Enhanced absorption of indomethacin after oral or rectal administration ofa self-emulsifying system containing indomethacin to rats

Authors
Citation
Jy. Kim et Ys. Ku, Enhanced absorption of indomethacin after oral or rectal administration ofa self-emulsifying system containing indomethacin to rats, INT J PHARM, 194(1), 2000, pp. 81-89
Citations number
11
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Pharmacology & Toxicology
Journal title
INTERNATIONAL JOURNAL OF PHARMACEUTICS
ISSN journal
0378-5173 → ACNP
Volume
194
Issue
1
Year of publication
2000
Pages
81 - 89
Database
ISI
SICI code
0378-5173(20000120)194:1<81:EAOIAO>2.0.ZU;2-E
Abstract
A self-emulsifying system (SES), a mixture of an oil and a surfactant which forms an oil-in-water emulsion, is expected to improve the in vitro drug d issolution and enhance the in vivo drug absorption. In this study, a poorly water-soluble drug, indomethacin (IDM) was incorporated into the SES to in crease bioavailability. The SES with 30% of Tween 85 and 70%: of ethyl olea te, EO (w/w) was selected as an optimized formulation (high drug loading, l ow surfactant concentration. and small particle size). After an oral admini stration of the SES containing IDM and IDM suspension, (IDM was suspended i n methyl cellulose), 22.5 mg/kg as IDM, to rats, the area under the plasma concentration-time curve from time zero to the last measured time in plasma , 12 h (AUC(0 12 h)) was significantly greater (57% increase) in the SES, s uggesting that oral absorption of IDM increased significantly by the SES. A fter a rectal administration of gelatin hollow type suppositories, filled w ith the SES containing IDM and IDM powder physically mixed with the SES, 22 .5 mg/kg, to rats, the AUG(0 12 h) also increased significantly (41% increa se) by the SES, suggesting that rectal absorption of IDM also increased sig nificantly by the SES. (C) 2000 Elsevier Science B.V. All rights reserved.