Formulation strategies for mitigating dissolution reduction of p-aminobenzoic acid by sodium lauryl sulfate through diffusion layer modulation

Yiwang Guo; Changquan Calvin Sun

doi:10.1016/j.ijpharm.2021.121310

Formulation strategies for mitigating dissolution reduction of p-aminobenzoic acid by sodium lauryl sulfate through diffusion layer modulation

Yiwang Guo, Changquan Calvin Sun

Pharmaceutics

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

3 Scopus citations

Abstract

The use of the surfactant, sodium lauryl sulfate (SLS), instead of enhancing drug dissolution, deteriorates the dissolution of some alkaline drugs through forming poorly soluble lauryl sulfate salts. The thermodynamic driving force for precipitation of such salts is the ratio of ion product in solution (Q) to the solubility product of the salt (K_sp). In this work, we have examined two formulation strategies for mitigating the negative effect of SLS on the dissolution of p-aminobenzoic acid (PABA) by reducing the Q value of its LS salt in the diffusion layer: 1) introducing alkalizing excipient, Na₃PO₄, to reduce the concentration of PABAH⁺ by elevating the microenvironment pH, and 2) introducing NaCl to reduce the LS^- monomer concentration by depressing the critical micelle concentration (CMC) of SLS.

Original language	English (US)
Article number	121310
Journal	International journal of pharmaceutics
Volume	611
DOIs	https://doi.org/10.1016/j.ijpharm.2021.121310
State	Published - Jan 5 2022

Bibliographical note

Funding Information:
Y.G. thanks the Graduate School of the University of Minnesota for a Doctoral Dissertation Fellowship (2020 – 2021) and the Department of Pharmaceutics, University of Minnesota for a David J.W. Grant & Marilyn J. Grant Fellowship in Physical Pharmacy (2020 – 2021). We also thank Gerrit Vreeman for performing the non-linear regression of pH-solubility data.

Publisher Copyright:
© 2021 Elsevier B.V.

Keywords

Diffusion layer
Dissolution
P-aminobenzoic acid
Sodium lauryl sulfate
Tablet formulation

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title = "Formulation strategies for mitigating dissolution reduction of p-aminobenzoic acid by sodium lauryl sulfate through diffusion layer modulation",

abstract = "The use of the surfactant, sodium lauryl sulfate (SLS), instead of enhancing drug dissolution, deteriorates the dissolution of some alkaline drugs through forming poorly soluble lauryl sulfate salts. The thermodynamic driving force for precipitation of such salts is the ratio of ion product in solution (Q) to the solubility product of the salt (Ksp). In this work, we have examined two formulation strategies for mitigating the negative effect of SLS on the dissolution of p-aminobenzoic acid (PABA) by reducing the Q value of its LS salt in the diffusion layer: 1) introducing alkalizing excipient, Na3PO4, to reduce the concentration of PABAH+ by elevating the microenvironment pH, and 2) introducing NaCl to reduce the LS- monomer concentration by depressing the critical micelle concentration (CMC) of SLS.",

keywords = "Diffusion layer, Dissolution, P-aminobenzoic acid, Sodium lauryl sulfate, Tablet formulation",

author = "Yiwang Guo and Sun, {Changquan Calvin}",

note = "Funding Information: Y.G. thanks the Graduate School of the University of Minnesota for a Doctoral Dissertation Fellowship (2020 – 2021) and the Department of Pharmaceutics, University of Minnesota for a David J.W. Grant & Marilyn J. Grant Fellowship in Physical Pharmacy (2020 – 2021). We also thank Gerrit Vreeman for performing the non-linear regression of pH-solubility data. Publisher Copyright: {\textcopyright} 2021 Elsevier B.V.",

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AU - Sun, Changquan Calvin

N1 - Funding Information: Y.G. thanks the Graduate School of the University of Minnesota for a Doctoral Dissertation Fellowship (2020 – 2021) and the Department of Pharmaceutics, University of Minnesota for a David J.W. Grant & Marilyn J. Grant Fellowship in Physical Pharmacy (2020 – 2021). We also thank Gerrit Vreeman for performing the non-linear regression of pH-solubility data. Publisher Copyright: © 2021 Elsevier B.V.

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Y1 - 2022/1/5

N2 - The use of the surfactant, sodium lauryl sulfate (SLS), instead of enhancing drug dissolution, deteriorates the dissolution of some alkaline drugs through forming poorly soluble lauryl sulfate salts. The thermodynamic driving force for precipitation of such salts is the ratio of ion product in solution (Q) to the solubility product of the salt (Ksp). In this work, we have examined two formulation strategies for mitigating the negative effect of SLS on the dissolution of p-aminobenzoic acid (PABA) by reducing the Q value of its LS salt in the diffusion layer: 1) introducing alkalizing excipient, Na3PO4, to reduce the concentration of PABAH+ by elevating the microenvironment pH, and 2) introducing NaCl to reduce the LS- monomer concentration by depressing the critical micelle concentration (CMC) of SLS.

AB - The use of the surfactant, sodium lauryl sulfate (SLS), instead of enhancing drug dissolution, deteriorates the dissolution of some alkaline drugs through forming poorly soluble lauryl sulfate salts. The thermodynamic driving force for precipitation of such salts is the ratio of ion product in solution (Q) to the solubility product of the salt (Ksp). In this work, we have examined two formulation strategies for mitigating the negative effect of SLS on the dissolution of p-aminobenzoic acid (PABA) by reducing the Q value of its LS salt in the diffusion layer: 1) introducing alkalizing excipient, Na3PO4, to reduce the concentration of PABAH+ by elevating the microenvironment pH, and 2) introducing NaCl to reduce the LS- monomer concentration by depressing the critical micelle concentration (CMC) of SLS.

KW - Diffusion layer

KW - Dissolution

KW - P-aminobenzoic acid

KW - Sodium lauryl sulfate

KW - Tablet formulation

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Formulation strategies for mitigating dissolution reduction of p-aminobenzoic acid by sodium lauryl sulfate through diffusion layer modulation

Abstract

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