Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin

This study aimed to increase the solubility of indomethacin in water by complexation it with hydroxypropyl-b-cyclodextrin (HPbCD). Phase-solubility analysis was used to investigate interactions in aqueous solution between HPbCD and indomethacin. Equimolar indomethacin-HPbCD solid systems were prepar...

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Main Authors: Jiradej Manosroi, Charinya Chankhampan, Kuncoro Foe, Maria Goretti Apriyani, Worapaka Manosroi, Aranya Manosroi
Language:English
Published: Science Faculty of Chiang Mai University 2019
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Online Access:http://it.science.cmu.ac.th/ejournal/dl.php?journal_id=6822
http://cmuir.cmu.ac.th/jspui/handle/6653943832/66120
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spelling th-cmuir.6653943832-661202019-08-21T09:18:22Z Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin Jiradej Manosroi Charinya Chankhampan Kuncoro Foe Maria Goretti Apriyani Worapaka Manosroi Aranya Manosroi Indomethacin Hydroxypropyl--cyclodextrin Inclusion complex Kneading Coevaporation Freeze-drying This study aimed to increase the solubility of indomethacin in water by complexation it with hydroxypropyl-b-cyclodextrin (HPbCD). Phase-solubility analysis was used to investigate interactions in aqueous solution between HPbCD and indomethacin. Equimolar indomethacin-HPbCD solid systems were prepared by four different methods including physical mixtures (PM), kneading (KN), coevaporation (COE) and freeze-drying (COL) methods. The complex was characterized by infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry, thin layer chromatography and dissolution rates. The complexation efficiency of indomethacin-HPbCD was determined spectrophotometrically. The solubility of indomethacin increased linearly as the concentration of HPbCD increased. This indicated a feature of the AL-type complex that the water-soluble complexes existed in the solution. The average of apparent 1:1 stability constant of the complex (K1:1) at 30°C was 340 M-1. The KN and COE methods formed partial inclusion complexes, whereas the COL method gave complete complexation. The dissolution rates of indomethacin increased when complexed with HPbCD. HPbCD complexation of an ionized drug molecule by the COL method exhibited the highest dissolution rate of indomethacin [the dissolution efficiency after 90 min (DE90) at 61.7±0.9% and t50% of 13 min., while the uncomplexed indomethacin showed DE90 at 15.4±0.1% and t50% more than 90 min. The COL process was the best because of the high content and dissolution rate of the drug. It is also the simple method to prepare the inclusion complexes. The result from this study has suggested the dissolution rate enhancement of indomethacin by the simple complexaion method with HPbCD. 2019-08-21T09:18:22Z 2019-08-21T09:18:22Z 2016 Chiang Mai Journal of Science 43, 3 (Apr 2016), 631 - 642 0125-2526 http://it.science.cmu.ac.th/ejournal/dl.php?journal_id=6822 http://cmuir.cmu.ac.th/jspui/handle/6653943832/66120 Eng Science Faculty of Chiang Mai University
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
language English
topic Indomethacin
Hydroxypropyl--cyclodextrin
Inclusion complex
Kneading
Coevaporation
Freeze-drying
spellingShingle Indomethacin
Hydroxypropyl--cyclodextrin
Inclusion complex
Kneading
Coevaporation
Freeze-drying
Jiradej Manosroi
Charinya Chankhampan
Kuncoro Foe
Maria Goretti Apriyani
Worapaka Manosroi
Aranya Manosroi
Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin
description This study aimed to increase the solubility of indomethacin in water by complexation it with hydroxypropyl-b-cyclodextrin (HPbCD). Phase-solubility analysis was used to investigate interactions in aqueous solution between HPbCD and indomethacin. Equimolar indomethacin-HPbCD solid systems were prepared by four different methods including physical mixtures (PM), kneading (KN), coevaporation (COE) and freeze-drying (COL) methods. The complex was characterized by infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry, thin layer chromatography and dissolution rates. The complexation efficiency of indomethacin-HPbCD was determined spectrophotometrically. The solubility of indomethacin increased linearly as the concentration of HPbCD increased. This indicated a feature of the AL-type complex that the water-soluble complexes existed in the solution. The average of apparent 1:1 stability constant of the complex (K1:1) at 30°C was 340 M-1. The KN and COE methods formed partial inclusion complexes, whereas the COL method gave complete complexation. The dissolution rates of indomethacin increased when complexed with HPbCD. HPbCD complexation of an ionized drug molecule by the COL method exhibited the highest dissolution rate of indomethacin [the dissolution efficiency after 90 min (DE90) at 61.7±0.9% and t50% of 13 min., while the uncomplexed indomethacin showed DE90 at 15.4±0.1% and t50% more than 90 min. The COL process was the best because of the high content and dissolution rate of the drug. It is also the simple method to prepare the inclusion complexes. The result from this study has suggested the dissolution rate enhancement of indomethacin by the simple complexaion method with HPbCD.
author Jiradej Manosroi
Charinya Chankhampan
Kuncoro Foe
Maria Goretti Apriyani
Worapaka Manosroi
Aranya Manosroi
author_facet Jiradej Manosroi
Charinya Chankhampan
Kuncoro Foe
Maria Goretti Apriyani
Worapaka Manosroi
Aranya Manosroi
author_sort Jiradej Manosroi
title Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin
title_short Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin
title_full Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin
title_fullStr Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin
title_full_unstemmed Inclusion Complexation of Indomethacin with Hydroxypropyl--cyclodextrin
title_sort inclusion complexation of indomethacin with hydroxypropyl--cyclodextrin
publisher Science Faculty of Chiang Mai University
publishDate 2019
url http://it.science.cmu.ac.th/ejournal/dl.php?journal_id=6822
http://cmuir.cmu.ac.th/jspui/handle/6653943832/66120
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