The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus

Lance R. Shaw, William J. Irwin, Tim J. Grattan, Barbara R. Conway

Research output: Contribution to journalArticle

25 Citations (Scopus)

Abstract

The aim of this study was to examine the diffusion of commonly administered analgesics, ibuprofen and paracetamol, through gastric mucus. As ibuprofen and paracetamol are often formulated with alkalising excipients, or are commonly co-administered with antacids that have been demonstrated to alter their absorption, diffusion was also studied in the presence of a range of soluble and insoluble antacids or buffering agents. The effect of pH, which has been demonstrated to modify the properties of mucus, was also studied. Mucus was a significant barrier to diffusion for both drugs, compared to an unstirred aqueous layer with diffusion rates significantly lower in the presence of a mucus barrier for both drugs; ibuprofen diffusion also demonstrated a significant increase in the lag time. Paracetamol diffusion was not significantly affected by addition of any antacid, whereas ibuprofen rates were affected and the diffusion lag time for ibuprofen was significantly reduced in all cases. Isolated increases in pH increased the rate and reduced the lag time for ibuprofen diffusion. It was shown that mucus acts as a passive barrier in the case of paracetamol diffusion, and an interactive barrier to ibuprofen diffusion. Changes in mucus viscosity at different pH values may be responsible for the observed changes in ibuprofen diffusion rate.

Original languageEnglish
Pages (from-to)145-154
Number of pages10
JournalInternational Journal of Pharmaceutics
Volume290
Issue number1-2
DOIs
Publication statusPublished - 16 Feb 2005
Externally publishedYes

Fingerprint

Ibuprofen
Excipients
Mucus
Acetaminophen
Stomach
Antacids
Viscosity
Pharmaceutical Preparations
Analgesics

Cite this

Shaw, Lance R. ; Irwin, William J. ; Grattan, Tim J. ; Conway, Barbara R. / The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus. In: International Journal of Pharmaceutics. 2005 ; Vol. 290, No. 1-2. pp. 145-154.
@article{7b01100fd7c74dd6b4dbae6643b020e0,
title = "The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus",
abstract = "The aim of this study was to examine the diffusion of commonly administered analgesics, ibuprofen and paracetamol, through gastric mucus. As ibuprofen and paracetamol are often formulated with alkalising excipients, or are commonly co-administered with antacids that have been demonstrated to alter their absorption, diffusion was also studied in the presence of a range of soluble and insoluble antacids or buffering agents. The effect of pH, which has been demonstrated to modify the properties of mucus, was also studied. Mucus was a significant barrier to diffusion for both drugs, compared to an unstirred aqueous layer with diffusion rates significantly lower in the presence of a mucus barrier for both drugs; ibuprofen diffusion also demonstrated a significant increase in the lag time. Paracetamol diffusion was not significantly affected by addition of any antacid, whereas ibuprofen rates were affected and the diffusion lag time for ibuprofen was significantly reduced in all cases. Isolated increases in pH increased the rate and reduced the lag time for ibuprofen diffusion. It was shown that mucus acts as a passive barrier in the case of paracetamol diffusion, and an interactive barrier to ibuprofen diffusion. Changes in mucus viscosity at different pH values may be responsible for the observed changes in ibuprofen diffusion rate.",
keywords = "Antacids, Diffusion, Ibuprofen, Mucus, Paracetamol",
author = "Shaw, {Lance R.} and Irwin, {William J.} and Grattan, {Tim J.} and Conway, {Barbara R.}",
year = "2005",
month = "2",
day = "16",
doi = "10.1016/j.ijpharm.2004.11.028",
language = "English",
volume = "290",
pages = "145--154",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus. / Shaw, Lance R.; Irwin, William J.; Grattan, Tim J.; Conway, Barbara R.

In: International Journal of Pharmaceutics, Vol. 290, No. 1-2, 16.02.2005, p. 145-154.

Research output: Contribution to journalArticle

TY - JOUR

T1 - The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus

AU - Shaw, Lance R.

AU - Irwin, William J.

AU - Grattan, Tim J.

AU - Conway, Barbara R.

PY - 2005/2/16

Y1 - 2005/2/16

N2 - The aim of this study was to examine the diffusion of commonly administered analgesics, ibuprofen and paracetamol, through gastric mucus. As ibuprofen and paracetamol are often formulated with alkalising excipients, or are commonly co-administered with antacids that have been demonstrated to alter their absorption, diffusion was also studied in the presence of a range of soluble and insoluble antacids or buffering agents. The effect of pH, which has been demonstrated to modify the properties of mucus, was also studied. Mucus was a significant barrier to diffusion for both drugs, compared to an unstirred aqueous layer with diffusion rates significantly lower in the presence of a mucus barrier for both drugs; ibuprofen diffusion also demonstrated a significant increase in the lag time. Paracetamol diffusion was not significantly affected by addition of any antacid, whereas ibuprofen rates were affected and the diffusion lag time for ibuprofen was significantly reduced in all cases. Isolated increases in pH increased the rate and reduced the lag time for ibuprofen diffusion. It was shown that mucus acts as a passive barrier in the case of paracetamol diffusion, and an interactive barrier to ibuprofen diffusion. Changes in mucus viscosity at different pH values may be responsible for the observed changes in ibuprofen diffusion rate.

AB - The aim of this study was to examine the diffusion of commonly administered analgesics, ibuprofen and paracetamol, through gastric mucus. As ibuprofen and paracetamol are often formulated with alkalising excipients, or are commonly co-administered with antacids that have been demonstrated to alter their absorption, diffusion was also studied in the presence of a range of soluble and insoluble antacids or buffering agents. The effect of pH, which has been demonstrated to modify the properties of mucus, was also studied. Mucus was a significant barrier to diffusion for both drugs, compared to an unstirred aqueous layer with diffusion rates significantly lower in the presence of a mucus barrier for both drugs; ibuprofen diffusion also demonstrated a significant increase in the lag time. Paracetamol diffusion was not significantly affected by addition of any antacid, whereas ibuprofen rates were affected and the diffusion lag time for ibuprofen was significantly reduced in all cases. Isolated increases in pH increased the rate and reduced the lag time for ibuprofen diffusion. It was shown that mucus acts as a passive barrier in the case of paracetamol diffusion, and an interactive barrier to ibuprofen diffusion. Changes in mucus viscosity at different pH values may be responsible for the observed changes in ibuprofen diffusion rate.

KW - Antacids

KW - Diffusion

KW - Ibuprofen

KW - Mucus

KW - Paracetamol

UR - http://www.scopus.com/inward/record.url?scp=12344314225&partnerID=8YFLogxK

U2 - 10.1016/j.ijpharm.2004.11.028

DO - 10.1016/j.ijpharm.2004.11.028

M3 - Article

VL - 290

SP - 145

EP - 154

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -