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Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-beta-cyclodextrin

Authorized Users Only
2015
Authors
Medarević, Đorđe
Kachrimanis, Kyriakos
Đurić, Zorica
Ibrić, Svetlana
Article (Published version)
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Abstract
In this study binary carbamazepine-hydroxypropyl-beta-cyclodextrin, as well as ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer systems were used to improve dissolution rate of carbamazepine. It has been shown that addition of hydrophilic polymers (Soluplus (R) and two types of hydroxypropyl methylcellulose-Metolose (R) 90SH-100 and Metolose (R) 65SH-1500) significantly increased solubilization capacity of hydroxypropyl-B-cyclodextrin for carbamazepine. Evaluation of carbamaze pine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer interactions using molecular modeling techniques showed interactions between carbamazepine, which dissociates from inclusion complexes and hydroxypropyl methylcellulose that can prevent crystallization of dissolved carbamazepine. These results can contribute to better understanding of drug-cyclodextrin-hydrophilic polymer interactions which are still not well understood. After evaluation of carbamazepine solubilization with hydroxyp...ropyl-beta-cyclodextrin and hydrophilic polymers, both binary carbamazepine-hydroxypropyl-beta-cyclodextrin and ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer systems were prepared by spray drying. The results of solid state characterization methods showed amorphous nature of carbamazepine in all spray dried systems, which together with the results of molecular modeling techniques indicates inclusion complex formation. Carbamazepine dissolution rate was significantly improved from spray dried formulations compared to pure drug. Binary carbamazepine-hydroxypropyl-beta-cyclodextrin and ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-Soluplus (R) systems exhibited the fastest carbamazepine release, wherein the entire amount of carbamazepine was released during first 5 min.

Source:
European Journal of Pharmaceutical Sciences, 2015, 78, 273-285
Publisher:
  • Elsevier Science BV, Amsterdam
Projects:
  • Advanced technologies for controlled release from solid drug delivery systems (RS-34007)

DOI: 10.1016/j.ejps.2015.08.001

ISSN: 0928-0987

PubMed: 26255049

WoS: 000361264000029

Scopus: 2-s2.0-84939797808
[ Google Scholar ]
34
34
URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/2321
Collections
  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy
TY  - JOUR
AU  - Medarević, Đorđe
AU  - Kachrimanis, Kyriakos
AU  - Đurić, Zorica
AU  - Ibrić, Svetlana
PY  - 2015
UR  - http://farfar.pharmacy.bg.ac.rs/handle/123456789/2321
AB  - In this study binary carbamazepine-hydroxypropyl-beta-cyclodextrin, as well as ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer systems were used to improve dissolution rate of carbamazepine. It has been shown that addition of hydrophilic polymers (Soluplus (R) and two types of hydroxypropyl methylcellulose-Metolose (R) 90SH-100 and Metolose (R) 65SH-1500) significantly increased solubilization capacity of hydroxypropyl-B-cyclodextrin for carbamazepine. Evaluation of carbamaze pine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer interactions using molecular modeling techniques showed interactions between carbamazepine, which dissociates from inclusion complexes and hydroxypropyl methylcellulose that can prevent crystallization of dissolved carbamazepine. These results can contribute to better understanding of drug-cyclodextrin-hydrophilic polymer interactions which are still not well understood. After evaluation of carbamazepine solubilization with hydroxypropyl-beta-cyclodextrin and hydrophilic polymers, both binary carbamazepine-hydroxypropyl-beta-cyclodextrin and ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer systems were prepared by spray drying. The results of solid state characterization methods showed amorphous nature of carbamazepine in all spray dried systems, which together with the results of molecular modeling techniques indicates inclusion complex formation. Carbamazepine dissolution rate was significantly improved from spray dried formulations compared to pure drug. Binary carbamazepine-hydroxypropyl-beta-cyclodextrin and ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-Soluplus (R) systems exhibited the fastest carbamazepine release, wherein the entire amount of carbamazepine was released during first 5 min.
PB  - Elsevier Science BV, Amsterdam
T2  - European Journal of Pharmaceutical Sciences
T1  - Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-beta-cyclodextrin
VL  - 78
SP  - 273
EP  - 285
DO  - 10.1016/j.ejps.2015.08.001
ER  - 
@article{
author = "Medarević, Đorđe and Kachrimanis, Kyriakos and Đurić, Zorica and Ibrić, Svetlana",
year = "2015",
url = "http://farfar.pharmacy.bg.ac.rs/handle/123456789/2321",
abstract = "In this study binary carbamazepine-hydroxypropyl-beta-cyclodextrin, as well as ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer systems were used to improve dissolution rate of carbamazepine. It has been shown that addition of hydrophilic polymers (Soluplus (R) and two types of hydroxypropyl methylcellulose-Metolose (R) 90SH-100 and Metolose (R) 65SH-1500) significantly increased solubilization capacity of hydroxypropyl-B-cyclodextrin for carbamazepine. Evaluation of carbamaze pine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer interactions using molecular modeling techniques showed interactions between carbamazepine, which dissociates from inclusion complexes and hydroxypropyl methylcellulose that can prevent crystallization of dissolved carbamazepine. These results can contribute to better understanding of drug-cyclodextrin-hydrophilic polymer interactions which are still not well understood. After evaluation of carbamazepine solubilization with hydroxypropyl-beta-cyclodextrin and hydrophilic polymers, both binary carbamazepine-hydroxypropyl-beta-cyclodextrin and ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-hydrophilic polymer systems were prepared by spray drying. The results of solid state characterization methods showed amorphous nature of carbamazepine in all spray dried systems, which together with the results of molecular modeling techniques indicates inclusion complex formation. Carbamazepine dissolution rate was significantly improved from spray dried formulations compared to pure drug. Binary carbamazepine-hydroxypropyl-beta-cyclodextrin and ternary carbamazepine-hydroxypropyl-beta-cyclodextrin-Soluplus (R) systems exhibited the fastest carbamazepine release, wherein the entire amount of carbamazepine was released during first 5 min.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "European Journal of Pharmaceutical Sciences",
title = "Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-beta-cyclodextrin",
volume = "78",
pages = "273-285",
doi = "10.1016/j.ejps.2015.08.001"
}
Medarević Đ, Kachrimanis K, Đurić Z, Ibrić S. Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-beta-cyclodextrin. European Journal of Pharmaceutical Sciences. 2015;78:273-285
Medarević, Đ., Kachrimanis, K., Đurić, Z.,& Ibrić, S. (2015). Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-beta-cyclodextrin.
European Journal of Pharmaceutical SciencesElsevier Science BV, Amsterdam., 78, 273-285.
https://doi.org/10.1016/j.ejps.2015.08.001
Medarević Đorđe, Kachrimanis Kyriakos, Đurić Zorica, Ibrić Svetlana, "Influence of hydrophilic polymers on the complexation of carbamazepine with hydroxypropyl-beta-cyclodextrin" 78 (2015):273-285,
https://doi.org/10.1016/j.ejps.2015.08.001 .

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