The effect of methanesulfonic and glutaric acids on the solubility of clofazimine
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In the modern drug research the number of practically insoluble potential drugs is
increasing. Poor aqueous solubility can cause poor oral absorption and low
bioavailability of drugs. Hence, solubility enhancement is considered as one of the most
important challenges in the formulation and development of the dosage forms of drugs.
Clofazimine (CFZ) is an antibiotic drug which is used in the treatment of tuberculosis
and leprosy. It is recently shown that CFZ has inhibitory activity against certain
coronaviruses and can antagonize the replication of SARS-CoV-2.1 Since CFZ is highly
lipophilic molecule with extremely low solubility, it is quite a challenge to find
appropriate method for CFZ solubilization. The aim of this work was to investigate the
effect of methanesulfonic (MSA) and glutaric (GA) acids on the solubility of CFZ. The
effect of MSA on the solubility of CFZ was studied by the pH-Ramp shake-flask method
(pH-RSF).2 The solubility of CFZ was determined i...n the presence of GA in two ways:
1) by melting a mixture of CFZ and GA in different molar ratios, and then dissolving in
water; 2) using the pH-RSF method. Interactions between CZ and GA were investigated
by IR spectroscopy. It is shown that both MSA and GA increase the solubility of CFZ
in acidic suspensions prepared by pH-RSF method. Also, solubility enhancement was
observed in the molten CFZ-GA mixtures (molar ratio 1:1 and 1:4) compared to mixtures
prepared without melting. Besides that, the IR spectra of these mixtures revealed that
characteristic CFZ band was shifted in molted CFZ-GA mixture (molar ratio 1:1)
probably due to CFZ-GA interactions. Preliminary results presented in this study
illustrate that MSA and GA can be used for solubility improvement of CFZ.
Извор:
8th Conference of Young Chemists of Serbia, Belgrade, Serbia, 29th October, 2022. In: Book of Abstracts, 2022, 40-40Издавач:
- Belgrade : Serbian Chemical Society
- Belgrade : Serbian Young Chemists’ Club
Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200026 (Универзитет у Београду, Институт за хемију, технологију и металургију - ИХТМ) (RS-MESTD-inst-2020-200026)
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200168 (Универзитет у Београду, Хемијски факултет) (RS-MESTD-inst-2020-200168)
Колекције
Институција/група
Hemijski fakultet / Faculty of ChemistryTY - CONF AU - Marjanović, Nemanja Ž. AU - Marković, Olivera S. AU - Pešić, Miloš P. AU - Verbić, Tatjana PY - 2022 UR - http://cherry.chem.bg.ac.rs/handle/123456789/5938 AB - In the modern drug research the number of practically insoluble potential drugs is increasing. Poor aqueous solubility can cause poor oral absorption and low bioavailability of drugs. Hence, solubility enhancement is considered as one of the most important challenges in the formulation and development of the dosage forms of drugs. Clofazimine (CFZ) is an antibiotic drug which is used in the treatment of tuberculosis and leprosy. It is recently shown that CFZ has inhibitory activity against certain coronaviruses and can antagonize the replication of SARS-CoV-2.1 Since CFZ is highly lipophilic molecule with extremely low solubility, it is quite a challenge to find appropriate method for CFZ solubilization. The aim of this work was to investigate the effect of methanesulfonic (MSA) and glutaric (GA) acids on the solubility of CFZ. The effect of MSA on the solubility of CFZ was studied by the pH-Ramp shake-flask method (pH-RSF).2 The solubility of CFZ was determined in the presence of GA in two ways: 1) by melting a mixture of CFZ and GA in different molar ratios, and then dissolving in water; 2) using the pH-RSF method. Interactions between CZ and GA were investigated by IR spectroscopy. It is shown that both MSA and GA increase the solubility of CFZ in acidic suspensions prepared by pH-RSF method. Also, solubility enhancement was observed in the molten CFZ-GA mixtures (molar ratio 1:1 and 1:4) compared to mixtures prepared without melting. Besides that, the IR spectra of these mixtures revealed that characteristic CFZ band was shifted in molted CFZ-GA mixture (molar ratio 1:1) probably due to CFZ-GA interactions. Preliminary results presented in this study illustrate that MSA and GA can be used for solubility improvement of CFZ. PB - Belgrade : Serbian Chemical Society PB - Belgrade : Serbian Young Chemists’ Club C3 - 8th Conference of Young Chemists of Serbia, Belgrade, Serbia, 29th October, 2022. In: Book of Abstracts T1 - The effect of methanesulfonic and glutaric acids on the solubility of clofazimine SP - 40 EP - 40 UR - https://hdl.handle.net/21.15107/rcub_cherry_5938 ER -
@conference{ author = "Marjanović, Nemanja Ž. and Marković, Olivera S. and Pešić, Miloš P. and Verbić, Tatjana", year = "2022", abstract = "In the modern drug research the number of practically insoluble potential drugs is increasing. Poor aqueous solubility can cause poor oral absorption and low bioavailability of drugs. Hence, solubility enhancement is considered as one of the most important challenges in the formulation and development of the dosage forms of drugs. Clofazimine (CFZ) is an antibiotic drug which is used in the treatment of tuberculosis and leprosy. It is recently shown that CFZ has inhibitory activity against certain coronaviruses and can antagonize the replication of SARS-CoV-2.1 Since CFZ is highly lipophilic molecule with extremely low solubility, it is quite a challenge to find appropriate method for CFZ solubilization. The aim of this work was to investigate the effect of methanesulfonic (MSA) and glutaric (GA) acids on the solubility of CFZ. The effect of MSA on the solubility of CFZ was studied by the pH-Ramp shake-flask method (pH-RSF).2 The solubility of CFZ was determined in the presence of GA in two ways: 1) by melting a mixture of CFZ and GA in different molar ratios, and then dissolving in water; 2) using the pH-RSF method. Interactions between CZ and GA were investigated by IR spectroscopy. It is shown that both MSA and GA increase the solubility of CFZ in acidic suspensions prepared by pH-RSF method. Also, solubility enhancement was observed in the molten CFZ-GA mixtures (molar ratio 1:1 and 1:4) compared to mixtures prepared without melting. Besides that, the IR spectra of these mixtures revealed that characteristic CFZ band was shifted in molted CFZ-GA mixture (molar ratio 1:1) probably due to CFZ-GA interactions. Preliminary results presented in this study illustrate that MSA and GA can be used for solubility improvement of CFZ.", publisher = "Belgrade : Serbian Chemical Society, Belgrade : Serbian Young Chemists’ Club", journal = "8th Conference of Young Chemists of Serbia, Belgrade, Serbia, 29th October, 2022. In: Book of Abstracts", title = "The effect of methanesulfonic and glutaric acids on the solubility of clofazimine", pages = "40-40", url = "https://hdl.handle.net/21.15107/rcub_cherry_5938" }
Marjanović, N. Ž., Marković, O. S., Pešić, M. P.,& Verbić, T.. (2022). The effect of methanesulfonic and glutaric acids on the solubility of clofazimine. in 8th Conference of Young Chemists of Serbia, Belgrade, Serbia, 29th October, 2022. In: Book of Abstracts Belgrade : Serbian Chemical Society., 40-40. https://hdl.handle.net/21.15107/rcub_cherry_5938
Marjanović NŽ, Marković OS, Pešić MP, Verbić T. The effect of methanesulfonic and glutaric acids on the solubility of clofazimine. in 8th Conference of Young Chemists of Serbia, Belgrade, Serbia, 29th October, 2022. In: Book of Abstracts. 2022;:40-40. https://hdl.handle.net/21.15107/rcub_cherry_5938 .
Marjanović, Nemanja Ž., Marković, Olivera S., Pešić, Miloš P., Verbić, Tatjana, "The effect of methanesulfonic and glutaric acids on the solubility of clofazimine" in 8th Conference of Young Chemists of Serbia, Belgrade, Serbia, 29th October, 2022. In: Book of Abstracts (2022):40-40, https://hdl.handle.net/21.15107/rcub_cherry_5938 .