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Vojinović T, Medarević D, Vranić E, et al. Development of ternary solid dispersions with hydrophilic polymer and surface adsorbent for improving dissolution rate of carbamazepine. Saudi Pharm J. 2018;26(5):725-732doi: 10.1016/j.jsps.2018.02.017.
Vojinović, T., Medarević, D., Vranić, E., Potpara, Z., Krstić, M., Djuriš, J., & Ibrić, S. (2018). Development of ternary solid dispersions with hydrophilic polymer and surface adsorbent for improving dissolution rate of carbamazepine. Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society, 26(5), 725-732. https://doi.org/10.1016/j.jsps.2018.02.017
Vojinović, Tanja, et al. "Development of ternary solid dispersions with hydrophilic polymer and surface adsorbent for improving dissolution rate of carbamazepine." Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society vol. 26,5 (2018): 725-732. doi: https://doi.org/10.1016/j.jsps.2018.02.017
Vojinović T, Medarević D, Vranić E, Potpara Z, Krstić M, Djuriš J, Ibrić S. Development of ternary solid dispersions with hydrophilic polymer and surface adsorbent for improving dissolution rate of carbamazepine. Saudi Pharm J. 2018 Jul;26(5):725-732. doi: 10.1016/j.jsps.2018.02.017. Epub 2018 Feb 07. PMID: 29991917; PMCID: PMC6035321.
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Saudi Pharm J. 2018 Jul;26(5):725-732. doi: 10.1016/j.jsps.2018.02.017. Epub 2018 Feb 07.

Development of ternary solid dispersions with hydrophilic polymer and surface adsorbent for improving dissolution rate of carbamazepine.

Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society

Tanja Vojinović, Djordje Medarević, Edina Vranić, Zorica Potpara, Marko Krstić, Jelena Djuriš, Svetlana Ibrić

Affiliations

  1. Department of Pharmacy, Faculty of Medicine, University of Montenegro, Ljubljanska bb, Podgorica, Montenegro.
  2. Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, Belgrade, Serbia.
  3. Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Sarajevo, Zmaja od Bosne 8, Sarajevo, Bosnia and Herzegovina.

PMID: 29991917 PMCID: PMC6035321 DOI: 10.1016/j.jsps.2018.02.017

Abstract

In this study solid dispersions of carbamazepine in the hydrophilic Kollidon® VA64 polymer, adsorbed onto Neusilin® UFL2 adsorption carrier have been employed to improve carbamazepine dissolution rate. In order to evaluate effects of changing in the proportions of all solid dispersion components on carbamazepine dissolution rate, D-optimal mixture experimental design was used in the formulation development. From all prepared solid dispersion formulations, significantly faster carbamazepine dissolution was observed compared to pure drug. Ternary solid dispersions containing carbamazepine, Kollidon® VA64 and Neusilin® UFL2 showed superior dissolution performances over binary ones, containing only carbamazepine and Neusilin® UFL2. Proportion of Kollidon® VA64 showed the most profound effect on the amount of carbamazepine dissolved after 10 and 30 min, whereby these parameters increase upon increasing in Kollidon® VA64 concentrations up to the middle values in the studied range of Kollidon® VA64 concentrations. Physicochemical characterization of the selected samples using differential scanning calorimetry, FT-IR spectroscopy, powder X-ray diffraction and polarizing light microscopy showed polymorphic transition of carbamazepine from more thermodynamically stable monoclinic form (form III) to less thermodynamically stable triclinic form (form I) in the case of ternary, but not of binary solid dispersion formulations. This polymorphic transition can be one of the factors responsible for improving of carbamazepine dissolution rate from studied solid dispersions. Ternary solid dispersions prepared with Kollidon® VA64 hydrophilic polymer and Neusilin® UFL2 adsorption carrier resulted in significantly improvement of carbamazepine dissolution rate, but formation of metastable polymorphic form of carbamazepine requires particular care to be taken in ensuring product long term stability.

Keywords: D-optimal mixture experimental design; Polymorphic conversion; Polymorphism; Poorly soluble drugs; Solid dispersions; Surface adsorbent

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