Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts

Substances in the form of weak acid salts have been found to be problematic for dissolution testing. Their absorption can start only after they are turned into the form of an acid following the gastric passage although they were administered in the form of a salt. Due to poor solubility, they cannot...

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Main Authors: Franc Aleš, Muselłk Jan, Goněc Roman, Vetchý David
Format: Article
Language:English
Published: Sciendo 2016-03-01
Series:Acta Pharmaceutica
Subjects:
Online Access:https://doi.org/10.1515/acph-2016-0010
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author Franc Aleš
Muselłk Jan
Goněc Roman
Vetchý David
author_facet Franc Aleš
Muselłk Jan
Goněc Roman
Vetchý David
author_sort Franc Aleš
collection DOAJ
description Substances in the form of weak acid salts have been found to be problematic for dissolution testing. Their absorption can start only after they are turned into the form of an acid following the gastric passage although they were administered in the form of a salt. Due to poor solubility, they cannot be tested in acidic gastric environment for a biased dissolution profile. The biphasic dissolution method is promising for overcoming this obstacle. Tablets with warfarin clathrate sodium salt in two concentrations and two different particle size distributions were tested as a suitable model for finding the medium and process conditions of dissolution. The dissolution method based on the use of the upper organic layer (1-octanol) and the lower aqueous layer 0.1 mol L−1 HCl) was found suitable and discriminatory for tablets containing active substances in the form of salts of weak acids. The method also reflects physical differences in the quality of used substances.
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institution Kabale University
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publishDate 2016-03-01
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series Acta Pharmaceutica
spelling doaj-art-defeca3b26a448c5bd3709df7808d4f52025-02-02T09:44:15ZengSciendoActa Pharmaceutica1846-95582016-03-0166113914510.1515/acph-2016-0010acph-2016-0010Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid saltsFranc Aleš0Muselłk Jan1Goněc Roman2Vetchý David3 Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Brno, Czech Republic Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Brno, Czech Republic Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Brno, Czech Republic Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Brno, Czech RepublicSubstances in the form of weak acid salts have been found to be problematic for dissolution testing. Their absorption can start only after they are turned into the form of an acid following the gastric passage although they were administered in the form of a salt. Due to poor solubility, they cannot be tested in acidic gastric environment for a biased dissolution profile. The biphasic dissolution method is promising for overcoming this obstacle. Tablets with warfarin clathrate sodium salt in two concentrations and two different particle size distributions were tested as a suitable model for finding the medium and process conditions of dissolution. The dissolution method based on the use of the upper organic layer (1-octanol) and the lower aqueous layer 0.1 mol L−1 HCl) was found suitable and discriminatory for tablets containing active substances in the form of salts of weak acids. The method also reflects physical differences in the quality of used substances.https://doi.org/10.1515/acph-2016-0010weak acid saltswarfarin sodiumdissolution method
spellingShingle Franc Aleš
Muselłk Jan
Goněc Roman
Vetchý David
Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
Acta Pharmaceutica
weak acid salts
warfarin sodium
dissolution method
title Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
title_full Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
title_fullStr Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
title_full_unstemmed Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
title_short Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
title_sort biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts
topic weak acid salts
warfarin sodium
dissolution method
url https://doi.org/10.1515/acph-2016-0010
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