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Formulation and characterization of amiodarone-methyl-beta-cyclodextrin inclusion complexes: A molecular modelling
Alexandre M Rubim1, Jaqueline B Rubenick2, Laura O Vendrame3
1Programa 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.
Journal of Molecular Graphics & Modelling
|September 29, 2023
Summary
This study enhances amiodarone hydrochloride solubility using methyl-β-cyclodextrin complexation via spray-drying. Developed tablets showed significantly improved dissolution rates, offering a promising approach for poorly soluble drugs.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Physical Chemistry
Background:
- Amiodarone hydrochloride (AM) is a BCS class II drug, characterized by high permeability and poor solubility.
- Poor solubility limits the therapeutic efficacy of many active pharmaceutical ingredients.
- Developing effective strategies to enhance drug solubility is crucial for improving oral bioavailability and therapeutic outcomes.
Purpose of the Study:
- To develop immediate-release tablets of amiodarone hydrochloride (AM).
- To enhance the solubility and dissolution rate of AM using methyl-β-cyclodextrin (MBC) complexation.
- To evaluate the in vitro performance of AM-MBC inclusion complex tablets.
Main Methods:
- Complexation of AM with MBC was achieved through a spray-drying process.
- Theoretical interactions were investigated using Density Functional Theory (DFT).
- Inclusion complex formation was characterized using techniques including SBET, XRD, DSC, SEM, FTIR, and 1H NMR.
- Immediate-release tablets were formulated by direct compression and dissolution testing was performed.
Main Results:
- Spray-drying with MBC significantly increased AM solubility to 93.31% and 87.14%.
- Solubility studies confirmed a 1:1 stoichiometry for the AM-MBC inclusion complex.
- Characterization techniques validated the formation of the inclusion complex.
- The developed tablets exhibited substantially higher dissolution rates compared to the pristine drug in various media.
Conclusions:
- Methyl-β-cyclodextrin is an effective excipient for enhancing the solubility of poorly soluble drugs like amiodarone hydrochloride.
- Spray-drying is a viable method for preparing AM-MBC inclusion complexes.
- The developed immediate-release tablets demonstrate improved drug release profiles, indicating potential for enhanced therapeutic efficacy.
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