Formulation and characterization of amiodarone-methyl-beta-cyclodextrin inclusion complexes: A molecular modelling perspective.

Autor: Rubim AM; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria - UFSM, Av. Roraima 1000, 97105-900, Santa Maria, RS, Brazil; Laboratório de Controle de Qualidade de Medicamentos, Universidade Franciscana - UFN, Andradas 1614, 97010-032, Santa Maria, RS, Brazil. Electronic address: alexandre.rubim01@gmail.com., Rubenick JB; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria - UFSM, Av. Roraima 1000, 97105-900, Santa Maria, RS, Brazil. Electronic address: jaquerubenick2@gmail.com., Vendrame LO; Laboratório de Materiais Magnéticos Nanoestruturados, Programa de Pós-Graduação em Nanociências, Universidade Franciscana - UFN, Andradas 1614, 97010-032, Santa Maria, RS, Brazil. Electronic address: laura.o.vendrame@gmail.com., Zanella I; Laboratório de Materiais Magnéticos Nanoestruturados, Programa de Pós-Graduação em Nanociências, Universidade Franciscana - UFN, Andradas 1614, 97010-032, Santa Maria, RS, Brazil. Electronic address: ivanazanella@gmail.com., Rolim CMB; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria - UFSM, Av. Roraima 1000, 97105-900, Santa Maria, RS, Brazil. Electronic address: clarice.rolim@gmail.com., Rhoden CRB; Laboratório de Materiais Magnéticos Nanoestruturados, Programa de Pós-Graduação em Nanociências, Universidade Franciscana - UFN, Andradas 1614, 97010-032, Santa Maria, RS, Brazil. Electronic address: cristianorbr@gmail.com.
Jazyk: angličtina
Zdroj: Journal of molecular graphics & modelling [J Mol Graph Model] 2024 Jan; Vol. 126, pp. 108639. Date of Electronic Publication: 2023 Sep 24.
DOI: 10.1016/j.jmgm.2023.108639
Abstrakt: This study aimed to develop immediate-release tablets containing amiodarone hydrochloride (AM). AM is a BCS class II compound, i.e., high permeable, and poorly soluble. The interactions between amiodarone and methyl-β-cyclodextrin were DFT-based, theoretically measured, supporting the complexation of AM with cyclodextrin by using methyl-β-cyclodextrin through a spray-drying process. Thus, increasing substantially the drug solubility to 93.31% and 87.14%, respectively. Solubility studies demonstrated the formation of the Drug-Methyl-β-cyclodextrin inclusion complex with 1:1 stoichiometry. The complex formation was characterized by SBET, XRD, DSC, SEM, FTIR, and 1H NMR. Complementing, immediate-release tablets containing the inclusion complex were developed by direct compression, and in vitro dissolution studies were performed in gastrointestinal fluids using USP Pharmacopeia standard dissolution rate testing equipment. The dissolution rate of immediate-release tablets was substantially higher than the pristine drug in all mediums evaluated. These results confirm the application of methyl-β-cyclodextrin as an effective excipient for incorporation in novel dosage forms to increase the solubility of poorly soluble drugs.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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