Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers

Co-crystal is believed to improve the solubility and dissolution rates and thus, enhanced the bioavailability of poor water soluble drugs particularly during the oral route of administration. With the existing of poorly soluble drugs in pharmaceutical industry, the screening of co-crystal formation...

Full description

Bibliographic Details
Main Authors:	Syarifah, Abd Rahim, Fatinah, Ab Rahman, Engku N. E. M., Nasir, Noor Ashila, Ramle
Format:	Article
Language:	English
Published:	World Academy of Science, Engineering and Technology 2015
Subjects:	TP Chemical technology
Online Access:	http://umpir.ump.edu.my/id/eprint/9423/ http://umpir.ump.edu.my/id/eprint/9423/ http://umpir.ump.edu.my/id/eprint/9423/1/Carbamazepine%20Co-crystal%20Screening%20with%20Dicarboxylic%20Acids%20Co-Crystal%20Formers.pdf

id	ump-9423
recordtype	eprints
spelling	ump-94232019-10-30T07:38:46Z http://umpir.ump.edu.my/id/eprint/9423/ Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers Syarifah, Abd Rahim Fatinah, Ab Rahman Engku N. E. M., Nasir Noor Ashila, Ramle TP Chemical technology Co-crystal is believed to improve the solubility and dissolution rates and thus, enhanced the bioavailability of poor water soluble drugs particularly during the oral route of administration. With the existing of poorly soluble drugs in pharmaceutical industry, the screening of co-crystal formation using carbamazepine (CBZ) as a model drug compound with dicarboxylic acids co-crystal formers(CCF) namely fumaric (FA) and succinic (SA) acids in ethanol has been studied. The co-crystal formations were studied by varying the mol ratio values of CCF to CBZ to access the effect of CCF concentration on the formation of the co-crystal. Solvent evaporation, slurry and cooling crystallization which representing the solution based method co-crystal screening were used. Based on the differential scanning calorimetry (DSC) analysis, the melting point of CBZ-SA in different ratio was in the range between 188oC-189oC. For CBZ-FA form A and CBZ-FA form B the melting point in different ratio were in the range of 174oC-175oC and 185oC-186oC respectively. The product crystal from the screening was also characterized using X-ray powder diffraction (XRPD). The XRPD pattern profile analysis has shown that the CBZ co-crystals with FA and SA were successfully formed for all ratios studied. The findings revealed that CBZ-FA co-crystal were formed in two different polymorphs. It was found that CBZ-FA form A and form B were formed from evaporation and slurry crystallization methods respectively. On the other hand, in cooling crystallization method, CBZ-FA form A was formed at lower mol ratio of CCF to CBZ and vice versa. This study disclosed that different methods and mol ratios during the co-crystal screening can affect the outcome of co-crystal produced such as polymorphic forms of co-crystal and thereof. Thus, it was suggested that careful attentions is needed during the screening since the co-crystal formation is currently one of the promising approach to be considered in research and development for pharmaceutical industry to improve the poorly soluble drugs. World Academy of Science, Engineering and Technology 2015 Article PeerReviewed application/pdf en http://umpir.ump.edu.my/id/eprint/9423/1/Carbamazepine%20Co-crystal%20Screening%20with%20Dicarboxylic%20Acids%20Co-Crystal%20Formers.pdf Syarifah, Abd Rahim and Fatinah, Ab Rahman and Engku N. E. M., Nasir and Noor Ashila, Ramle (2015) Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers. International Journal of Environmental, Chemical, Ecological, Geological and Geophysical Engineering, 9 (5). pp. 414-417. http://www.waset.org/publications/10001142
repository_type	Digital Repository
institution_category	Local University
institution	Universiti Malaysia Pahang
building	UMP Institutional Repository
collection	Online Access
language	English
topic	TP Chemical technology
spellingShingle	TP Chemical technology Syarifah, Abd Rahim Fatinah, Ab Rahman Engku N. E. M., Nasir Noor Ashila, Ramle Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers
description	Co-crystal is believed to improve the solubility and dissolution rates and thus, enhanced the bioavailability of poor water soluble drugs particularly during the oral route of administration. With the existing of poorly soluble drugs in pharmaceutical industry, the screening of co-crystal formation using carbamazepine (CBZ) as a model drug compound with dicarboxylic acids co-crystal formers(CCF) namely fumaric (FA) and succinic (SA) acids in ethanol has been studied. The co-crystal formations were studied by varying the mol ratio values of CCF to CBZ to access the effect of CCF concentration on the formation of the co-crystal. Solvent evaporation, slurry and cooling crystallization which representing the solution based method co-crystal screening were used. Based on the differential scanning calorimetry (DSC) analysis, the melting point of CBZ-SA in different ratio was in the range between 188oC-189oC. For CBZ-FA form A and CBZ-FA form B the melting point in different ratio were in the range of 174oC-175oC and 185oC-186oC respectively. The product crystal from the screening was also characterized using X-ray powder diffraction (XRPD). The XRPD pattern profile analysis has shown that the CBZ co-crystals with FA and SA were successfully formed for all ratios studied. The findings revealed that CBZ-FA co-crystal were formed in two different polymorphs. It was found that CBZ-FA form A and form B were formed from evaporation and slurry crystallization methods respectively. On the other hand, in cooling crystallization method, CBZ-FA form A was formed at lower mol ratio of CCF to CBZ and vice versa. This study disclosed that different methods and mol ratios during the co-crystal screening can affect the outcome of co-crystal produced such as polymorphic forms of co-crystal and thereof. Thus, it was suggested that careful attentions is needed during the screening since the co-crystal formation is currently one of the promising approach to be considered in research and development for pharmaceutical industry to improve the poorly soluble drugs.
format	Article
author	Syarifah, Abd Rahim Fatinah, Ab Rahman Engku N. E. M., Nasir Noor Ashila, Ramle
author_facet	Syarifah, Abd Rahim Fatinah, Ab Rahman Engku N. E. M., Nasir Noor Ashila, Ramle
author_sort	Syarifah, Abd Rahim
title	Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers
title_short	Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers
title_full	Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers
title_fullStr	Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers
title_full_unstemmed	Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers
title_sort	carbamazepine co-crystal screening with dicarboxylic acids co-crystal formers
publisher	World Academy of Science, Engineering and Technology
publishDate	2015
url	http://umpir.ump.edu.my/id/eprint/9423/ http://umpir.ump.edu.my/id/eprint/9423/ http://umpir.ump.edu.my/id/eprint/9423/1/Carbamazepine%20Co-crystal%20Screening%20with%20Dicarboxylic%20Acids%20Co-Crystal%20Formers.pdf
first_indexed	2023-09-18T22:07:59Z
last_indexed	2023-09-18T22:07:59Z
_version_	1777414836698742784

Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers

Similar Items