|
KMID : 0617319940040010047
|
|
Journal of Pharmacetical Sceiences Ewha Womans University
1994 Volume.4 No. 1 p.47 ~ p.52
|
|
|
Bioavailability of Gentamicin from a New Rectal Dosage Vehicle in Rabbits
|
|
WATANABE, YOSHITERU
MATSUMOTO, YOSHIAKI/KIRIYAMA, MIYUKI/KAKUHARI, TAKESHI/MATSUMOTO, MITSUO/KU, YOUNG-SOON/OBAYASHI, MASAHIKO
|
|
|
Abstract
|
|
|
|
The bioavailability of gentamicin (GM), a model drug of aminoglycoside antibiotics, from a new rectal dosage vehicle, hollow-type suppositories containing GM and fatty acids (sodium salts) with different acyl chain lengths in their chemical structure, was investigated in rabbits. Fatty acids with chain lengths varying from 6 to 12 carbon atoms (C_6-C_12) enhanced GM absorption in the rectum. Consequently, it was observed that an optimum length of the acyl chain of between C_8 and C_10 enhanced the extent of GM absorption. The absorption-enhancing effect of valproic acid (VPA), a C_8 branched-chain molecule, was less than that of octanoic acid (OA), a C_8 straight-chain molecule. Branching of the acyl chain of the fatty acid seems to decrease the absorption-enhancing effect. This study demonstrates that the C_8- C_10 acyl group appears to play an essential role in the mechanism of GM absorption enhancement. The hollow-type suppositories containing GM and fatty acids, particularly decanoic acid (DA) and OA, are one of the most promising and practical dosage vehicles for rectal delivery of aminoglycoside antibiotics such as GM, instead of the use of injection dosage form.
|
|
|
KEYWORD
|
|
|
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|
|
|