Preparation and evaluation of Eudragit gels. III: Rectal gel preparations for sustained release of pentoxifylline.
A novel method was established for the preparation of Eudragit S, Eudragit L, and Eudispert high-viscosity (hv) hydrogel and xerogel preparations containing a medicinal component such as pentoxifylline (an agent that improves cerebral microcirculation). A significant correlation was found between the in vitro mean dissolution time and the in vivo mean residence time of pentoxifylline after rectal administration of these preparations in rabbits. Staying properties of the hydrogel and xerogel preparations in the lower part of the rectum were compared with those of polyethylene glycol 2000 and Witepsol S-55 suppositories in rats, with water-insoluble dye. Eudispert hv hydrogel and xerogel preparations have excellent staying properties in the rectum. The efficacy of Eudispert hv xerogel preparations may be reduced by first passage through the liver after oral administration.
Kim
N S
NS
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Kawata
M
M
Uchida
T
T
Goto
S
S
D000180:Acrylic Resins; D000284:Administration, Oral; D000285:Administration, Rectal; D000818:Animals; D001682:Biological Availability; D005782:Gels; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D007275:Injections, Intravenous; D008099:Liver / Q000378:metabolism; D008297:Male; D010431:Pentoxifylline / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011092:Polyethylene Glycols; D011109:Polymethacrylic Acids; D011817:Rabbits; D012995:Solubility
D000180:Acrylic Resins; D005782:Gels; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D011092:Polyethylene Glycols; D010431:Pentoxifylline