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Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes

Rudrangi, S R S, Bhomia, Ruchir, Trivedi, Vivek, Vine, G J, Mitchell, John C., Alexander, Bruce D., Wicks, Stephen (2015) Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes. International Journal of Pharmaceutics, 479 (2). pp. 381-390. ISSN 0378-5173. (doi:10.1016/j.ijpharm.2015.01.010) (Access to this publication is currently restricted. You may be able to access a copy if URLs are provided)

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https://doi.org/10.1016/j.ijpharm.2015.01.010

Abstract

The main objective of this study was to investigate different manufacturing processes claimed to promote inclusion complexation between indomethacin and cyclodextrins in order to enhance the apparent solubility and dissolution properties of indomethacin. Especially, the effectiveness of supercritical carbon dioxide processing for preparing solid drug–cyclodextrin inclusion complexes was investigated and compared to other preparation methods. The complexes were prepared by physical mixing, co-evaporation, freeze drying from aqueous solution, spray drying and supercritical carbon dioxide processing methods. The prepared complexes were then evaluated by scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, solubility and dissolution studies. The method of preparation of the inclusion complexes was shown to influence the physicochemical properties of the formed complexes. Indomethacin exists in a highly crystalline solid form. Physical mixing of indomethacin and methyl-β-cyclodextrin appeared not to reduce the degree of crystallinity of the drug. The co-evaporated and freeze dried complexes had a lower degree of crystallinity than the physical mix; however the lowest degree of crystallinity was achieved in complexes prepared by spray drying and supercritical carbon dioxide processing methods. All systems based on methyl-β-cyclodextrin exhibited better dissolution properties than the drug alone. The greatest improvement in drug dissolution properties was obtained from complexes prepared using supercritical carbon dioxide processing, thereafter by spray drying, freeze drying, co-evaporation and finally by physical mixing. Supercritical carbon dioxide processing is well known as an energy efficient alternative to other pharmaceutical processes and may have application for the preparation of solid-state drug–cyclodextrin inclusion complexes. It is an effective and economic method that allows the formation of solid complexes with a high yield, without the use of organic solvents and problems associated with their residues.

Item Type: Article
DOI/Identification number: 10.1016/j.ijpharm.2015.01.010
Uncontrolled keywords: Indomethacin, Methyl-β-cyclodextrin, Inclusion complexes, Spray drying, Supercritical carbon dioxide
Subjects: R Medicine > RS Pharmacy and materia medica
Divisions: Central Services > Universities at Medway
Faculties > Sciences > Medway School of Pharmacy
Depositing User: Vivek Trivedi
Date Deposited: 25 Apr 2019 13:08 UTC
Last Modified: 03 Jun 2019 09:44 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/73635 (The current URI for this page, for reference purposes)
Trivedi, Vivek: https://orcid.org/0000-0001-9304-9214
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