Cooling crystallization of Indomethacin from different organic solvents

Chandrakant Ramkrishna Malwade, Haiyan Qu

Publikation: Konferencebidrag uden forlag/tidsskriftPaperForskningpeer review

Resumé

In the present work, crystallization of an anti-inflammatory drug Indomethacin (IMC) from different organic solvents was investigated concerning the polymorphism and particulate properties of the final product. Initially, the solvents were screened by measuring solubility of IMC at temperatures 15, 25, 35, and 45 °C. The solvents with varying polarities (ethanol, methanol, ethyl acetate, acetone, acetonitrile, and dichloromethane) were used for solubility measurement. Maximum solubility of IMC was observed in acetone, while acetonitrile showed the lowest solubility. Solid phase analysis of excess solute with XRPD and Raman spectroscopy confirmed formation of IMC solvate in acetone, methanol and dichloromethane at 15 °C. Based on solubility of IMC, the solvents ethanol, ethyl acetate, acetone, and dichloromethane were selected for crystallization experiments. Nucleation kinetics of IMC in selected solvents was investigated through the measurement of induction time at 5 °C and 15 °C. Longer induction times were observed for IMC in ethanol at both temperatures compared to the one in acetone. Metastable α form of IMC was obtained from ethanol, while solvate of IMC was produced from acetone.
OriginalsprogEngelsk
Publikationsdato2017
Antal sider6
StatusUdgivet - 2017
Begivenhed24th International Symposium on Industrial Crystallization - Technical University, Dortmund, Tyskland
Varighed: 29 aug. 201731 aug. 2017
http://www.apt.bci.tu-dortmund.de/cms/en/BIWIC2017/index.html

Konference

Konference24th International Symposium on Industrial Crystallization
LokationTechnical University
LandTyskland
ByDortmund
Periode29/08/201731/08/2017
Internetadresse

Fingeraftryk

Crystallization
Indomethacin
Organic solvents
Acetone
Cooling
Solubility
Methylene Chloride
Ethanol
Methanol
Polymorphism
Raman spectroscopy
Nucleation
Anti-Inflammatory Agents
Temperature
Kinetics
Pharmaceutical Preparations

Citer dette

Malwade, C. R., & Qu, H. (2017). Cooling crystallization of Indomethacin from different organic solvents. Afhandling præsenteret på 24th International Symposium on Industrial Crystallization, Dortmund, Tyskland.
Malwade, Chandrakant Ramkrishna ; Qu, Haiyan. / Cooling crystallization of Indomethacin from different organic solvents. Afhandling præsenteret på 24th International Symposium on Industrial Crystallization, Dortmund, Tyskland.6 s.
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abstract = "In the present work, crystallization of an anti-inflammatory drug Indomethacin (IMC) from different organic solvents was investigated concerning the polymorphism and particulate properties of the final product. Initially, the solvents were screened by measuring solubility of IMC at temperatures 15, 25, 35, and 45 °C. The solvents with varying polarities (ethanol, methanol, ethyl acetate, acetone, acetonitrile, and dichloromethane) were used for solubility measurement. Maximum solubility of IMC was observed in acetone, while acetonitrile showed the lowest solubility. Solid phase analysis of excess solute with XRPD and Raman spectroscopy confirmed formation of IMC solvate in acetone, methanol and dichloromethane at 15 °C. Based on solubility of IMC, the solvents ethanol, ethyl acetate, acetone, and dichloromethane were selected for crystallization experiments. Nucleation kinetics of IMC in selected solvents was investigated through the measurement of induction time at 5 °C and 15 °C. Longer induction times were observed for IMC in ethanol at both temperatures compared to the one in acetone. Metastable α form of IMC was obtained from ethanol, while solvate of IMC was produced from acetone.",
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Malwade, CR & Qu, H 2017, 'Cooling crystallization of Indomethacin from different organic solvents' Paper fremlagt ved 24th International Symposium on Industrial Crystallization, Dortmund, Tyskland, 29/08/2017 - 31/08/2017, .

Cooling crystallization of Indomethacin from different organic solvents. / Malwade, Chandrakant Ramkrishna; Qu, Haiyan.

2017. Afhandling præsenteret på 24th International Symposium on Industrial Crystallization, Dortmund, Tyskland.

Publikation: Konferencebidrag uden forlag/tidsskriftPaperForskningpeer review

TY - CONF

T1 - Cooling crystallization of Indomethacin from different organic solvents

AU - Malwade, Chandrakant Ramkrishna

AU - Qu, Haiyan

PY - 2017

Y1 - 2017

N2 - In the present work, crystallization of an anti-inflammatory drug Indomethacin (IMC) from different organic solvents was investigated concerning the polymorphism and particulate properties of the final product. Initially, the solvents were screened by measuring solubility of IMC at temperatures 15, 25, 35, and 45 °C. The solvents with varying polarities (ethanol, methanol, ethyl acetate, acetone, acetonitrile, and dichloromethane) were used for solubility measurement. Maximum solubility of IMC was observed in acetone, while acetonitrile showed the lowest solubility. Solid phase analysis of excess solute with XRPD and Raman spectroscopy confirmed formation of IMC solvate in acetone, methanol and dichloromethane at 15 °C. Based on solubility of IMC, the solvents ethanol, ethyl acetate, acetone, and dichloromethane were selected for crystallization experiments. Nucleation kinetics of IMC in selected solvents was investigated through the measurement of induction time at 5 °C and 15 °C. Longer induction times were observed for IMC in ethanol at both temperatures compared to the one in acetone. Metastable α form of IMC was obtained from ethanol, while solvate of IMC was produced from acetone.

AB - In the present work, crystallization of an anti-inflammatory drug Indomethacin (IMC) from different organic solvents was investigated concerning the polymorphism and particulate properties of the final product. Initially, the solvents were screened by measuring solubility of IMC at temperatures 15, 25, 35, and 45 °C. The solvents with varying polarities (ethanol, methanol, ethyl acetate, acetone, acetonitrile, and dichloromethane) were used for solubility measurement. Maximum solubility of IMC was observed in acetone, while acetonitrile showed the lowest solubility. Solid phase analysis of excess solute with XRPD and Raman spectroscopy confirmed formation of IMC solvate in acetone, methanol and dichloromethane at 15 °C. Based on solubility of IMC, the solvents ethanol, ethyl acetate, acetone, and dichloromethane were selected for crystallization experiments. Nucleation kinetics of IMC in selected solvents was investigated through the measurement of induction time at 5 °C and 15 °C. Longer induction times were observed for IMC in ethanol at both temperatures compared to the one in acetone. Metastable α form of IMC was obtained from ethanol, while solvate of IMC was produced from acetone.

M3 - Paper

ER -

Malwade CR, Qu H. Cooling crystallization of Indomethacin from different organic solvents. 2017. Afhandling præsenteret på 24th International Symposium on Industrial Crystallization, Dortmund, Tyskland.