Aqueous and hydro-alcoholic media effects on polyols

Kofi Asare-Addo, Barbara R Conway, Mohamed J Hajamohaideen, Waseem Kaialy, Ali Nokhodchi, El Hassanne Larhrib

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

The ingestion of drug products with alcohol can have an adverse effect on drug levels in a patient's blood. The Food and Drug Agency (FDA) issued an alert in 2005 after hydromorphone was withdrawn from the market after clinical trials showed ingestion with alcohol to potentially result in lethal drug peak plasma concentrations. The potential impact of alcohol on extended release (ER) tablet matrices and the need to develop ER matrices robust to alcohol effects has then been of interest. This study investigated the compaction properties of polyols and their effect on drug release. Polyols (erythritol, xylitol, mannitol and maltitol) with increasing hydroxyl groups were used as diluents for HPMC matrices containing theophylline. Release profiles were determined in pH 1.2 and 6.8 dissolution media with hydro-alcoholic concentrations of 5-40%. Increases in the polyols' hydroxyl groups brought about an increase in tablet strength and a decrease in the drug release rates. This is likely due to stronger bond formation with increasing hydroxyls. The impact of alcohol on drug release was studied further for maltitol formulations. Maltitol was resilient to the presence of ethanol (5-40% v/v) at pH 1.2 (f2=57-74) but not at pH 6.8 (f2=36-48). Drug release was not different above 5% alcohol concentration at pH 6.8. The results of this in vitro study suggest that ethanol concentrations as high as 40% do not substantially alter the drug release properties of theophylline from maltitol matrix tablets. However, care and consideration should be given to the choice of polyol or mixture of polyols in obtaining a desired drug release profile.

Original languageEnglish
Pages (from-to)24-9
Number of pages6
JournalColloids and Surfaces B: Biointerfaces
Volume111
DOIs
Publication statusPublished - 1 Nov 2013

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Polyols
drugs
Alcohols
alcohols
Pharmaceutical Preparations
Hydroxyl Radical
Tablets
tablets
Theophylline
Ethanol
Eating
ingestion
Hydromorphone
Erythritol
Xylitol
matrices
Mannitol
ethyl alcohol
Drug products
Drug Liberation

Cite this

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title = "Aqueous and hydro-alcoholic media effects on polyols",
abstract = "The ingestion of drug products with alcohol can have an adverse effect on drug levels in a patient's blood. The Food and Drug Agency (FDA) issued an alert in 2005 after hydromorphone was withdrawn from the market after clinical trials showed ingestion with alcohol to potentially result in lethal drug peak plasma concentrations. The potential impact of alcohol on extended release (ER) tablet matrices and the need to develop ER matrices robust to alcohol effects has then been of interest. This study investigated the compaction properties of polyols and their effect on drug release. Polyols (erythritol, xylitol, mannitol and maltitol) with increasing hydroxyl groups were used as diluents for HPMC matrices containing theophylline. Release profiles were determined in pH 1.2 and 6.8 dissolution media with hydro-alcoholic concentrations of 5-40{\%}. Increases in the polyols' hydroxyl groups brought about an increase in tablet strength and a decrease in the drug release rates. This is likely due to stronger bond formation with increasing hydroxyls. The impact of alcohol on drug release was studied further for maltitol formulations. Maltitol was resilient to the presence of ethanol (5-40{\%} v/v) at pH 1.2 (f2=57-74) but not at pH 6.8 (f2=36-48). Drug release was not different above 5{\%} alcohol concentration at pH 6.8. The results of this in vitro study suggest that ethanol concentrations as high as 40{\%} do not substantially alter the drug release properties of theophylline from maltitol matrix tablets. However, care and consideration should be given to the choice of polyol or mixture of polyols in obtaining a desired drug release profile.",
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author = "Kofi Asare-Addo and Conway, {Barbara R} and Hajamohaideen, {Mohamed J} and Waseem Kaialy and Ali Nokhodchi and Larhrib, {El Hassanne}",
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language = "English",
volume = "111",
pages = "24--9",
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Aqueous and hydro-alcoholic media effects on polyols. / Asare-Addo, Kofi; Conway, Barbara R; Hajamohaideen, Mohamed J; Kaialy, Waseem; Nokhodchi, Ali; Larhrib, El Hassanne.

In: Colloids and Surfaces B: Biointerfaces, Vol. 111, 01.11.2013, p. 24-9.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Aqueous and hydro-alcoholic media effects on polyols

AU - Asare-Addo, Kofi

AU - Conway, Barbara R

AU - Hajamohaideen, Mohamed J

AU - Kaialy, Waseem

AU - Nokhodchi, Ali

AU - Larhrib, El Hassanne

N1 - Copyright © 2013 Elsevier B.V. All rights reserved.

PY - 2013/11/1

Y1 - 2013/11/1

N2 - The ingestion of drug products with alcohol can have an adverse effect on drug levels in a patient's blood. The Food and Drug Agency (FDA) issued an alert in 2005 after hydromorphone was withdrawn from the market after clinical trials showed ingestion with alcohol to potentially result in lethal drug peak plasma concentrations. The potential impact of alcohol on extended release (ER) tablet matrices and the need to develop ER matrices robust to alcohol effects has then been of interest. This study investigated the compaction properties of polyols and their effect on drug release. Polyols (erythritol, xylitol, mannitol and maltitol) with increasing hydroxyl groups were used as diluents for HPMC matrices containing theophylline. Release profiles were determined in pH 1.2 and 6.8 dissolution media with hydro-alcoholic concentrations of 5-40%. Increases in the polyols' hydroxyl groups brought about an increase in tablet strength and a decrease in the drug release rates. This is likely due to stronger bond formation with increasing hydroxyls. The impact of alcohol on drug release was studied further for maltitol formulations. Maltitol was resilient to the presence of ethanol (5-40% v/v) at pH 1.2 (f2=57-74) but not at pH 6.8 (f2=36-48). Drug release was not different above 5% alcohol concentration at pH 6.8. The results of this in vitro study suggest that ethanol concentrations as high as 40% do not substantially alter the drug release properties of theophylline from maltitol matrix tablets. However, care and consideration should be given to the choice of polyol or mixture of polyols in obtaining a desired drug release profile.

AB - The ingestion of drug products with alcohol can have an adverse effect on drug levels in a patient's blood. The Food and Drug Agency (FDA) issued an alert in 2005 after hydromorphone was withdrawn from the market after clinical trials showed ingestion with alcohol to potentially result in lethal drug peak plasma concentrations. The potential impact of alcohol on extended release (ER) tablet matrices and the need to develop ER matrices robust to alcohol effects has then been of interest. This study investigated the compaction properties of polyols and their effect on drug release. Polyols (erythritol, xylitol, mannitol and maltitol) with increasing hydroxyl groups were used as diluents for HPMC matrices containing theophylline. Release profiles were determined in pH 1.2 and 6.8 dissolution media with hydro-alcoholic concentrations of 5-40%. Increases in the polyols' hydroxyl groups brought about an increase in tablet strength and a decrease in the drug release rates. This is likely due to stronger bond formation with increasing hydroxyls. The impact of alcohol on drug release was studied further for maltitol formulations. Maltitol was resilient to the presence of ethanol (5-40% v/v) at pH 1.2 (f2=57-74) but not at pH 6.8 (f2=36-48). Drug release was not different above 5% alcohol concentration at pH 6.8. The results of this in vitro study suggest that ethanol concentrations as high as 40% do not substantially alter the drug release properties of theophylline from maltitol matrix tablets. However, care and consideration should be given to the choice of polyol or mixture of polyols in obtaining a desired drug release profile.

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KW - Ethanol

KW - Hypromellose Derivatives

KW - Maltose

KW - Mannitol

KW - Polymers

KW - Sugar Alcohols

KW - Tablets

KW - Theophylline

KW - Water

KW - Xylitol

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

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DO - 10.1016/j.colsurfb.2013.05.003

M3 - Article

VL - 111

SP - 24

EP - 29

JO - Colloids and Surfaces B: Biointerfaces

JF - Colloids and Surfaces B: Biointerfaces

SN - 0927-7765

ER -