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Enhancement of Valsartan Oral Bioavailability by Preparing a Microwave-Irradiated Inclusion Complex with Sulfobutyl Etherβ-Cyclodextrin Using a Central Composite Face Design for Optimising Process Parameters

Enhancement of Valsartan Oral Bioavailability by Preparing a Microwave-Irradiated Inclusion... The purpose of the study is to investigate the influence of sulfobutyl ether β-cyclodextrin (SBE7-β-CD) on the bioavailability of valsartan. Phase solubility investigations showed an AL type curve. The estimated apparent stability constant for valsartan SBE7-β-CD is 427 ± 0.32 M−1. Inclusion complexes of valsartan SBE7-β-CD in equal molar ratio were prepared by microwave irradiation technique. The process parameters were optimised with a central composite face design. Response surface graphs and contour plots showed how process factors affected drug content. The inclusion complexes prepared by optimising process variables are characterised. The DSC and X-ray diffraction confirm the formation of inclusion complexes and the drug’s transition from a crystalline to an amorphous state. FTIR suggests hydrogen bonding between valsartan and SBE7-β-CD. SEM showed changes in drug morphology and shape. The dissolution rate of the prepared SBE7-β-CD complex using microwave irradiation was 2.85 times that of pure valsartan. The inclusion complex was formulated into tablet dosage forms F1 to F4. Furthermore, oral bioavailability studies in rats with tablet formulation F3 were carried out and compared to the marketed Diovan® tablet as a reference standard. The F3 tablet formulation exhibited significantly higher values of AUC0-∞ and Cmax than the reference. Finally, the microwave-irradiated valsartan SBE7-β-CD inclusion complex converted into tablet dosage form may be a promising approach to increasing valsartan oral bioavailability. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png AAPS PharmSciTech Springer Journals

Enhancement of Valsartan Oral Bioavailability by Preparing a Microwave-Irradiated Inclusion Complex with Sulfobutyl Etherβ-Cyclodextrin Using a Central Composite Face Design for Optimising Process Parameters

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References (48)

Publisher
Springer Journals
Copyright
Copyright © The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists 2023. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.
eISSN
1530-9932
DOI
10.1208/s12249-023-02571-2
Publisher site
See Article on Publisher Site

Abstract

The purpose of the study is to investigate the influence of sulfobutyl ether β-cyclodextrin (SBE7-β-CD) on the bioavailability of valsartan. Phase solubility investigations showed an AL type curve. The estimated apparent stability constant for valsartan SBE7-β-CD is 427 ± 0.32 M−1. Inclusion complexes of valsartan SBE7-β-CD in equal molar ratio were prepared by microwave irradiation technique. The process parameters were optimised with a central composite face design. Response surface graphs and contour plots showed how process factors affected drug content. The inclusion complexes prepared by optimising process variables are characterised. The DSC and X-ray diffraction confirm the formation of inclusion complexes and the drug’s transition from a crystalline to an amorphous state. FTIR suggests hydrogen bonding between valsartan and SBE7-β-CD. SEM showed changes in drug morphology and shape. The dissolution rate of the prepared SBE7-β-CD complex using microwave irradiation was 2.85 times that of pure valsartan. The inclusion complex was formulated into tablet dosage forms F1 to F4. Furthermore, oral bioavailability studies in rats with tablet formulation F3 were carried out and compared to the marketed Diovan® tablet as a reference standard. The F3 tablet formulation exhibited significantly higher values of AUC0-∞ and Cmax than the reference. Finally, the microwave-irradiated valsartan SBE7-β-CD inclusion complex converted into tablet dosage form may be a promising approach to increasing valsartan oral bioavailability.

Journal

AAPS PharmSciTechSpringer Journals

Published: May 9, 2023

Keywords: Microwave-irradiated inclusion complexes; Modified β-cyclodextrin; Response surface methodology; SBE7-β-CD; Valsartan

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