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.

journal_name

Int J Pharm

authors

Shaw LR,Irwin WJ,Grattan TJ,Conway BR

doi

10.1016/j.ijpharm.2004.11.028

keywords:

subject

Has Abstract

pub_date

2005-02-16 00:00:00

pages

145-54

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(04)00708-2

journal_volume

290

pub_type

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