Nasal absorption and disposition of prostaglandin E1 and E2 in the rat

摘要

Nasal absorption and the disposition of prostaglandin(PG) E1 and E2 were evaluated in this study. The totalbody clearances of PGE1 and PGE2 were and 8.8 mL/minand 85.8 mL/min, with plasma half life of 28.3 sec and23.8 sec, respectively. Following nasal application, theprofiles showed the peak at 5 min and the concentrationwas decreased thereafter. Bioavailability was 16.1 % forPGE1 and 65.8 % for PGE2. In vitro permeation studyusing Caco-2 cells showed that the permeabilities are 5.0×10-6 cm/sec (PGE1) and 3.6×10-6 cm/sec, respectively,which are comparable to the previously reported relationof nasal bioavailability to Caco-2 permeability. In vitrostudy on the degradation of PGs in the cerebrospinal fluid(CSF) indicated that both PGs are stable in the CSF.These findings are important information for thedevelopment of nasal delivery system of PGs to the CSFand the brain.