Gastric emptying-limited oral absorption of alpha-linolenic acid administered as a milk fat-globule membrane (MFGM) emulsion in rats.
As a study to assess the potential application of milk fat-globule membrane (MFGM), which is of natural origin and expected to be a safer alternative to synthetic emulsifiers, to pharmaceutical dosage forms, the oral absorption of alpha-linolenic acid was evaluated by the analysis of gastrointestinal disposition after oral administration as an MFGM emulsion to rats. A linear model incorporated with first-order gastric emptying followed by first-order intestinal absorption was fitted to the data of the remaining fraction of alpha-linolenic acid versus time profiles for the stomach and small intestine to estimate the rate constants of gastric emptying (kg) and intestinal absorption (ka). The ka (0.045 min-1) was about 4 times larger than the kg (0.011 min-1). The kg was comparable to the apparent oral absorption rate constant estimated by the pharmacokinetic analysis of plasma concentration data. These results suggest that the oral absorption of alpha-linolenic acid administered as MFGM emulsion is gastric emptying-limited and, hence, any change in the intestinal absorption process would only modestly affect its oral absorption.
Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.
H
H
Yuasa
M
M
Sekiya
S
S
Ozeki
J
J
Watanabe
D000818:Animals; D002463:Cell Membrane Permeability; D004655:Emulsions; D005223:Fats / Q000737:chemistry*; D005746:Gastric Emptying / Q000502:physiology*; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000378:metabolism; D007444:Inulin; D008297:Male; D008892:Milk / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D017962:alpha-Linolenic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics*
D004655:Emulsions; D005223:Fats; D017962:alpha-Linolenic Acid; D007444:Inulin