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Using NMR Chemical Shift Imaging To Monitor Swelling and Molecular Transport in Drug-Loaded Tablets of Hydrophobically Modified Poly(acrylic acid): Methodology and Effects of Polymer (In)solubility

Knöös, Patrik LU ; Topgaard, Daniel LU ; Wahlgren, Marie LU ; Ulvenlund, Stefan LU and Piculell, Lennart LU (2013) In Langmuir 29(45). p.13898-13908
Abstract
A new technique has been developed using NMR chemical shift imaging (CSI) to monitor water penetration and molecular transport in initially dry polymer tablets that also contain small low-molecular weight compounds to be released from the tablets. Concentration profiles of components contained in the swelling tablets could be extracted via the intensities and chemical shift changes of peaks corresponding to protons of the components. The studied tablets contained hydrophobically modified poly(acrylic acid) (HMPAA) as the polymer component and griseofulvin and ethanol as hydrophobic and hydrophilic, respectively, low-molecular weight model compounds. The water solubility of HMPAA could be altered by titration with NaOH. In the pure acid... (More)
A new technique has been developed using NMR chemical shift imaging (CSI) to monitor water penetration and molecular transport in initially dry polymer tablets that also contain small low-molecular weight compounds to be released from the tablets. Concentration profiles of components contained in the swelling tablets could be extracted via the intensities and chemical shift changes of peaks corresponding to protons of the components. The studied tablets contained hydrophobically modified poly(acrylic acid) (HMPAA) as the polymer component and griseofulvin and ethanol as hydrophobic and hydrophilic, respectively, low-molecular weight model compounds. The water solubility of HMPAA could be altered by titration with NaOH. In the pure acid form, HMPAA tablets only underwent a finite swelling until the maximum water content of the polymer-rich phase, as confirmed by independent phase studies, had been reached. By contrast, after partial neutralization with NaOH, the polyacid became fully miscible with water. The solubility of the polymer affected the water penetration, the polymer release, and the releases of both ethanol and griseofulvin. The detailed NMR CSI concentration profiles obtained highlighted the clear differences in the disintegration/dissolution/release behavior for the two types of tablet and provided insights into their molecular origin. The study illustrates the potential of the NMR CSI technique to give information of importance for the development of pharmaceutical tablets and, more broadly, for the general understanding of any operation that involves the immersion and ultimate disintegration of a dry polymer matrix in a solvent. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Langmuir
volume
29
issue
45
pages
13898 - 13908
publisher
The American Chemical Society (ACS)
external identifiers
  • wos:000327044600027
  • scopus:84887598023
  • pmid:24106807
ISSN
0743-7463
DOI
10.1021/la4024458
language
English
LU publication?
yes
id
59d043bb-5c13-4edd-94bc-4158ba3ca713 (old id 4196721)
date added to LUP
2016-04-01 10:23:53
date last changed
2019-05-14 01:19:15
@article{59d043bb-5c13-4edd-94bc-4158ba3ca713,
  abstract     = {A new technique has been developed using NMR chemical shift imaging (CSI) to monitor water penetration and molecular transport in initially dry polymer tablets that also contain small low-molecular weight compounds to be released from the tablets. Concentration profiles of components contained in the swelling tablets could be extracted via the intensities and chemical shift changes of peaks corresponding to protons of the components. The studied tablets contained hydrophobically modified poly(acrylic acid) (HMPAA) as the polymer component and griseofulvin and ethanol as hydrophobic and hydrophilic, respectively, low-molecular weight model compounds. The water solubility of HMPAA could be altered by titration with NaOH. In the pure acid form, HMPAA tablets only underwent a finite swelling until the maximum water content of the polymer-rich phase, as confirmed by independent phase studies, had been reached. By contrast, after partial neutralization with NaOH, the polyacid became fully miscible with water. The solubility of the polymer affected the water penetration, the polymer release, and the releases of both ethanol and griseofulvin. The detailed NMR CSI concentration profiles obtained highlighted the clear differences in the disintegration/dissolution/release behavior for the two types of tablet and provided insights into their molecular origin. The study illustrates the potential of the NMR CSI technique to give information of importance for the development of pharmaceutical tablets and, more broadly, for the general understanding of any operation that involves the immersion and ultimate disintegration of a dry polymer matrix in a solvent.},
  author       = {Knöös, Patrik and Topgaard, Daniel and Wahlgren, Marie and Ulvenlund, Stefan and Piculell, Lennart},
  issn         = {0743-7463},
  language     = {eng},
  number       = {45},
  pages        = {13898--13908},
  publisher    = {The American Chemical Society (ACS)},
  series       = {Langmuir},
  title        = {Using NMR Chemical Shift Imaging To Monitor Swelling and Molecular Transport in Drug-Loaded Tablets of Hydrophobically Modified Poly(acrylic acid): Methodology and Effects of Polymer (In)solubility},
  url          = {http://dx.doi.org/10.1021/la4024458},
  doi          = {10.1021/la4024458},
  volume       = {29},
  year         = {2013},
}