to prevent but enhanced hydrate formation of theophylline. Even though SMCC is able to take large amounts of water into its internal structure, it was able to inhibit the formation of theophylline monohydrate only at low moisture contents, not at the amounts of water needed to form granules. Both the spectroscopic methods used could identify the hydrate formation even though there were excipients in the formulation.

KW - Absorption

KW - Chemistry, Pharmaceutical

KW - Excipients

KW - Lactose

KW - Theophylline

KW - Water

KW - Wettability

U2 - 10.1002/jps.10328

DO - 10.1002/jps.10328

M3 - Journal article

C2 - 12587113

VL - 92

SP - 516

EP - 528

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

SN - 0022-3549

IS - 3

ER -

ID: 140622166