Experimental antidiarrheal activity of a traditionally used medication
, Salicairine(R), was demonstrated in comparison to loperamide by sign
ificant inhibition of castor oil-induced diarrhea in mice (increases i
n hard faeces/total faeces ratio of 38 and 54 and 5 and 54% with respe
ct to controls, at 0.5 and 1 mL/kg and 1 and 2 mg/kg, respectively) an
d bisacodyl-induced increase in large intestine transit in rats (125 a
nd 280 and 210% with respect to controls, at 0.4 and 2 mL/kg Salicairi
ne(R) and 5 mg/kg loperamide, respectively). Salicairine(R) was able t
o reduce contractions of isolated rat duodenum induced by barium chlor
ide and acetylcholine, although not completely (that is about 60%) as
seen with loperamide. Also, it did not change normal gastrointestinal
transit in mice at doses of 0.5 to 1 mL/kg, conversely to loperamide w
hich had a significant effect (decrease of 50%) at 2 mg/kg. Finally, S
alicairine(R) at 0.01 mL/mL, like loperamide at 0.2 mg/mL, significant
ly increased net fluid absorption in rat colon, either in basal condit
ions (30 and 64% respectively) or after a prostaglandin E-1-induced in
crease in net fluid secretion (41 and 35%, respectively). The antidiar
rheal activity of Salicairine(R) is possibly related, at least in part
, to an increase in colon net fluid absorption or a decrease in net fl
uid secretion. (C) 1998 Elsevier, Paris.