Enhancement of the intestinal absorption of a cyclosporine derivative by milk fat globule membrane.
A cyclosporine derivative, dihydrocyclosporine D, was used for the evaluation of milk fat globule membrane (MFGM) as an emulsifier of lipophilic cyclopeptides. As compared with olive oil formulation, MFGM emulsion significantly enhanced the blood and lymphatic fluid concentrations of the cyclosporine derivative after intraduodenal dosing in rats. Thus, it was suggested that MFGM can be used as an intestinal absorption enhancer of cyclosporines.
Sato
H
H
Department of Hospital Pharmacy, Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
Liu
H X
HX
Adachi
I
I
Ueno
M
M
Lemaire
M
M
Horikoshi
I
I
D000818:Animals; D003524:Cyclosporins / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004042:Dietary Fats, Unsaturated / Q000378:metabolism*; D016503:Drug Delivery Systems; D004386:Duodenum / Q000187:drug effects; D004655:Emulsions; D005223:Fats / Q000737:chemistry / Q000378:metabolism; D005224:Fats, Unsaturated / Q000737:chemistry; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D008562:Membrane Glycoproteins / Q000494:pharmacology*; D008823:Micelles; D008892:Milk / Q000378:metabolism; D018396:Mucin-1; D009077:Mucins / Q000494:pharmacology*; D000069463:Olive Oil; D010938:Plant Oils / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar
D003524:Cyclosporins; D004042:Dietary Fats, Unsaturated; D004655:Emulsions; D005223:Fats; D005224:Fats, Unsaturated; D008562:Membrane Glycoproteins; D008823:Micelles; D018396:Mucin-1; D009077:Mucins; D000069463:Olive Oil; D010938:Plant Oils; C041326:dihydrocyclosporin D