Site of drug absorption after oral administration: Assessment of membrane permeability and luminal concentration of drugs in each segment of gastrointestinal tract

2006 ◽  
Vol 29 (3-4) ◽  
pp. 240-250 ◽  
Author(s):  
Yoshie Masaoka ◽  
Yusuke Tanaka ◽  
Makoto Kataoka ◽  
Shinji Sakuma ◽  
Shinji Yamashita
1987 ◽  
Vol 15 (3) ◽  
pp. 225-239 ◽  
Author(s):  
Yves Plusquellec ◽  
G. Campistron ◽  
S. Staveris ◽  
J. Barre ◽  
L. Jung ◽  
...  

Amino Acids ◽  
2013 ◽  
Vol 45 (5) ◽  
pp. 1169-1177 ◽  
Author(s):  
Jun Zhang ◽  
Yulong Yin ◽  
Xu Gang Shu ◽  
Tiejun Li ◽  
Fengna Li ◽  
...  

1985 ◽  
Vol 19 (S2) ◽  
pp. 107S-112S ◽  
Author(s):  
N Vidon ◽  
D Evard ◽  
J Godbillon ◽  
M Rongier ◽  
M Duval ◽  
...  

1998 ◽  
Vol 42 (10) ◽  
pp. 2492-2494 ◽  
Author(s):  
Naoki Nagahara ◽  
Yohko Akiyama ◽  
Masafumi Nakao ◽  
Mayumi Tada ◽  
Megumi Kitano ◽  
...  

ABSTRACT In an effort to augment the anti-Helicobacter pylorieffect of amoxicillin, mucoadhesive microspheres, which have the ability to reside in the gastrointestinal tract for an extended period, were prepared. The microspheres contained the antimicrobial agent and an adhesive polymer (carboxyvinyl polymer) powder dispersed in waxy hydrogenated castor oil. The percentage of amoxicillin remaining in the stomach both 2 and 4 h after oral administration of the mucoadhesive microspheres to Mongolian gerbils under fed conditions was about three times higher than that after administration in the form of a 0.5% methylcellulose suspension. The in vivo clearance ofH. pylori following oral administration of the mucoadhesive microspheres and the 0.5% methylcellulose suspension to infected Mongolian gerbils was examined under fed conditions. The mucoadhesive microspheres and the 0.5% methylcellulose suspension both showed anti-H. pylori effects in this experimental model of infection, but the required dose of amoxicillin was effectively reduced by a factor of 10 when the mucoadhesive microspheres were used. In conclusion, the mucoadhesive microspheres more effectively cleared H. pylori from the gastrointestinal tract than the 0.5% methylcellulose suspension due to the prolonged gastrointestinal residence time resulting from mucoadhesion. A dosage form consisting of mucoadhesive microspheres containing an appropriate antimicrobial agent should be useful for the eradication of H. pylori.


1986 ◽  
Vol 251 (3) ◽  
pp. G332-G340 ◽  
Author(s):  
J. A. Fix ◽  
K. Engle ◽  
P. A. Porter ◽  
P. S. Leppert ◽  
S. J. Selk ◽  
...  

Acylcarnitines were tested as potential absorption-enhancing agents for drugs that are poorly absorbed from the gastrointestinal tract. Urethan-anesthetized Sprague-Dawley rats and conscious Beagle dogs were used. Palmitoyl-DL-carnitine was the most effective acylcarnitine tested, although significant increases in drug absorption were observed with acylcarnitines containing C12 through C18 fatty acid chains. Palmitoyl-DL-carnitine afforded significant increases in the absorption of cefoxitin, gentamicin, cytarabine, somatostatin analogue, and alpha-methyldopa. The response to palmitoyl-DL-carnitine was concentration dependent and reversible within 60-120 min. Histological examination of the intestinal tissue revealed no apparent change in mucosal structural integrity at doses of palmitoyl-DL-carnitine that resulted in increased drug absorption. The acylcarnitines were effective in increasing drug absorption from the small intestine and the rectal compartment of both rats and dogs. The data also demonstrated effectiveness with aqueous and solid dosage forms (Witepsol H-15 suppositories). The data suggest that acylcarnitines may be effective and safe absorption-enhancing agents for a variety of drugs.


1985 ◽  
Vol 19 (S2) ◽  
pp. 113S-118S ◽  
Author(s):  
J Godbillon ◽  
D Evard ◽  
N Vidon ◽  
M Duval ◽  
JP Schoeller ◽  
...  

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