In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets

Manish Ghimire, Lee Ann Hodges, Janet Band, Bridget O'Mahony, Fiona J McInnes, Alexander B Mullen, Howard N E Stevens

Research output: Contribution to journalArticle

42 Citations (Scopus)

Abstract

The purpose of this study was to evaluate and compare the in-vitro and in-vivo erosion profiles of two tablet formulations primarily consisting of hydroxypropylmethylcellulose (HPMC) and lactose. HPMC was used at concentrations below and above the reported values for polymer percolation threshold in controlled release matrix formulations: 20 and 40% (w/w) HPMC. In-vitro erosion behaviour was studied using traditional gravimetric and scintigraphic methods, with radiolabelled charcoal used as a marker to quantify erosion profiles in scintigraphic studies. Six healthy male subjects participated in a randomised crossover scintigraphic erosion study. Both in-vitro and in-vivo erosion profiles determined using the gravimetric and/or scintigraphic method for matrix tablets were dependent upon the concentration of HPMC, and erosion was faster for tablets containing 20% (w/w) HPMC than those containing 40% (w/w) HPMC. Good correlation was found between in-vitro gravimetric and scintigraphic erosion profiles for both tablets. Tablets containing 40% (w/w) HPMC (polymer level above percolation threshold) demonstrated robust in-vivo performance and showed stronger correlation with in-vitro erosion profiles. The study demonstrated that a matrix formulation with a lower concentration of HPMC and higher lactose concentration is more likely to perform poorly in the in-vivo environment.
Original languageEnglish
Pages (from-to)70-75
Number of pages6
JournalJournal of Controlled Release
Volume147
Issue number1
DOIs
Publication statusPublished - 1 Oct 2010

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Tablets
Lactose
Polymers
In Vitro Techniques
Hypromellose Derivatives
Charcoal
Healthy Volunteers

Keywords

  • adult
  • charcoal
  • cross-over studies
  • delayed-action preparations
  • drug carriers
  • drug compounding
  • humans
  • lactose
  • male
  • methylcellulose
  • radionuclide imaging
  • solubility
  • tablets
  • technetium Tc 99m pentetate
  • viscosity
  • young adult

Cite this

Ghimire, Manish ; Hodges, Lee Ann ; Band, Janet ; O'Mahony, Bridget ; McInnes, Fiona J ; Mullen, Alexander B ; Stevens, Howard N E. / In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets. In: Journal of Controlled Release. 2010 ; Vol. 147, No. 1. pp. 70-75.
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abstract = "The purpose of this study was to evaluate and compare the in-vitro and in-vivo erosion profiles of two tablet formulations primarily consisting of hydroxypropylmethylcellulose (HPMC) and lactose. HPMC was used at concentrations below and above the reported values for polymer percolation threshold in controlled release matrix formulations: 20 and 40{\%} (w/w) HPMC. In-vitro erosion behaviour was studied using traditional gravimetric and scintigraphic methods, with radiolabelled charcoal used as a marker to quantify erosion profiles in scintigraphic studies. Six healthy male subjects participated in a randomised crossover scintigraphic erosion study. Both in-vitro and in-vivo erosion profiles determined using the gravimetric and/or scintigraphic method for matrix tablets were dependent upon the concentration of HPMC, and erosion was faster for tablets containing 20{\%} (w/w) HPMC than those containing 40{\%} (w/w) HPMC. Good correlation was found between in-vitro gravimetric and scintigraphic erosion profiles for both tablets. Tablets containing 40{\%} (w/w) HPMC (polymer level above percolation threshold) demonstrated robust in-vivo performance and showed stronger correlation with in-vitro erosion profiles. The study demonstrated that a matrix formulation with a lower concentration of HPMC and higher lactose concentration is more likely to perform poorly in the in-vivo environment.",
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In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets. / Ghimire, Manish; Hodges, Lee Ann; Band, Janet; O'Mahony, Bridget; McInnes, Fiona J; Mullen, Alexander B; Stevens, Howard N E.

In: Journal of Controlled Release, Vol. 147, No. 1, 01.10.2010, p. 70-75.

Research output: Contribution to journalArticle

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T1 - In-vitro and in-vivo erosion profiles of hydroxypropylmethylcellulose (HPMC) matrix tablets

AU - Ghimire, Manish

AU - Hodges, Lee Ann

AU - Band, Janet

AU - O'Mahony, Bridget

AU - McInnes, Fiona J

AU - Mullen, Alexander B

AU - Stevens, Howard N E

N1 - Copyright © 2010 Elsevier B.V. All rights reserved.

PY - 2010/10/1

Y1 - 2010/10/1

N2 - The purpose of this study was to evaluate and compare the in-vitro and in-vivo erosion profiles of two tablet formulations primarily consisting of hydroxypropylmethylcellulose (HPMC) and lactose. HPMC was used at concentrations below and above the reported values for polymer percolation threshold in controlled release matrix formulations: 20 and 40% (w/w) HPMC. In-vitro erosion behaviour was studied using traditional gravimetric and scintigraphic methods, with radiolabelled charcoal used as a marker to quantify erosion profiles in scintigraphic studies. Six healthy male subjects participated in a randomised crossover scintigraphic erosion study. Both in-vitro and in-vivo erosion profiles determined using the gravimetric and/or scintigraphic method for matrix tablets were dependent upon the concentration of HPMC, and erosion was faster for tablets containing 20% (w/w) HPMC than those containing 40% (w/w) HPMC. Good correlation was found between in-vitro gravimetric and scintigraphic erosion profiles for both tablets. Tablets containing 40% (w/w) HPMC (polymer level above percolation threshold) demonstrated robust in-vivo performance and showed stronger correlation with in-vitro erosion profiles. The study demonstrated that a matrix formulation with a lower concentration of HPMC and higher lactose concentration is more likely to perform poorly in the in-vivo environment.

AB - The purpose of this study was to evaluate and compare the in-vitro and in-vivo erosion profiles of two tablet formulations primarily consisting of hydroxypropylmethylcellulose (HPMC) and lactose. HPMC was used at concentrations below and above the reported values for polymer percolation threshold in controlled release matrix formulations: 20 and 40% (w/w) HPMC. In-vitro erosion behaviour was studied using traditional gravimetric and scintigraphic methods, with radiolabelled charcoal used as a marker to quantify erosion profiles in scintigraphic studies. Six healthy male subjects participated in a randomised crossover scintigraphic erosion study. Both in-vitro and in-vivo erosion profiles determined using the gravimetric and/or scintigraphic method for matrix tablets were dependent upon the concentration of HPMC, and erosion was faster for tablets containing 20% (w/w) HPMC than those containing 40% (w/w) HPMC. Good correlation was found between in-vitro gravimetric and scintigraphic erosion profiles for both tablets. Tablets containing 40% (w/w) HPMC (polymer level above percolation threshold) demonstrated robust in-vivo performance and showed stronger correlation with in-vitro erosion profiles. The study demonstrated that a matrix formulation with a lower concentration of HPMC and higher lactose concentration is more likely to perform poorly in the in-vivo environment.

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KW - solubility

KW - tablets

KW - technetium Tc 99m pentetate

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KW - young adult

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EP - 75

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

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