Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures

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Standard

Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures. / Priemel, Petra A; Laitinen, Riikka; Barthold, Sarah; Grohganz, Holger; Lehto, Vesa-Pekka; Rades, Thomas; Strachan, Clare J.

In: International Journal of Pharmaceutics, Vol. 456, No. 2, 18.11.2013, p. 301-6.

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

Harvard

Priemel, PA, Laitinen, R, Barthold, S, Grohganz, H, Lehto, V-P, Rades, T & Strachan, CJ 2013, 'Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures', International Journal of Pharmaceutics, vol. 456, no. 2, pp. 301-6. https://doi.org/10.1016/j.ijpharm.2013.08.046

APA

Priemel, P. A., Laitinen, R., Barthold, S., Grohganz, H., Lehto, V-P., Rades, T., & Strachan, C. J. (2013). Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures. International Journal of Pharmaceutics, 456(2), 301-6. https://doi.org/10.1016/j.ijpharm.2013.08.046

Vancouver

Priemel PA, Laitinen R, Barthold S, Grohganz H, Lehto V-P, Rades T et al. Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures. International Journal of Pharmaceutics. 2013 Nov 18;456(2):301-6. https://doi.org/10.1016/j.ijpharm.2013.08.046

Author

Priemel, Petra A ; Laitinen, Riikka ; Barthold, Sarah ; Grohganz, Holger ; Lehto, Vesa-Pekka ; Rades, Thomas ; Strachan, Clare J. / Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures. In: International Journal of Pharmaceutics. 2013 ; Vol. 456, No. 2. pp. 301-6.

Bibtex

@article{b7349069ac43465f904a3ab6c004d6ea,
title = "Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures",
abstract = "Surface coverage may affect the crystallisation behaviour of amorphous materials. This study investigates crystallisation inhibition in powder mixtures of amorphous drug and pharmaceutical excipients. Pure amorphous indomethacin (IMC) powder and physical mixtures thereof with Eudragit({\textregistered}) E or Soluplus({\textregistered}) in 3:1, 1:1 and 1:3 (w/w) ratios were stored at 30°C and 23 or 42% RH. Samples were analysed during storage by X-ray powder diffraction, thermogravimetric analysis, differential scanning calorimetry, and scanning electron microscopy (SEM). IMC Eudragit({\textregistered}) mixtures showed higher physical stability than pure IMC whereas IMC Soluplus({\textregistered}) mixtures did not. Water uptake was higher for mixtures containing Soluplus({\textregistered}) than for amorphous IMC or IMC Eudragit({\textregistered}) mixtures. However, the Tg of amorphous IMC was unaffected by the presence (and nature) of polymer. SEM revealed that Eudragit({\textregistered}) particles aggregated on the surface of IMC particles, whereas Soluplus({\textregistered}) particles did not. The drug particles developed multiple crystallites at their surface with subsequent crystal growth. The intimate contact between the surface agglomerated Eudragit({\textregistered}) particles and drug is believed to inhibit crystallisation through reduced IMC surface molecular mobility. Polymer particles may also mechanically hinder crystal growth outwards from the surface. This work highlights the importance of microparticulate surface coverage of amorphous drug particles on their stability.",
author = "Priemel, {Petra A} and Riikka Laitinen and Sarah Barthold and Holger Grohganz and Vesa-Pekka Lehto and Thomas Rades and Strachan, {Clare J}",
note = "Copyright {\textcopyright} 2013 Elsevier B.V. All rights reserved.",
year = "2013",
month = nov,
day = "18",
doi = "10.1016/j.ijpharm.2013.08.046",
language = "English",
volume = "456",
pages = "301--6",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "2",

}

RIS

TY - JOUR

T1 - Inhibition of surface crystallisation of amorphous indomethacin particles in physical drug-polymer mixtures

AU - Priemel, Petra A

AU - Laitinen, Riikka

AU - Barthold, Sarah

AU - Grohganz, Holger

AU - Lehto, Vesa-Pekka

AU - Rades, Thomas

AU - Strachan, Clare J

N1 - Copyright © 2013 Elsevier B.V. All rights reserved.

PY - 2013/11/18

Y1 - 2013/11/18

N2 - Surface coverage may affect the crystallisation behaviour of amorphous materials. This study investigates crystallisation inhibition in powder mixtures of amorphous drug and pharmaceutical excipients. Pure amorphous indomethacin (IMC) powder and physical mixtures thereof with Eudragit(®) E or Soluplus(®) in 3:1, 1:1 and 1:3 (w/w) ratios were stored at 30°C and 23 or 42% RH. Samples were analysed during storage by X-ray powder diffraction, thermogravimetric analysis, differential scanning calorimetry, and scanning electron microscopy (SEM). IMC Eudragit(®) mixtures showed higher physical stability than pure IMC whereas IMC Soluplus(®) mixtures did not. Water uptake was higher for mixtures containing Soluplus(®) than for amorphous IMC or IMC Eudragit(®) mixtures. However, the Tg of amorphous IMC was unaffected by the presence (and nature) of polymer. SEM revealed that Eudragit(®) particles aggregated on the surface of IMC particles, whereas Soluplus(®) particles did not. The drug particles developed multiple crystallites at their surface with subsequent crystal growth. The intimate contact between the surface agglomerated Eudragit(®) particles and drug is believed to inhibit crystallisation through reduced IMC surface molecular mobility. Polymer particles may also mechanically hinder crystal growth outwards from the surface. This work highlights the importance of microparticulate surface coverage of amorphous drug particles on their stability.

AB - Surface coverage may affect the crystallisation behaviour of amorphous materials. This study investigates crystallisation inhibition in powder mixtures of amorphous drug and pharmaceutical excipients. Pure amorphous indomethacin (IMC) powder and physical mixtures thereof with Eudragit(®) E or Soluplus(®) in 3:1, 1:1 and 1:3 (w/w) ratios were stored at 30°C and 23 or 42% RH. Samples were analysed during storage by X-ray powder diffraction, thermogravimetric analysis, differential scanning calorimetry, and scanning electron microscopy (SEM). IMC Eudragit(®) mixtures showed higher physical stability than pure IMC whereas IMC Soluplus(®) mixtures did not. Water uptake was higher for mixtures containing Soluplus(®) than for amorphous IMC or IMC Eudragit(®) mixtures. However, the Tg of amorphous IMC was unaffected by the presence (and nature) of polymer. SEM revealed that Eudragit(®) particles aggregated on the surface of IMC particles, whereas Soluplus(®) particles did not. The drug particles developed multiple crystallites at their surface with subsequent crystal growth. The intimate contact between the surface agglomerated Eudragit(®) particles and drug is believed to inhibit crystallisation through reduced IMC surface molecular mobility. Polymer particles may also mechanically hinder crystal growth outwards from the surface. This work highlights the importance of microparticulate surface coverage of amorphous drug particles on their stability.

U2 - 10.1016/j.ijpharm.2013.08.046

DO - 10.1016/j.ijpharm.2013.08.046

M3 - Journal article

C2 - 24012867

VL - 456

SP - 301

EP - 306

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 2

ER -

ID: 56125239