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Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes.
Int J Pharm. 2015 Feb 20; 479(2):381-90.IJ

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.

Authors+Show Affiliations

Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom. Electronic address: S.R.Rudrangi@greenwich.ac.uk.Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom.Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom.Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom.Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom.Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom. Electronic address: B.Alexander@greenwich.ac.uk.Medway Centre for Pharmaceutical Sciences, University of Greenwich, Central Avenue, Chatham Maritime, Kent ME4 4TB, United Kingdom.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25579867

Citation

Rudrangi, Shashi Ravi Suman, et al. "Influence of the Preparation Method On the Physicochemical Properties of Indomethacin and Methyl-β-cyclodextrin Complexes." International Journal of Pharmaceutics, vol. 479, no. 2, 2015, pp. 381-90.
Rudrangi SR, Bhomia R, Trivedi V, et al. Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes. Int J Pharm. 2015;479(2):381-90.
Rudrangi, S. R., Bhomia, R., Trivedi, V., Vine, G. J., Mitchell, J. C., Alexander, B. D., & Wicks, S. R. (2015). Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes. International Journal of Pharmaceutics, 479(2), 381-90. https://doi.org/10.1016/j.ijpharm.2015.01.010
Rudrangi SR, et al. Influence of the Preparation Method On the Physicochemical Properties of Indomethacin and Methyl-β-cyclodextrin Complexes. Int J Pharm. 2015 Feb 20;479(2):381-90. PubMed PMID: 25579867.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes. AU - Rudrangi,Shashi Ravi Suman, AU - Bhomia,Ruchir, AU - Trivedi,Vivek, AU - Vine,George J, AU - Mitchell,John C, AU - Alexander,Bruce David, AU - Wicks,Stephen Richard, Y1 - 2015/01/08/ PY - 2014/11/07/received PY - 2015/01/06/revised PY - 2015/01/07/accepted PY - 2015/1/13/entrez PY - 2015/1/13/pubmed PY - 2015/12/15/medline KW - Inclusion complexes KW - Indomethacin KW - Methyl-β-cyclodextrin KW - Spray drying KW - Supercritical carbon dioxide SP - 381 EP - 90 JF - International journal of pharmaceutics JO - Int J Pharm VL - 479 IS - 2 N2 - 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. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25579867/Influence_of_the_preparation_method_on_the_physicochemical_properties_of_indomethacin_and_methyl_β_cyclodextrin_complexes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)00012-5 DB - PRIME DP - Unbound Medicine ER -