Low dose lipid formulations: effects on gastric emptying and biliary secretion.
OBJECTIVE
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.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Kossena
Greg A
GA
Department of Pharmaceutics, Victorian College of Pharmacy, Monash University, Melbourne, Victoria, 3052, Australia.
Charman
William N
WN
Wilson
Clive G
CG
O'Mahony
Bridget
B
Lindsay
Blythe
B
Hempenstall
John M
JM
Davison
Christopher L
CL
Crowley
Patrick J
PJ
Porter
Christopher J H
CJ
D001646:Bile / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D004386:Duodenum / Q000378:metabolism; D005704:Gallbladder / Q000502:physiology; D005746:Gastric Emptying / Q000187:drug effects*; D006801:Humans; D008055:Lipids / Q000008:administration & dosage* / Q000032:analysis; D008297:Male; D016284:Technetium Tc 99m Pentetate
D008055:Lipids; D016284:Technetium Tc 99m Pentetate