Is bisacodyl absorbed at all from suppositories in man?
A HPLC procedure was developed to determine free BHPM in human plasma and urine after prior deconjugation of its glucuronides with glucuronidase. A single dose administration of a 10 mg bisacodyl suppository from Glaxo Wellcome, Poznań (Poland) to 16 volunteers each resulted in its low active metabolite (BHPM) plasma levels (10-55 microgram l(-1)) according to general assumptions. Its prompt laxative effect appeared within 56.6+/-10.8 min. The calculated serum half-life time of BHPM glucuronide excretion in urine was approximately 7.32+/-0.99 h. BHPM was excreted in urine in only 3. 36+/-0.52% if compared with the above bisacodyl rectal dose administered. Any relationship between BHPM plasma and/or urine levels and its laxative action does not occur. These results confirm the thesis that the laxative action of bisacodyl suppositories is initiated through a direct interaction of the drug in the rectum.
Flig
E
E
Department of Physical Chemistry, K. Marcinkowski University of Medical Sciences, 6 Swiecickiego Street, 60 781, Poznań, Poland.
Hermann
T W
TW
Zabel
M
M
D000293:Adolescent; D000328:Adult; D001726:Bisacodyl / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D002400:Cathartics / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D003672:Defecation / Q000187:drug effects; D005260:Female; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D016032:Randomized Controlled Trials as Topic; D012007:Rectum / Q000187:drug effects / Q000378:metabolism*; D013488:Suppositories
D002400:Cathartics; D013488:Suppositories; D001726:Bisacodyl