The influence of protonation ratio on properties of carboxymethyl starch excipient at various substitution degrees: Structural insights and drug release kinetics

International Journal of Pharmaceutics
E Assaad, M A Mateescu

Abstract

Carboxymethyl starch (CMS) with pH sensitivity modulated by the protonation ratio (PR 0-100%) and the degree of substitution (DS 0.07-0.20) was synthesized in aqueous medium. The properties of CMS excipient and the mechanism of acetaminophen release from monolithic tablets in simulated gastric fluid (SGF, pH 1.2) and in simulated intestinal fluid (SIF, pH 6.8) were investigated. Compared to sodium CMS, the protonated CMS provided a longer release time which increases with the increase of PR. Over storage time, the highly protonated CMS showed a decrease in solubility and a progressive structural alteration due to hydrogen bonded carboxyl groups. Simultaneously, an acceleration of release rate of formulated drug was observed. The CMS(DS 0.11) with PR up to 50% showed relatively low sensitivity to dissolution medium pH and sustained release pattern almost independent of tablet preincubation in SGF and of drug loading (20% and 40%). The CMS(DS 0.20) was more sensitive to pH and showed an accelerated release rate in SIF. For the CMS formulations, a diffusion mechanism was suggested in SGF, whereas in SIF the release was mostly controlled by swelling and erosion.

References

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Jun 14, 2002·International Journal of Pharmaceutics·S EdgeJ N Staniforth
Nov 16, 2004·Colloids and Surfaces. B, Biointerfaces·Tomofumi HaradaMasayuki Tokita
Jun 1, 2007·International Journal of Pharmaceutics·Carmen CalinescuMircea-Alexandru Mateescu
Jan 24, 2009·Biomaterials·Lan WeiTao Chen

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Citations

Apr 9, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Maria Mihaela FriciuMircea Alexandru Mateescu
Jan 28, 2014·Colloids and Surfaces. B, Biointerfaces·Jinlong YangXinjie Zhang
Dec 25, 2015·Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society·Sonia Lefnaoui, Nadji Moulai-Mostefa
Apr 8, 2017·Drug Delivery and Translational Research·Tien Canh Le, Mircea Alexandru Mateescu
Oct 1, 2016·AAPS PharmSciTech·Pompilia Ispas-SzaboMircea Alexandru Mateescu
Mar 18, 2015·Biotechnology and Applied Biochemistry·Lindsay BlemurMircea Alexandru Mateescu
Jun 5, 2019·Pharmaceutics·Nassim BenyerbahMircea Alexandru Mateescu
Oct 5, 2011·Journal of Biomaterials Science. Polymer Edition·Elias AssaadMircea Alexandru Mateescu
Feb 18, 2021·Carbohydrate Polymers·Malihe Pooresmaeil, Hassan Namazi
Jul 17, 2020·International Journal of Biological Macromolecules·Leire UrbinaAloña Retegi
Sep 29, 2020·Journal of Pharmaceutical Sciences·Kouadio Victorien KonanMircea Alexandru Mateescu

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