期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 78, 期 -, 页码 273-285出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2015.08.001
关键词
Cyclodextrins; Drug-cyclodextrin-polymer interactions; Molecular dynamics simulation; Poorly soluble drugs; Dissolution rate enhancement; Carbamazepine
资金
- Ministry of Education, Science and Technological Development, Republic of Serbia [TR 34007]
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. (C) 2015 Elsevier B.V. All rights reserved.
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