Strategies to overcome pH-dependent solubility of weakly basic drugs by using different types of alginates

Drug Development and Industrial Pharmacy
S GutscheH Kranz

Abstract

Weakly basic drugs demonstrate higher solubility at lower pH, thus often leading to faster drug release at lower pH. The objective of this study was to achieve pH-independent release of weakly basic drugs from extended release formulations based on the naturally occurring polymer sodium alginate. Three approaches to overcome the pH-dependent solubility of the weakly basic model drug verapamil hydrochloride were investigated. First, matrix tablets were prepared by direct compression of drug substance with different types of sodium alginate only. Second, pH-modifiers were added to the drug/alginate matrix systems. Third, press-coated tablets consisting of an inner pH-modifier tablet core and an outer drug/sodium alginate coat were prepared. pH-Independent drug release was achieved from matrix tablets consisting of selected alginates and drug substance only. Alginates are better soluble at higher pH. Therefore, they are able to compensate the poor solubility of weakly basic drugs at higher pH as the matrix of the tablets dissolves faster. This approach was successful when using alginates that demonstrated fast hydration and erosion at higher pH. The approach failed for alginates with less-pronounced erosion at higher pH. The addit...Continue Reading

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Citations

Jan 11, 2011·Indian Journal of Pharmaceutical Sciences·N R KotagaleM J Umekar
Mar 30, 2010·Drug Development and Industrial Pharmacy·Fa-Qin WangQin Wei
Oct 13, 2010·International Journal of Pharmaceutics·Friederike EisenächerKarsten Mäder
Aug 16, 2015·International Journal of Pharmaceutics·Nizar Al-ZoubiStavros Malamataris
Oct 16, 2012·Biopharmaceutics & Drug Disposition·Sarah J NicholsonIan Wilding
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter

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