The influence of ethanol on superdisintegrants and on tablets disintegration

Lorina Bisharat; Hatim S. AlKhatib; Suha Muhaissen; Julian Quodbach; Anaheed Blaibleh; Marco Cespi; Alberto Berardi

doi:10.1016/j.ejps.2019.01.004

The influence of ethanol on superdisintegrants and on tablets disintegration

Lorina Bisharat, Hatim S. AlKhatib, Suha Muhaissen, Julian Quodbach, Anaheed Blaibleh, Marco Cespi, Alberto Berardi^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › Academic › peer-review

Abstract

Disintegration of immediate release tablets originates from the volume expansion of disintegrants within the formulation. Here, we study the impact of ethanol on the disintegrant expansion and on tablets disintegration. The three most commonly used superdisintegrants, namely sodium starch glycolate (SSG), crospovidone (PVPP) and croscarmellose sodium (CCS) were investigated alone and incorporated in dicalcium phosphate and in drug-containing tablets. High (i.e. 40%), but not moderate (i.e. 10%), aqueous ethanol concentrations reduce the size expansion of the three disintegrants compared to water. This “ethanol effect” is the greatest for SSG, followed by CCS and then PVPP. Moreover, the presence of ethanol in the media can significantly influence the disintegration time of drug-containing tablets via affecting both the disintegrant action itself and the drug solubility. For example, the disintegration time of theophylline tablets containing SSG is 8.1-fold greater in 40% aqueous ethanol compared to water. Overall, this study brought to light the existence of a potentially significant interference of alcohol with the disintegration phenomenon, suggesting that the concomitant administration of tablets and intake of alcoholic beverages may affect, in some cases, tablets disintegration. More studies are now needed to verify the importance of the “ethanol effect” on disintegration of commercial dosage forms. Our findings also suggest that PVPP is the disintegrant that is the least affected by alcohol.

Original language	English
Pages (from-to)	140-147
Number of pages	8
Journal	European Journal of Pharmaceutical Sciences
Volume	129
DOIs	https://doi.org/10.1016/j.ejps.2019.01.004
Publication status	Published - 1 Mar 2019
Externally published	Yes

Bibliographical note

Funding Information:
The authors thank the Applied Science Private University , Jordan and The University of Jordan , Jordan for the financial support. The authors are also grateful to Ms. Abeer Al-Salahat and Ms. Sara Bisharat for helping in data acquisition.

Publisher Copyright:
© 2019 Elsevier B.V.

Funding

The authors thank the Applied Science Private University , Jordan and The University of Jordan , Jordan for the financial support. The authors are also grateful to Ms. Abeer Al-Salahat and Ms. Sara Bisharat for helping in data acquisition.

Keywords

Disintegration
Drug solubility
Ethanol
Image analysis
Superdisintegrants
Swelling

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10.1016/j.ejps.2019.01.004

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title = "The influence of ethanol on superdisintegrants and on tablets disintegration",

abstract = "Disintegration of immediate release tablets originates from the volume expansion of disintegrants within the formulation. Here, we study the impact of ethanol on the disintegrant expansion and on tablets disintegration. The three most commonly used superdisintegrants, namely sodium starch glycolate (SSG), crospovidone (PVPP) and croscarmellose sodium (CCS) were investigated alone and incorporated in dicalcium phosphate and in drug-containing tablets. High (i.e. 40%), but not moderate (i.e. 10%), aqueous ethanol concentrations reduce the size expansion of the three disintegrants compared to water. This “ethanol effect” is the greatest for SSG, followed by CCS and then PVPP. Moreover, the presence of ethanol in the media can significantly influence the disintegration time of drug-containing tablets via affecting both the disintegrant action itself and the drug solubility. For example, the disintegration time of theophylline tablets containing SSG is 8.1-fold greater in 40% aqueous ethanol compared to water. Overall, this study brought to light the existence of a potentially significant interference of alcohol with the disintegration phenomenon, suggesting that the concomitant administration of tablets and intake of alcoholic beverages may affect, in some cases, tablets disintegration. More studies are now needed to verify the importance of the “ethanol effect” on disintegration of commercial dosage forms. Our findings also suggest that PVPP is the disintegrant that is the least affected by alcohol.",

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author = "Lorina Bisharat and AlKhatib, {Hatim S.} and Suha Muhaissen and Julian Quodbach and Anaheed Blaibleh and Marco Cespi and Alberto Berardi",

note = "Funding Information: The authors thank the Applied Science Private University , Jordan and The University of Jordan , Jordan for the financial support. The authors are also grateful to Ms. Abeer Al-Salahat and Ms. Sara Bisharat for helping in data acquisition. Publisher Copyright: {\textcopyright} 2019 Elsevier B.V.",

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AU - Bisharat, Lorina

AU - AlKhatib, Hatim S.

AU - Muhaissen, Suha

AU - Quodbach, Julian

AU - Blaibleh, Anaheed

AU - Cespi, Marco

AU - Berardi, Alberto

N1 - Funding Information: The authors thank the Applied Science Private University , Jordan and The University of Jordan , Jordan for the financial support. The authors are also grateful to Ms. Abeer Al-Salahat and Ms. Sara Bisharat for helping in data acquisition. Publisher Copyright: © 2019 Elsevier B.V.

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N2 - Disintegration of immediate release tablets originates from the volume expansion of disintegrants within the formulation. Here, we study the impact of ethanol on the disintegrant expansion and on tablets disintegration. The three most commonly used superdisintegrants, namely sodium starch glycolate (SSG), crospovidone (PVPP) and croscarmellose sodium (CCS) were investigated alone and incorporated in dicalcium phosphate and in drug-containing tablets. High (i.e. 40%), but not moderate (i.e. 10%), aqueous ethanol concentrations reduce the size expansion of the three disintegrants compared to water. This “ethanol effect” is the greatest for SSG, followed by CCS and then PVPP. Moreover, the presence of ethanol in the media can significantly influence the disintegration time of drug-containing tablets via affecting both the disintegrant action itself and the drug solubility. For example, the disintegration time of theophylline tablets containing SSG is 8.1-fold greater in 40% aqueous ethanol compared to water. Overall, this study brought to light the existence of a potentially significant interference of alcohol with the disintegration phenomenon, suggesting that the concomitant administration of tablets and intake of alcoholic beverages may affect, in some cases, tablets disintegration. More studies are now needed to verify the importance of the “ethanol effect” on disintegration of commercial dosage forms. Our findings also suggest that PVPP is the disintegrant that is the least affected by alcohol.

AB - Disintegration of immediate release tablets originates from the volume expansion of disintegrants within the formulation. Here, we study the impact of ethanol on the disintegrant expansion and on tablets disintegration. The three most commonly used superdisintegrants, namely sodium starch glycolate (SSG), crospovidone (PVPP) and croscarmellose sodium (CCS) were investigated alone and incorporated in dicalcium phosphate and in drug-containing tablets. High (i.e. 40%), but not moderate (i.e. 10%), aqueous ethanol concentrations reduce the size expansion of the three disintegrants compared to water. This “ethanol effect” is the greatest for SSG, followed by CCS and then PVPP. Moreover, the presence of ethanol in the media can significantly influence the disintegration time of drug-containing tablets via affecting both the disintegrant action itself and the drug solubility. For example, the disintegration time of theophylline tablets containing SSG is 8.1-fold greater in 40% aqueous ethanol compared to water. Overall, this study brought to light the existence of a potentially significant interference of alcohol with the disintegration phenomenon, suggesting that the concomitant administration of tablets and intake of alcoholic beverages may affect, in some cases, tablets disintegration. More studies are now needed to verify the importance of the “ethanol effect” on disintegration of commercial dosage forms. Our findings also suggest that PVPP is the disintegrant that is the least affected by alcohol.

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ER -

The influence of ethanol on superdisintegrants and on tablets disintegration

Abstract

Bibliographical note

Funding

Keywords

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