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.
Liu
Chen
C
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, People's Republic of China.
Zhu
Saijie
S
Zhou
Ying
Y
Wei
Yupu
Y
Pei
Yuanying
Y
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