The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution

Julie L. Calahan; Shubhajit Paul; Evelyn G. Yanez; Daniel DeNeve; Changquan C. Sun; Eric J. Munson

doi:10.1080/10837450.2020.1839763

The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution

Julie L. Calahan, Shubhajit Paul, Evelyn G. Yanez, Daniel DeNeve, Changquan C. Sun, Eric J. Munson

Pharmaceutics

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

8 Scopus citations

Abstract

Magnesium stearate (MgSt) is a widely used pharmaceutical lubricant in tablet manufacturing. However, batch-to-batch variability in hydrate form and surface area can lead to inconsistency in tablet performance. In this work, several unique MgSt samples were studied: traditional monohydrate samples with high surface area, dihydrate forms with high and low surface area, and disordered forms with low and medium water content. The effects of solid-state form and particle properties on lubrication efficiency, tabletability and dissolution were studied for tablets in a model direct compression formulation. It was found that the monohydrate and dihydrate forms had good lubrication efficiency compared to the disordered form, while the disordered form had the best tabletability. The dissolution rate correlated with surface area, where slower dissolution rates corresponded with higher MgSt surface areas. The dihydrate sample with lower surface area had the best performance for this model formulation, in terms of lubrication efficiency, tabletability and dissolution. Overall, it is concluded that the choice of the most appropriate grade of MgSt for a particular formulation depends on a comprehensive evaluation of the impact of MgSt properties on lubrication efficiency, tabletability and dissolution.

Original language	English (US)
Pages (from-to)	150-156
Number of pages	7
Journal	Pharmaceutical Development and Technology
Volume	26
Issue number	2
DOIs	https://doi.org/10.1080/10837450.2020.1839763
State	Published - Dec 10 2020

Bibliographical note

Funding Information:
The authors would like to thank Carl Huetteman for valuable discussions and assistance editing this paper. JLC was funded by a Pre-Doctoral Fellowship in Pharmaceutics from the PhRMA Foundation. The authors would also like to thank NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879, IIP-1540011 and industrial contributions) forfinancial support. Additionally, this material is based upon work supported by the National Science Foundation under Grant No.Grant No. 1710453.

Funding Information:
The authors would like to thank Carl Huetteman for valuable discussions and assistance editing this paper. JLC was funded by a Pre-Doctoral Fellowship in Pharmaceutics from the PhRMA Foundation. The authors would also like to thank NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879, IIP-1540011 and industrial contributions) forfinancial support. Additionally, this material is based upon work supported by the National Science Foundation under Grant No.Grant No. 1710453.

Publisher Copyright:
© 2020 Informa UK Limited, trading as Taylor & Francis Group.

Keywords

Magnesium stearate
compaction
dissolution
ejection force
lubrication
solid-state NMR
tensile strength

PubMed: MeSH publication types

Journal Article
Comparative Study

Publisher link

10.1080/10837450.2020.1839763

Find It

Find It at U of M Libraries

Cite this

@article{5eb7fabdf75f47b1a8fecbfc230645c4,

title = "The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution",

abstract = "Magnesium stearate (MgSt) is a widely used pharmaceutical lubricant in tablet manufacturing. However, batch-to-batch variability in hydrate form and surface area can lead to inconsistency in tablet performance. In this work, several unique MgSt samples were studied: traditional monohydrate samples with high surface area, dihydrate forms with high and low surface area, and disordered forms with low and medium water content. The effects of solid-state form and particle properties on lubrication efficiency, tabletability and dissolution were studied for tablets in a model direct compression formulation. It was found that the monohydrate and dihydrate forms had good lubrication efficiency compared to the disordered form, while the disordered form had the best tabletability. The dissolution rate correlated with surface area, where slower dissolution rates corresponded with higher MgSt surface areas. The dihydrate sample with lower surface area had the best performance for this model formulation, in terms of lubrication efficiency, tabletability and dissolution. Overall, it is concluded that the choice of the most appropriate grade of MgSt for a particular formulation depends on a comprehensive evaluation of the impact of MgSt properties on lubrication efficiency, tabletability and dissolution.",

keywords = "Magnesium stearate, compaction, dissolution, ejection force, lubrication, solid-state NMR, tensile strength",

author = "Calahan, {Julie L.} and Shubhajit Paul and Yanez, {Evelyn G.} and Daniel DeNeve and Sun, {Changquan C.} and Munson, {Eric J.}",

note = "Funding Information: The authors would like to thank Carl Huetteman for valuable discussions and assistance editing this paper. JLC was funded by a Pre-Doctoral Fellowship in Pharmaceutics from the PhRMA Foundation. The authors would also like to thank NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879, IIP-1540011 and industrial contributions) forfinancial support. Additionally, this material is based upon work supported by the National Science Foundation under Grant No.Grant No. 1710453. Funding Information: The authors would like to thank Carl Huetteman for valuable discussions and assistance editing this paper. JLC was funded by a Pre-Doctoral Fellowship in Pharmaceutics from the PhRMA Foundation. The authors would also like to thank NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879, IIP-1540011 and industrial contributions) forfinancial support. Additionally, this material is based upon work supported by the National Science Foundation under Grant No.Grant No. 1710453. Publisher Copyright: {\textcopyright} 2020 Informa UK Limited, trading as Taylor & Francis Group.",

year = "2020",

month = dec,

day = "10",

doi = "10.1080/10837450.2020.1839763",

language = "English (US)",

volume = "26",

pages = "150--156",

journal = "Pharmaceutical Development and Technology",

issn = "1083-7450",

publisher = "Informa Healthcare",

number = "2",

}

TY - JOUR

T1 - The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution

AU - Calahan, Julie L.

AU - Paul, Shubhajit

AU - Yanez, Evelyn G.

AU - DeNeve, Daniel

AU - Sun, Changquan C.

AU - Munson, Eric J.

N1 - Funding Information: The authors would like to thank Carl Huetteman for valuable discussions and assistance editing this paper. JLC was funded by a Pre-Doctoral Fellowship in Pharmaceutics from the PhRMA Foundation. The authors would also like to thank NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879, IIP-1540011 and industrial contributions) forfinancial support. Additionally, this material is based upon work supported by the National Science Foundation under Grant No.Grant No. 1710453. Funding Information: The authors would like to thank Carl Huetteman for valuable discussions and assistance editing this paper. JLC was funded by a Pre-Doctoral Fellowship in Pharmaceutics from the PhRMA Foundation. The authors would also like to thank NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879, IIP-1540011 and industrial contributions) forfinancial support. Additionally, this material is based upon work supported by the National Science Foundation under Grant No.Grant No. 1710453. Publisher Copyright: © 2020 Informa UK Limited, trading as Taylor & Francis Group.

PY - 2020/12/10

Y1 - 2020/12/10

N2 - Magnesium stearate (MgSt) is a widely used pharmaceutical lubricant in tablet manufacturing. However, batch-to-batch variability in hydrate form and surface area can lead to inconsistency in tablet performance. In this work, several unique MgSt samples were studied: traditional monohydrate samples with high surface area, dihydrate forms with high and low surface area, and disordered forms with low and medium water content. The effects of solid-state form and particle properties on lubrication efficiency, tabletability and dissolution were studied for tablets in a model direct compression formulation. It was found that the monohydrate and dihydrate forms had good lubrication efficiency compared to the disordered form, while the disordered form had the best tabletability. The dissolution rate correlated with surface area, where slower dissolution rates corresponded with higher MgSt surface areas. The dihydrate sample with lower surface area had the best performance for this model formulation, in terms of lubrication efficiency, tabletability and dissolution. Overall, it is concluded that the choice of the most appropriate grade of MgSt for a particular formulation depends on a comprehensive evaluation of the impact of MgSt properties on lubrication efficiency, tabletability and dissolution.

AB - Magnesium stearate (MgSt) is a widely used pharmaceutical lubricant in tablet manufacturing. However, batch-to-batch variability in hydrate form and surface area can lead to inconsistency in tablet performance. In this work, several unique MgSt samples were studied: traditional monohydrate samples with high surface area, dihydrate forms with high and low surface area, and disordered forms with low and medium water content. The effects of solid-state form and particle properties on lubrication efficiency, tabletability and dissolution were studied for tablets in a model direct compression formulation. It was found that the monohydrate and dihydrate forms had good lubrication efficiency compared to the disordered form, while the disordered form had the best tabletability. The dissolution rate correlated with surface area, where slower dissolution rates corresponded with higher MgSt surface areas. The dihydrate sample with lower surface area had the best performance for this model formulation, in terms of lubrication efficiency, tabletability and dissolution. Overall, it is concluded that the choice of the most appropriate grade of MgSt for a particular formulation depends on a comprehensive evaluation of the impact of MgSt properties on lubrication efficiency, tabletability and dissolution.

KW - Magnesium stearate

KW - compaction

KW - dissolution

KW - ejection force

KW - lubrication

KW - solid-state NMR

KW - tensile strength

UR - http://www.scopus.com/inward/record.url?scp=85099268140&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85099268140&partnerID=8YFLogxK

U2 - 10.1080/10837450.2020.1839763

DO - 10.1080/10837450.2020.1839763

M3 - Article

C2 - 33267700

AN - SCOPUS:85099268140

SN - 1083-7450

VL - 26

SP - 150

EP - 156

JO - Pharmaceutical Development and Technology

JF - Pharmaceutical Development and Technology

IS - 2

ER -

The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution

Abstract

Bibliographical note

Keywords

PubMed: MeSH publication types

Publisher link

Find It

Other files and links

Fingerprint

Cite this