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Indomethacin-saccharin cocrystal: design, synthesis and preliminary pharmaceutical characterization
Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.
Energy Technology and Thermal Process Chemistry, Umeå University.
Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.ORCID-id: 0000-0002-0654-5410
2008 (engelsk)Inngår i: Pharmaceutical research, ISSN 0724-8741, E-ISSN 1573-904X, Vol. 25, nr 3, s. 530-41Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

PURPOSE: To design and prepare cocrystals of indomethacin using crystal engineering approaches, with the ultimate objective of improving the physical properties of indomethacin, especially solubility and dissolution rate. MATERIALS AND METHODS: Various cocrystal formers, including saccharin, were used in endeavours to obtain indomethacin cocrystals by slow evaporation from a series of solvents. The melting point of crystalline phases was determined. The potential cocrystalline phase was characterized by DSC, IR, Raman and PXRD techniques. The indomethacin-saccharin cocrystal (hereafter IND-SAC cocrystal) structure was determined from single crystal X-ray diffraction data. Pharmaceutically relevant properties such as the dissolution rate and dynamic vapour sorption (DVS) of the IND-SAC cocrystal were evaluated. Solid state and liquid-assisted (solvent-drop) cogrinding methods were also applied to indomethacin and saccharin. RESULTS: The IND-SAC cocrystals were obtained from ethyl acetate. Physical characterization showed that the IND-SAC cocrystal is unique vis-a-vis thermal, spectroscopic and X-ray diffraction properties. The cocrystals were obtained in a 1:1 ratio with a carboxylic acid and imide dimer synthons. The dissolution rate of IND-SAC cocrystal system was considerably faster than that of the stable indomethacin gamma-form. DVS studies indicated that the cocrystals gained less than 0.05% in weight at 98%RH. IND-SAC cocrystal was also obtained by solid state and liquid-assisted cogrinding methods. CONCLUSIONS: The IND-SAC cocrystal was formed with a unique and interesting carboxylic acid and imide dimer synthons interconnected by weak N-Hcdots, three dots, centeredO hydrogen bonds. The cocrystals were non-hygroscopic and were associated with a significantly faster dissolution rate than indomethacin (gamma-form).

sted, utgiver, år, opplag, sider
2008. Vol. 25, nr 3, s. 530-41
Identifikatorer
URN: urn:nbn:se:ltu:diva-12286DOI: 10.1007/s11095-007-9394-1ISI: 000253765900006Scopus ID: 2-s2.0-40549089922Lokal ID: b6521030-75a4-11dc-824d-000ea68e967bOAI: oai:DiVA.org:ltu-12286DiVA, id: diva2:985236
Merknad

Validerad; 2008; 20071008 (andbra)

Tilgjengelig fra: 2016-09-29 Laget: 2016-09-29 Sist oppdatert: 2018-07-10bibliografisk kontrollert

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