In situ intestinal absorption of cyclosporine A solid dispersion in rats.
Effects of concentration of Polyoxyethylene (40) stearate, Na(+) and P-gp inhibitor on cyclosporin A (CyA-SD) absorption were investigated by in situ circulation method. The results showed that the absorption of CyA increased linearly with its concentration, indicating a passive diffusion process was dominated. CyA absorption decreased with the carrier concentration. The concentration of Na(+) didn't influence the drug absorbed (P > 0.05). The P-gp inhibitor enhanced the CyA absorption significantly (P < 0.05). The passive diffusion process during the intestinal absorption indicated that the solubility enhancement of CyA is one of the mechanisms for the absorption of this water insoluble drug.
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, People's Republic of China.
Chen
C
Liu
Saijie
S
Zhu
Ying
Y
Zhou
Yupu
Y
Wei
Yuanying
Y
Pei
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D016572:Cyclosporine / Q000737:chemistry* / Q000493:pharmacokinetics*; D004058:Diffusion; D004337:Drug Carriers; D007166:Immunosuppressive Agents / Q000737:chemistry* / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D008297:Male; D011092:Polyethylene Glycols; D011802:Quinidine / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004337:Drug Carriers; D007166:Immunosuppressive Agents; C526284:polyoxyethylene 40 stearate; D011092:Polyethylene Glycols; D016572:Cyclosporine; D011802:Quinidine