A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms
Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its b...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
de Melo, Cybelly Marques [verfasserIn] de Medeiros Vieira, Amanda Carla Quintas da Silva do Nascimento, André Luiz Figueirêdo, Camila Bezerra Melo Soares-Sobrinho, José Lamartine |
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| Format: |
Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2014 |
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| Anmerkung: |
© Akadémiai Kiadó, Budapest, Hungary 2014 |
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| Übergeordnetes Werk: |
Enthalten in: Journal of thermal analysis and calorimetry - Springer Netherlands, 1998, 120(2014), 1 vom: 24. Sept., Seite 689-697 |
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| Übergeordnetes Werk: |
volume:120 ; year:2014 ; number:1 ; day:24 ; month:09 ; pages:689-697 |
| Links: |
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| DOI / URN: |
10.1007/s10973-014-4163-y |
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OLC2049836538 |
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| 520 | |a Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. | ||
| 650 | 4 | |a Physical–chemical characterization | |
| 650 | 4 | |a Thermal compatibility | |
| 650 | 4 | |a Epiisopiloturine | |
| 700 | 1 | |a de Medeiros Vieira, Amanda Carla Quintas |4 aut | |
| 700 | 1 | |a da Silva do Nascimento, André Luiz |4 aut | |
| 700 | 1 | |a Figueirêdo, Camila Bezerra Melo |4 aut | |
| 700 | 1 | |a Rolim, Larissa Araújo |4 aut | |
| 700 | 1 | |a Soares-Sobrinho, José Lamartine |4 aut | |
| 700 | 1 | |a Veras, Leiz Maria Costa |4 aut | |
| 700 | 1 | |a de Souza de Almeida Leite, José Roberto |4 aut | |
| 700 | 1 | |a Neto, Pedro José Rolim |4 aut | |
| 700 | 1 | |a de La Roca Soares, Mônica Felts |4 aut | |
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10.1007/s10973-014-4163-y doi (DE-627)OLC2049836538 (DE-He213)s10973-014-4163-y-p DE-627 ger DE-627 rakwb eng 660 VZ de Melo, Cybelly Marques verfasserin aut A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms 2014 Text txt rdacontent ohne Hilfsmittel zu benutzen n rdamedia Band nc rdacarrier © Akadémiai Kiadó, Budapest, Hungary 2014 Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. Physical–chemical characterization Thermal compatibility Epiisopiloturine de Medeiros Vieira, Amanda Carla Quintas aut da Silva do Nascimento, André Luiz aut Figueirêdo, Camila Bezerra Melo aut Rolim, Larissa Araújo aut Soares-Sobrinho, José Lamartine aut Veras, Leiz Maria Costa aut de Souza de Almeida Leite, José Roberto aut Neto, Pedro José Rolim aut de La Roca Soares, Mônica Felts aut Enthalten in Journal of thermal analysis and calorimetry Springer Netherlands, 1998 120(2014), 1 vom: 24. Sept., Seite 689-697 (DE-627)244148767 (DE-600)1429493-X (DE-576)066397693 1388-6150 nnns volume:120 year:2014 number:1 day:24 month:09 pages:689-697 https://doi.org/10.1007/s10973-014-4163-y lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_OLC SSG-OLC-TEC SSG-OLC-CHE SSG-OLC-PHA SSG-OLC-DE-84 GBV_ILN_70 AR 120 2014 1 24 09 689-697 |
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10.1007/s10973-014-4163-y doi (DE-627)OLC2049836538 (DE-He213)s10973-014-4163-y-p DE-627 ger DE-627 rakwb eng 660 VZ de Melo, Cybelly Marques verfasserin aut A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms 2014 Text txt rdacontent ohne Hilfsmittel zu benutzen n rdamedia Band nc rdacarrier © Akadémiai Kiadó, Budapest, Hungary 2014 Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. Physical–chemical characterization Thermal compatibility Epiisopiloturine de Medeiros Vieira, Amanda Carla Quintas aut da Silva do Nascimento, André Luiz aut Figueirêdo, Camila Bezerra Melo aut Rolim, Larissa Araújo aut Soares-Sobrinho, José Lamartine aut Veras, Leiz Maria Costa aut de Souza de Almeida Leite, José Roberto aut Neto, Pedro José Rolim aut de La Roca Soares, Mônica Felts aut Enthalten in Journal of thermal analysis and calorimetry Springer Netherlands, 1998 120(2014), 1 vom: 24. Sept., Seite 689-697 (DE-627)244148767 (DE-600)1429493-X (DE-576)066397693 1388-6150 nnns volume:120 year:2014 number:1 day:24 month:09 pages:689-697 https://doi.org/10.1007/s10973-014-4163-y lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_OLC SSG-OLC-TEC SSG-OLC-CHE SSG-OLC-PHA SSG-OLC-DE-84 GBV_ILN_70 AR 120 2014 1 24 09 689-697 |
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10.1007/s10973-014-4163-y doi (DE-627)OLC2049836538 (DE-He213)s10973-014-4163-y-p DE-627 ger DE-627 rakwb eng 660 VZ de Melo, Cybelly Marques verfasserin aut A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms 2014 Text txt rdacontent ohne Hilfsmittel zu benutzen n rdamedia Band nc rdacarrier © Akadémiai Kiadó, Budapest, Hungary 2014 Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. Physical–chemical characterization Thermal compatibility Epiisopiloturine de Medeiros Vieira, Amanda Carla Quintas aut da Silva do Nascimento, André Luiz aut Figueirêdo, Camila Bezerra Melo aut Rolim, Larissa Araújo aut Soares-Sobrinho, José Lamartine aut Veras, Leiz Maria Costa aut de Souza de Almeida Leite, José Roberto aut Neto, Pedro José Rolim aut de La Roca Soares, Mônica Felts aut Enthalten in Journal of thermal analysis and calorimetry Springer Netherlands, 1998 120(2014), 1 vom: 24. Sept., Seite 689-697 (DE-627)244148767 (DE-600)1429493-X (DE-576)066397693 1388-6150 nnns volume:120 year:2014 number:1 day:24 month:09 pages:689-697 https://doi.org/10.1007/s10973-014-4163-y lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_OLC SSG-OLC-TEC SSG-OLC-CHE SSG-OLC-PHA SSG-OLC-DE-84 GBV_ILN_70 AR 120 2014 1 24 09 689-697 |
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10.1007/s10973-014-4163-y doi (DE-627)OLC2049836538 (DE-He213)s10973-014-4163-y-p DE-627 ger DE-627 rakwb eng 660 VZ de Melo, Cybelly Marques verfasserin aut A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms 2014 Text txt rdacontent ohne Hilfsmittel zu benutzen n rdamedia Band nc rdacarrier © Akadémiai Kiadó, Budapest, Hungary 2014 Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. Physical–chemical characterization Thermal compatibility Epiisopiloturine de Medeiros Vieira, Amanda Carla Quintas aut da Silva do Nascimento, André Luiz aut Figueirêdo, Camila Bezerra Melo aut Rolim, Larissa Araújo aut Soares-Sobrinho, José Lamartine aut Veras, Leiz Maria Costa aut de Souza de Almeida Leite, José Roberto aut Neto, Pedro José Rolim aut de La Roca Soares, Mônica Felts aut Enthalten in Journal of thermal analysis and calorimetry Springer Netherlands, 1998 120(2014), 1 vom: 24. Sept., Seite 689-697 (DE-627)244148767 (DE-600)1429493-X (DE-576)066397693 1388-6150 nnns volume:120 year:2014 number:1 day:24 month:09 pages:689-697 https://doi.org/10.1007/s10973-014-4163-y lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_OLC SSG-OLC-TEC SSG-OLC-CHE SSG-OLC-PHA SSG-OLC-DE-84 GBV_ILN_70 AR 120 2014 1 24 09 689-697 |
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10.1007/s10973-014-4163-y doi (DE-627)OLC2049836538 (DE-He213)s10973-014-4163-y-p DE-627 ger DE-627 rakwb eng 660 VZ de Melo, Cybelly Marques verfasserin aut A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms 2014 Text txt rdacontent ohne Hilfsmittel zu benutzen n rdamedia Band nc rdacarrier © Akadémiai Kiadó, Budapest, Hungary 2014 Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. Physical–chemical characterization Thermal compatibility Epiisopiloturine de Medeiros Vieira, Amanda Carla Quintas aut da Silva do Nascimento, André Luiz aut Figueirêdo, Camila Bezerra Melo aut Rolim, Larissa Araújo aut Soares-Sobrinho, José Lamartine aut Veras, Leiz Maria Costa aut de Souza de Almeida Leite, José Roberto aut Neto, Pedro José Rolim aut de La Roca Soares, Mônica Felts aut Enthalten in Journal of thermal analysis and calorimetry Springer Netherlands, 1998 120(2014), 1 vom: 24. Sept., Seite 689-697 (DE-627)244148767 (DE-600)1429493-X (DE-576)066397693 1388-6150 nnns volume:120 year:2014 number:1 day:24 month:09 pages:689-697 https://doi.org/10.1007/s10973-014-4163-y lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_OLC SSG-OLC-TEC SSG-OLC-CHE SSG-OLC-PHA SSG-OLC-DE-84 GBV_ILN_70 AR 120 2014 1 24 09 689-697 |
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de Melo, Cybelly Marques @@aut@@ de Medeiros Vieira, Amanda Carla Quintas @@aut@@ da Silva do Nascimento, André Luiz @@aut@@ Figueirêdo, Camila Bezerra Melo @@aut@@ Rolim, Larissa Araújo @@aut@@ Soares-Sobrinho, José Lamartine @@aut@@ Veras, Leiz Maria Costa @@aut@@ de Souza de Almeida Leite, José Roberto @@aut@@ Neto, Pedro José Rolim @@aut@@ de La Roca Soares, Mônica Felts @@aut@@ |
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However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. 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de Melo, Cybelly Marques de Medeiros Vieira, Amanda Carla Quintas da Silva do Nascimento, André Luiz Figueirêdo, Camila Bezerra Melo Rolim, Larissa Araújo Soares-Sobrinho, José Lamartine Veras, Leiz Maria Costa de Souza de Almeida Leite, José Roberto Neto, Pedro José Rolim de La Roca Soares, Mônica Felts |
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a compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms |
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A compatibility study of the prototype epiisopiloturine and pharmaceutical excipients aiming at the attainment of solid pharmaceutical forms |
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Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. © Akadémiai Kiadó, Budapest, Hungary 2014 |
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Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. © Akadémiai Kiadó, Budapest, Hungary 2014 |
| abstract_unstemmed |
Abstract Epiisopiloturine (EPI) is an alkaloid extracted from pilocarpine production residue that has shown promising activity for neglected illnesses like Schistosomiasis and Leishmaniasis according to in vitro studies carried out since 2009. However, its physical–chemical characteristics and its behavior in the presence of certain situations have been little explored. Since this approach provides support to the acquisition of pharmaceutical products from this molecule, this study has aimed at identifying and characterizing, through physical–chemical studies, EPI, besides evaluating its physical–chemical compatibility in the presence of excipients for solid formulations. The identification of the raw material was carried out through infrared spectroscopy. Its physical–chemical characterization was conducted using x-ray diffraction and thermal analysis thermogravimetry (TG), differential thermogravimetry, and differential scanning calorimetry (DSC) curves, besides obtaining thermal/non-isothermal decay kinetics (TNIDK). Infrared confirmed the identity of the molecule. X-ray diffraction showed crystalline behavior, with the main peak expressing at 11.1°(2θ). From the DSC curve and TG, its melting range was identified at 221.72–228.24 °C (∆E = −148.75 J $ g^{−1} $) and its initial decay temperature at 224 °C (∆m = 79.27 %), respectively, suggesting that EPI appears thermally stable. Starting from TNIDK activation energy parameters (−88.95 kJ $ mol^{−1} $), frequency factor (1.165 × $ 10^{8} $ $ min^{−1} $), and reaction order were made clear (1). Finally, in the thermal compatibility study, EPI showed to be compatible with excipients such as starch, lactose, PVP K-30, microcrystalline cellulose, and hydroxypropyl methyl cellulose. Thus, the results presented serve as support for future directed research, based on EPI, for development of solid formulations. © Akadémiai Kiadó, Budapest, Hungary 2014 |
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