Low dose lipid formulations

effects on gastric emptying and biliary secretion

Greg A Kossena, William N Charman, Clive Wilson, Bridget O'Mahony, Blythe Lindsay, John M Hempenstall, Christopher L Davison, Patrick J Crowley, Christopher J. H Porter

Research output: Contribution to journalArticle

66 Citations (Scopus)

Abstract

Food stimulates changes to gastrointestinal secretion and motility patterns, however, the effect of smaller quantities of lipid, such as that contained in a lipid-based drug formulation, has not been detailed. This study aimed to examine the effects of small quantities of lipid on gastric emptying and biliary secretion.
The influence of oral administration of three lipid-based formulations and a negative control formulation on gastric emptying and biliary secretion was evaluated in 16 healthy male subjects using gamma scintigraphy, ultrasonography and duodenal aspiration.
Low quantities (2 g) of long chain lipid stimulated gall bladder contraction and elevated intestinal bile salt, phospholipid and cholesterol levels. Changes in gastric emptying were also evident, although these did not reach statistical significance. Administration of a similar quantity of medium chain lipid, however, had little effect on gastric emptying and gallbladder contraction and did not stimulate appreciable increases in intestinal concentrations of biliary-derived lipids.
The quantities of long chain lipid that might be administered in a pharmaceutical formulation stimulate gallbladder contraction and elevate intestinal levels of bile salt and phospholipid. This effect is a likely contributor to the ability of lipid based formulations to enhance the absorption of poorly water-soluble drugs.
Original languageEnglish
Pages (from-to)2084-2096
Number of pages12
JournalPharmaceutical Research
Volume24
Issue number11
DOIs
Publication statusPublished - Nov 2007

Fingerprint

Gastric Emptying
Lipids
Drug Compounding
Gallbladder
Bile Acids and Salts
Phospholipids
Ultrasonography
Gastrointestinal Motility
Radionuclide Imaging
Pharmaceutical Preparations
Oral Administration
Healthy Volunteers
Urinary Bladder
Cholesterol
Food
Water

Keywords

  • biliary secretion
  • solubilisation
  • poorly water soluble-drug
  • lipid-based formulations
  • gastric transit
  • gamma scintigraphy
  • drug formulation
  • drug absorption

Cite this

Kossena, G. A., Charman, W. N., Wilson, C., O'Mahony, B., Lindsay, B., Hempenstall, J. M., ... Porter, C. J. H. (2007). Low dose lipid formulations: effects on gastric emptying and biliary secretion. Pharmaceutical Research, 24(11), 2084-2096. https://doi.org/10.1007/s11095-007-9363-8
Kossena, Greg A ; Charman, William N ; Wilson, Clive ; O'Mahony, Bridget ; Lindsay, Blythe ; Hempenstall, John M ; Davison, Christopher L ; Crowley, Patrick J ; Porter, Christopher J. H. / Low dose lipid formulations : effects on gastric emptying and biliary secretion. In: Pharmaceutical Research. 2007 ; Vol. 24, No. 11. pp. 2084-2096.
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Kossena, GA, Charman, WN, Wilson, C, O'Mahony, B, Lindsay, B, Hempenstall, JM, Davison, CL, Crowley, PJ & Porter, CJH 2007, 'Low dose lipid formulations: effects on gastric emptying and biliary secretion', Pharmaceutical Research, vol. 24, no. 11, pp. 2084-2096. https://doi.org/10.1007/s11095-007-9363-8

Low dose lipid formulations : effects on gastric emptying and biliary secretion. / Kossena, Greg A; Charman, William N; Wilson, Clive; O'Mahony, Bridget; Lindsay, Blythe; Hempenstall, John M; Davison, Christopher L; Crowley, Patrick J; Porter, Christopher J. H.

In: Pharmaceutical Research, Vol. 24, No. 11, 11.2007, p. 2084-2096.

Research output: Contribution to journalArticle

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T2 - effects on gastric emptying and biliary secretion

AU - Kossena, Greg A

AU - Charman, William N

AU - Wilson, Clive

AU - O'Mahony, Bridget

AU - Lindsay, Blythe

AU - Hempenstall, John M

AU - Davison, Christopher L

AU - Crowley, Patrick J

AU - Porter, Christopher J. H

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AB - Food stimulates changes to gastrointestinal secretion and motility patterns, however, the effect of smaller quantities of lipid, such as that contained in a lipid-based drug formulation, has not been detailed. This study aimed to examine the effects of small quantities of lipid on gastric emptying and biliary secretion. The influence of oral administration of three lipid-based formulations and a negative control formulation on gastric emptying and biliary secretion was evaluated in 16 healthy male subjects using gamma scintigraphy, ultrasonography and duodenal aspiration. Low quantities (2 g) of long chain lipid stimulated gall bladder contraction and elevated intestinal bile salt, phospholipid and cholesterol levels. Changes in gastric emptying were also evident, although these did not reach statistical significance. Administration of a similar quantity of medium chain lipid, however, had little effect on gastric emptying and gallbladder contraction and did not stimulate appreciable increases in intestinal concentrations of biliary-derived lipids. The quantities of long chain lipid that might be administered in a pharmaceutical formulation stimulate gallbladder contraction and elevate intestinal levels of bile salt and phospholipid. This effect is a likely contributor to the ability of lipid based formulations to enhance the absorption of poorly water-soluble drugs.

KW - biliary secretion

KW - solubilisation

KW - poorly water soluble-drug

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KW - gastric transit

KW - gamma scintigraphy

KW - drug formulation

KW - drug absorption

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