Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy

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

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC>MG>DS tablets. The mean in vivo onset time for all tablets (DC: 6.7±3.8 min, MG: 18.3±8.1 min, DS: 67±18.9 min) did not differ significantly from in vitro onset time (DC: 5.3±1 min, MG: 16.8±3.9 min, DS: 61.8±4.7 min). The mean in vivo completion times were found to be 36.6±9.7 (DC tablets), 70±18.3 min (MG tablets) and 192.5±39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.
Original languageEnglish
Pages (from-to)148-157
Number of pages10
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume77
Issue number1
DOIs
Publication statusPublished - Jan 2011

Fingerprint

Radionuclide Imaging
Tablets
In Vitro Techniques
Charcoal
Healthy Volunteers
Water

Keywords

  • adult
  • cellulose
  • cross-over studies
  • delayed-action preparations
  • drug compounding
  • drug delivery systems
  • excipients
  • fatty acids
  • gastrointestinal transit
  • humans
  • kinetics
  • male
  • middle aged
  • radionuclide imaging
  • solubility
  • tablets
  • technetium Tc 99m pentetate
  • young adult

Cite this

Ghimire, Manish ; Hodges, Lee Ann ; Band, Janet ; Lindsay, Blythe ; O'Mahony, Bridget ; McInnes, Fiona J ; Mullen, Alexander B ; Stevens, Howard N E. / Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy. In: European Journal of Pharmaceutics and Biopharmaceutics . 2011 ; Vol. 77, No. 1. pp. 148-157.
@article{d57009123032472ca047c94a0f00c075,
title = "Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy",
abstract = "In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC>MG>DS tablets. The mean in vivo onset time for all tablets (DC: 6.7±3.8 min, MG: 18.3±8.1 min, DS: 67±18.9 min) did not differ significantly from in vitro onset time (DC: 5.3±1 min, MG: 16.8±3.9 min, DS: 61.8±4.7 min). The mean in vivo completion times were found to be 36.6±9.7 (DC tablets), 70±18.3 min (MG tablets) and 192.5±39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.",
keywords = "adult, cellulose, cross-over studies, delayed-action preparations, drug compounding, drug delivery systems, excipients, fatty acids, gastrointestinal transit, humans, kinetics, male, middle aged, radionuclide imaging, solubility, tablets, technetium Tc 99m pentetate, young adult",
author = "Manish Ghimire and Hodges, {Lee Ann} and Janet Band and Blythe Lindsay and Bridget O'Mahony and McInnes, {Fiona J} and Mullen, {Alexander B} and Stevens, {Howard N E}",
note = "Copyright {\circledC} 2010 Elsevier B.V. All rights reserved.",
year = "2011",
month = "1",
doi = "10.1016/j.ejpb.2010.10.005",
language = "English",
volume = "77",
pages = "148--157",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
number = "1",

}

Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy. / Ghimire, Manish; Hodges, Lee Ann; Band, Janet; Lindsay, Blythe; O'Mahony, Bridget; McInnes, Fiona J; Mullen, Alexander B; Stevens, Howard N E.

In: European Journal of Pharmaceutics and Biopharmaceutics , Vol. 77, No. 1, 01.2011, p. 148-157.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy

AU - Ghimire, Manish

AU - Hodges, Lee Ann

AU - Band, Janet

AU - Lindsay, Blythe

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 - 2011/1

Y1 - 2011/1

N2 - In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC>MG>DS tablets. The mean in vivo onset time for all tablets (DC: 6.7±3.8 min, MG: 18.3±8.1 min, DS: 67±18.9 min) did not differ significantly from in vitro onset time (DC: 5.3±1 min, MG: 16.8±3.9 min, DS: 61.8±4.7 min). The mean in vivo completion times were found to be 36.6±9.7 (DC tablets), 70±18.3 min (MG tablets) and 192.5±39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.

AB - In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC>MG>DS tablets. The mean in vivo onset time for all tablets (DC: 6.7±3.8 min, MG: 18.3±8.1 min, DS: 67±18.9 min) did not differ significantly from in vitro onset time (DC: 5.3±1 min, MG: 16.8±3.9 min, DS: 61.8±4.7 min). The mean in vivo completion times were found to be 36.6±9.7 (DC tablets), 70±18.3 min (MG tablets) and 192.5±39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.

KW - adult

KW - cellulose

KW - cross-over studies

KW - delayed-action preparations

KW - drug compounding

KW - drug delivery systems

KW - excipients

KW - fatty acids

KW - gastrointestinal transit

KW - humans

KW - kinetics

KW - male

KW - middle aged

KW - radionuclide imaging

KW - solubility

KW - tablets

KW - technetium Tc 99m pentetate

KW - young adult

U2 - 10.1016/j.ejpb.2010.10.005

DO - 10.1016/j.ejpb.2010.10.005

M3 - Article

VL - 77

SP - 148

EP - 157

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

IS - 1

ER -