Albendazole-cyclodextrins binary systems

Thermal and spectral investigation on drug-excipient interaction

Cristina Trandafirescu, Ionuţ Ledeţi, Codruţa Şoica, Adriana Ledeţi, Gabriela Vlase, Florin Borcan, Cristina Dehelean, Dorina Coricovac, Roxana Racoviceanu, Z. Aigner

Research output: Article

Abstract

The aim of this study was to characterize the interaction between the binary systems of albendazole (ABZ)—cyclodextrins (CDs) with pharmaceutical excipients. Hydroxyl-propyl-beta-cyclodextrin (HPBCD) and random methyl-beta-cyclodextrin (RAMEB) were used as cyclodextrins and magnesium stearate, mannitol, polyvinylpyrrolidone K30 (PVP K30), colloidal silica, starch, and talc were used as excipients. The utilized investigation techniques were attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), powder X-ray diffractometry (PXRD) and thermoanalytical techniques: thermogravimetry (TG)/derivative thermogravimetry (DTG)/heat flow (HF) and differential scanning calorimetry (DSC). The ATR-FTIR analysis clearly suggested interactions under ambient conditions between ABZ-HPBCD with PVP K30 and SiO 2 and between ABZ-RAMEB with SiO 2 and talc. The PXRD patterns indicated the formation of less crystalline mixtures but with no clear indication of interactions, since no peaks appeared nor disappeared. The modifications on the DSC curves suggested an interaction between ABZ-HPBCD and PVP K30 and SiO 2 respectively, and in case of ABZ-RAMEB was observed an interaction with talc. Thermal analysis (TG/DTG/HF) carried out in open crucibles in dynamic air atmosphere suggested that at temperatures over 40 °C dehydration of samples occurred, later followed by thermolysis and appearance of interactions in all studied cases. Our study concludes by recommending precautionary measures in elaborating new solid formulations containing ABZ, HPBCD and PVP K30/SiO 2 and for the ones containing ABZ, RAMEB and Talc/SiO 2 , due to the present interactions under ambient conditions.

Original languageEnglish
JournalJournal of Thermal Analysis and Calorimetry
DOIs
Publication statusPublished - jan. 1 2019

Fingerprint

Drug interactions
Albendazole
Excipients
Cyclodextrins
drugs
Talc
Povidone
talc
thermogravimetry
Hydroxyl Radical
Thermogravimetric analysis
interactions
heat transmission
Powders
X ray diffraction analysis
Differential scanning calorimetry
heat measurement
infrared spectroscopy
mannitol
Heat transfer

ASJC Scopus subject areas

  • Condensed Matter Physics
  • Physical and Theoretical Chemistry

Cite this

Albendazole-cyclodextrins binary systems : Thermal and spectral investigation on drug-excipient interaction. / Trandafirescu, Cristina; Ledeţi, Ionuţ; Şoica, Codruţa; Ledeţi, Adriana; Vlase, Gabriela; Borcan, Florin; Dehelean, Cristina; Coricovac, Dorina; Racoviceanu, Roxana; Aigner, Z.

In: Journal of Thermal Analysis and Calorimetry, 01.01.2019.

Research output: Article

Trandafirescu, Cristina ; Ledeţi, Ionuţ ; Şoica, Codruţa ; Ledeţi, Adriana ; Vlase, Gabriela ; Borcan, Florin ; Dehelean, Cristina ; Coricovac, Dorina ; Racoviceanu, Roxana ; Aigner, Z. / Albendazole-cyclodextrins binary systems : Thermal and spectral investigation on drug-excipient interaction. In: Journal of Thermal Analysis and Calorimetry. 2019.
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abstract = "The aim of this study was to characterize the interaction between the binary systems of albendazole (ABZ)—cyclodextrins (CDs) with pharmaceutical excipients. Hydroxyl-propyl-beta-cyclodextrin (HPBCD) and random methyl-beta-cyclodextrin (RAMEB) were used as cyclodextrins and magnesium stearate, mannitol, polyvinylpyrrolidone K30 (PVP K30), colloidal silica, starch, and talc were used as excipients. The utilized investigation techniques were attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), powder X-ray diffractometry (PXRD) and thermoanalytical techniques: thermogravimetry (TG)/derivative thermogravimetry (DTG)/heat flow (HF) and differential scanning calorimetry (DSC). The ATR-FTIR analysis clearly suggested interactions under ambient conditions between ABZ-HPBCD with PVP K30 and SiO 2 and between ABZ-RAMEB with SiO 2 and talc. The PXRD patterns indicated the formation of less crystalline mixtures but with no clear indication of interactions, since no peaks appeared nor disappeared. The modifications on the DSC curves suggested an interaction between ABZ-HPBCD and PVP K30 and SiO 2 respectively, and in case of ABZ-RAMEB was observed an interaction with talc. Thermal analysis (TG/DTG/HF) carried out in open crucibles in dynamic air atmosphere suggested that at temperatures over 40 °C dehydration of samples occurred, later followed by thermolysis and appearance of interactions in all studied cases. Our study concludes by recommending precautionary measures in elaborating new solid formulations containing ABZ, HPBCD and PVP K30/SiO 2 and for the ones containing ABZ, RAMEB and Talc/SiO 2 , due to the present interactions under ambient conditions.",
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author = "Cristina Trandafirescu and Ionuţ Ledeţi and Codruţa Şoica and Adriana Ledeţi and Gabriela Vlase and Florin Borcan and Cristina Dehelean and Dorina Coricovac and Roxana Racoviceanu and Z. Aigner",
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T2 - Thermal and spectral investigation on drug-excipient interaction

AU - Trandafirescu, Cristina

AU - Ledeţi, Ionuţ

AU - Şoica, Codruţa

AU - Ledeţi, Adriana

AU - Vlase, Gabriela

AU - Borcan, Florin

AU - Dehelean, Cristina

AU - Coricovac, Dorina

AU - Racoviceanu, Roxana

AU - Aigner, Z.

PY - 2019/1/1

Y1 - 2019/1/1

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AB - The aim of this study was to characterize the interaction between the binary systems of albendazole (ABZ)—cyclodextrins (CDs) with pharmaceutical excipients. Hydroxyl-propyl-beta-cyclodextrin (HPBCD) and random methyl-beta-cyclodextrin (RAMEB) were used as cyclodextrins and magnesium stearate, mannitol, polyvinylpyrrolidone K30 (PVP K30), colloidal silica, starch, and talc were used as excipients. The utilized investigation techniques were attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), powder X-ray diffractometry (PXRD) and thermoanalytical techniques: thermogravimetry (TG)/derivative thermogravimetry (DTG)/heat flow (HF) and differential scanning calorimetry (DSC). The ATR-FTIR analysis clearly suggested interactions under ambient conditions between ABZ-HPBCD with PVP K30 and SiO 2 and between ABZ-RAMEB with SiO 2 and talc. The PXRD patterns indicated the formation of less crystalline mixtures but with no clear indication of interactions, since no peaks appeared nor disappeared. The modifications on the DSC curves suggested an interaction between ABZ-HPBCD and PVP K30 and SiO 2 respectively, and in case of ABZ-RAMEB was observed an interaction with talc. Thermal analysis (TG/DTG/HF) carried out in open crucibles in dynamic air atmosphere suggested that at temperatures over 40 °C dehydration of samples occurred, later followed by thermolysis and appearance of interactions in all studied cases. Our study concludes by recommending precautionary measures in elaborating new solid formulations containing ABZ, HPBCD and PVP K30/SiO 2 and for the ones containing ABZ, RAMEB and Talc/SiO 2 , due to the present interactions under ambient conditions.

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KW - Compatibility study

KW - Cyclodextrins

KW - Pharmaceutical excipients

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