Effects of the physicochemical properties of the emulsion formulation on the bioavailability of ethyl 2-chloro-3-[4-(2-methyl-2-phenylpropyloxy)phenyl]propionate in rats.
The effect of the physicochemical properties of the emulsion formulation on the absorption of ethyl 2-chloro-3-[4-(2-methyl-2-phenylpropyloxy)phenyl]propionate (AL-294) in rats and dogs was studied. When emulsions of different particle sizes were administered to rats, the higher the ratio of Tween-80 to the drug was, the smaller was the particle size and the higher was the absorption. When the emulsions of similar particle size (2 microns) with different Tween-80 ratios were administered to rats, no significant difference was observed in the extent of absorption. The absorption of AL-294 was correlated with the dissolution rate from the oil phase to the aqueous phase but not correlated with the amount of AL-294 solubilized by Tween-80. These results indicate that the absorption of AL-294 from emulsions depends mainly on the particle size in the gastro-intestinal fluid and that Tween-80 serves only to reduce the particle size in the emulsion.
Toguchi
H
H
Research and Development Division, Takeda Chemical Industries, Ltd., Osaka, Japan.
Ogawa
Y
Y
Shimamoto
T
T
D000818:Animals; D001682:Biological Availability; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002994:Clofibrate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D004655:Emulsions; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D010316:Particle Size; D051381:Rats
D004655:Emulsions; D000960:Hypolipidemic Agents; C067636:AL 294; D002994:Clofibrate